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Isoform-selective Products

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Ras Signaling Pathway

Ras Products

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  • Ras Inhibitors (50)
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  • New Ras Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1314 Zoledronic acid (Zoledronate) Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Cells, 2024, 13(10)862
Cells, 2024, 13(10)862
Cancer Immunol Immunother, 2024, 73(4):62
S8830 Sotorasib (AMG510) Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
Nat Genet, 2024, 10.1038/s41588-024-01948-8
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):6076
S2797 Lonafarnib (SCH66336) Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
J Cell Biol, 2024, 223(1)e202303007
J Cell Biol, 2024, 223(1)e202303007
EMBO Rep, 2024, 25(10):4311-4336
S8707 ARS-1620 ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C and could achieve rapid and sustained in vivo target occupancy to induce tumor regression.
Nat Commun, 2024, 15(1):3741
Cell Death Dis, 2024, 15(1):56
bioRxiv, 2024, 2024.09.26.615226
S5244 Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.
J Immunother Cancer, 2022, 10(12)e005660
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Oncol Lett, 2022, 23(2):51
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Biol Chem, 2023, 299(4):103017
Microbiol Spectr, 2023, 11(4):e0055223
Nat Commun, 2022, 13(1):7113
S8884 Adagrasib (MRTX849) Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
Nat Genet, 2024, 10.1038/s41588-024-01948-8
Nat Commun, 2024, 15(1):6076
Cancer Lett, 2024, 587:216692
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Eur J Cell Biol, 2023, 102(2):151314
Cell Death Differ, 2019, 26(11):2400-2415
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
S8156 ARS-853 ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis.
Sci Rep, 2023, 10.1038/s41598-023-46623-w
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00216-8
SLAS Discov, 2022, S2472-5552(22)12517-7
S8916 BI-3406 BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities.
Mol Oncol, 2024, 10.1002/1878-0261.13725
Sci Adv, 2023, 9(28):eadf4766
Sci Adv, 2023, 9(28):eadf4766
E1051 MRTX1133

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.
Science, 2024, 384(6700):eadk0775
Science, 2024, 384(6700):eadk0850
Cancer Lett, 2024, 604:217258
S8826 BAY-293 BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM.
Int J Mol Sci, 2023, 24(2)997
Clin Cancer Res, 2022, clincanres.4291.2021
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00216-8
S7331 K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
Cancers -Basel), 2023, 15(19)4772
Biomedicines, 2022, 10(3)592
Oncotarget, 2016, 7(9):10064-72
S7606 RBC8 RBC8 is a selective inhibitor of the GTPases RalA and RalB by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases Ras and RhoA.
J Exp Clin Cancer Res, 2022, 41(1):301
Haematologica, 2019, 10.3324/haematol.2019.223024
Oncotarget, 2016, 7(15):20561-73
S8303 Kobe0065 Kobe0065 is an H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Acta Pharm Sin B, 2019, 9(2):294-303
Cell Death Differ, 2019, 10.1038/s41418-019-0416-4
S8499 KRpep-2d KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
J Exp Clin Cancer Res, 2022, 41(1):73
Heliyon, 2022, 8(12):e12518
S8955 Sotorasib (AMG510) racemate Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.
Mol Cancer Ther, 2023, 22(12):1422-1433
Commun Biol, 2021, 4(1):834
Mol Clin Oncol, 2021, 15(1):148
S7607 BQU57 BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
J Adv Res, 2024, S2090-1232(24)00171-1
PLoS One, 2019, 14(4):e0214764
S8959 BI-2852 BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
Eur J Cell Biol, 2023, 102(2):151314
E0135 CID-1067700 (ML282)

CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.
Int J Mol Sci, 2022, 23(24)15834
S7332 K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
E1474 BI-2865 BI-2865 is a none-covalent pan-KRAS Inhibitor. It binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively and inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 ce
S6996 LC-2 LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling.
S0730 (Rac)-Antineoplaston A10 (rac)-Antineoplaston A10 is the racemate of Antineoplaston A10, which is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
S0023 K-Ras-IN-1 K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.
E1187 Divarasib (GDC-6036) Divarasib (GDC-6036, RG6330) is a KRAS G12C inhibitor that binds irreversibly to switch II pocket of KRAS G12C (when in the inactive GDP-bound state) thereby blocking GTP binding and activation.
E1433 LY3537982 (KRAS G12C inhibitor 19) LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the  KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively.
E1578 garsorasib (D-1553 ) Garsorasib (D-1553 ) is a potent and selective oral KRASG12C inhibitor with antitumor activity. It has the potential to treat KRAS G12C-mutated non-small cell lung cancer (NSCLC).
E1606 RMC-6291 RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA).
S3493 APS6-45 APS6-45(Compound 10) is an orally active tumor-calibrated inhibitor (TCI) that inhibits RAS/MAPK signaling and exhibits antitumor activity.
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors.
S7330 6H05 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
S7333 K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
E1858New RMC-7977 RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC).
E1857New TH-Z816 TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide.
E1356New BI-0474 BI-0474 is a potent inhibitor of KRASG12C with an IC50 value of 7.0 nM. It inhibits GDP-KRAS::SOS1 protein-protein interactions. It exhibits anti-proliferative and anti-tumour activity and can be used in cancer research.
E1969New ADT-007 ADT-007 is a potent and orally active pan-RAS inhibitor. ADT-007 effectively targets and suppresses the proliferation of cancer cells harboring mutated or hyper-activated wild-type RAS isozymes. ADT-007 exhibits potent anti-cancer effects.
bioRxiv, 2024, 2024.10.04.616725
E4651New HRS-4642 HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo.
E1056 Opnurasib (JDQ-443) Opnurasib (JDQ-443,NVP-JDQ443) , a potent and selective, orally bioavailable covalent inhibitor of GDP-bound KRASG12C with an IC50 of 0.012 µM for inhibition of c-Raf recruitment.
S6527 Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).
E1597New RMC-6236 RMC-6236 (RAS-IN-2) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS.
E1047 NAV-2729 NAV-2729, an inhibitor of Arf6 activation which directly binds to Arf6, also inhibits all Arf guanine nucleotide exchange factors (ArfGEFs) with a strongest effect against BRAG2 and Arf1 .
S0323 Antineoplaston A10 Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
S5279 Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
E4697New RGT-018 RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer.
E1856New ARS-1323 ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C.
S3853 Perillyl alcohol Perillyl alcohol (Perilla alcohol, Isocarveol) is a monoterpene isolated from the essential oils of lavendin, peppermint, spearmint, cherries, celery seeds, and several other plants.
E1071 ASP2453 ASP2453, a potent, selective and covalent KRAS G12C inhibitor, inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf. ASP2453 is a potential therapeutic agent for KRAS G12C-mutated cancer.
E1157 Pan-RAS-IN-1 Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.
E4700New ML-099 ML099(CID-888706) is a pan-activator of Ras-related GTPases. It enhances GTPase activity by increasing its affinity for guanine nucleotides through binding to an allosteric site between switch regions I and II.
E1962New RMC-9805 RMC-9805(KRAS G12D ON inhibitor) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation.
S8831 MRTX-1257 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.
E1564New BI-2493 BI-2493, a structural analogue of BI-2865, is a highly selective inhibitor of pan-KRAS. BI-2493 attenuates tumor growth and can be used for cancer research.
S1314 Zoledronic acid (Zoledronate) Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Cells, 2024, 13(10)862
Cells, 2024, 13(10)862
Cancer Immunol Immunother, 2024, 73(4):62
S8830 Sotorasib (AMG510) Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
Nat Genet, 2024, 10.1038/s41588-024-01948-8
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):6076
S2797 Lonafarnib (SCH66336) Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
J Cell Biol, 2024, 223(1)e202303007
J Cell Biol, 2024, 223(1)e202303007
EMBO Rep, 2024, 25(10):4311-4336
S8707 ARS-1620 ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C and could achieve rapid and sustained in vivo target occupancy to induce tumor regression.
Nat Commun, 2024, 15(1):3741
Cell Death Dis, 2024, 15(1):56
bioRxiv, 2024, 2024.09.26.615226
S5244 Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.
J Immunother Cancer, 2022, 10(12)e005660
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Oncol Lett, 2022, 23(2):51
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Biol Chem, 2023, 299(4):103017
Microbiol Spectr, 2023, 11(4):e0055223
Nat Commun, 2022, 13(1):7113
S8884 Adagrasib (MRTX849) Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
Nat Genet, 2024, 10.1038/s41588-024-01948-8
Nat Commun, 2024, 15(1):6076
Cancer Lett, 2024, 587:216692
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Eur J Cell Biol, 2023, 102(2):151314
Cell Death Differ, 2019, 26(11):2400-2415
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
S8156 ARS-853 ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis.
Sci Rep, 2023, 10.1038/s41598-023-46623-w
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00216-8
SLAS Discov, 2022, S2472-5552(22)12517-7
S8916 BI-3406 BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities.
Mol Oncol, 2024, 10.1002/1878-0261.13725
Sci Adv, 2023, 9(28):eadf4766
Sci Adv, 2023, 9(28):eadf4766
E1051 MRTX1133

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.
Science, 2024, 384(6700):eadk0775
Science, 2024, 384(6700):eadk0850
Cancer Lett, 2024, 604:217258
S8826 BAY-293 BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM.
Int J Mol Sci, 2023, 24(2)997
Clin Cancer Res, 2022, clincanres.4291.2021
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00216-8
S7331 K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
Cancers -Basel), 2023, 15(19)4772
Biomedicines, 2022, 10(3)592
Oncotarget, 2016, 7(9):10064-72
S7606 RBC8 RBC8 is a selective inhibitor of the GTPases RalA and RalB by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases Ras and RhoA.
J Exp Clin Cancer Res, 2022, 41(1):301
Haematologica, 2019, 10.3324/haematol.2019.223024
Oncotarget, 2016, 7(15):20561-73
S8303 Kobe0065 Kobe0065 is an H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Acta Pharm Sin B, 2019, 9(2):294-303
Cell Death Differ, 2019, 10.1038/s41418-019-0416-4
S8499 KRpep-2d KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
J Exp Clin Cancer Res, 2022, 41(1):73
Heliyon, 2022, 8(12):e12518
S8955 Sotorasib (AMG510) racemate Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.
Mol Cancer Ther, 2023, 22(12):1422-1433
Commun Biol, 2021, 4(1):834
Mol Clin Oncol, 2021, 15(1):148
S7607 BQU57 BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
J Adv Res, 2024, S2090-1232(24)00171-1
PLoS One, 2019, 14(4):e0214764
S8959 BI-2852 BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
Eur J Cell Biol, 2023, 102(2):151314
E0135 CID-1067700 (ML282)

CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.
Int J Mol Sci, 2022, 23(24)15834
S7332 K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
E1474 BI-2865 BI-2865 is a none-covalent pan-KRAS Inhibitor. It binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively and inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 ce
S0730 (Rac)-Antineoplaston A10 (rac)-Antineoplaston A10 is the racemate of Antineoplaston A10, which is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
S0023 K-Ras-IN-1 K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.
E1187 Divarasib (GDC-6036) Divarasib (GDC-6036, RG6330) is a KRAS G12C inhibitor that binds irreversibly to switch II pocket of KRAS G12C (when in the inactive GDP-bound state) thereby blocking GTP binding and activation.
E1433 LY3537982 (KRAS G12C inhibitor 19) LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the  KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively.
E1578 garsorasib (D-1553 ) Garsorasib (D-1553 ) is a potent and selective oral KRASG12C inhibitor with antitumor activity. It has the potential to treat KRAS G12C-mutated non-small cell lung cancer (NSCLC).
E1606 RMC-6291 RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA).
S3493 APS6-45 APS6-45(Compound 10) is an orally active tumor-calibrated inhibitor (TCI) that inhibits RAS/MAPK signaling and exhibits antitumor activity.
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors.
S7330 6H05 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
S7333 K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
E1858New RMC-7977 RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC).
E1857New TH-Z816 TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide.
E1356New BI-0474 BI-0474 is a potent inhibitor of KRASG12C with an IC50 value of 7.0 nM. It inhibits GDP-KRAS::SOS1 protein-protein interactions. It exhibits anti-proliferative and anti-tumour activity and can be used in cancer research.
E1969New ADT-007 ADT-007 is a potent and orally active pan-RAS inhibitor. ADT-007 effectively targets and suppresses the proliferation of cancer cells harboring mutated or hyper-activated wild-type RAS isozymes. ADT-007 exhibits potent anti-cancer effects.
bioRxiv, 2024, 2024.10.04.616725
E4651New HRS-4642 HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo.
E1056 Opnurasib (JDQ-443) Opnurasib (JDQ-443,NVP-JDQ443) , a potent and selective, orally bioavailable covalent inhibitor of GDP-bound KRASG12C with an IC50 of 0.012 µM for inhibition of c-Raf recruitment.
S6527 Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).
E1597New RMC-6236 RMC-6236 (RAS-IN-2) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS.
E1047 NAV-2729 NAV-2729, an inhibitor of Arf6 activation which directly binds to Arf6, also inhibits all Arf guanine nucleotide exchange factors (ArfGEFs) with a strongest effect against BRAG2 and Arf1 .
S0323 Antineoplaston A10 Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
S5279 Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
E4697New RGT-018 RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer.
E1856New ARS-1323 ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C.
E1071 ASP2453 ASP2453, a potent, selective and covalent KRAS G12C inhibitor, inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf. ASP2453 is a potential therapeutic agent for KRAS G12C-mutated cancer.
E1157 Pan-RAS-IN-1 Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.
E1962New RMC-9805 RMC-9805(KRAS G12D ON inhibitor) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation.
S8831 MRTX-1257 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
E1564New BI-2493 BI-2493, a structural analogue of BI-2865, is a highly selective inhibitor of pan-KRAS. BI-2493 attenuates tumor growth and can be used for cancer research.
E4700New ML-099 ML099(CID-888706) is a pan-activator of Ras-related GTPases. It enhances GTPase activity by increasing its affinity for guanine nucleotides through binding to an allosteric site between switch regions I and II.
E1858New RMC-7977 RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC).
E1857New TH-Z816 TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide.
E1356New BI-0474 BI-0474 is a potent inhibitor of KRASG12C with an IC50 value of 7.0 nM. It inhibits GDP-KRAS::SOS1 protein-protein interactions. It exhibits anti-proliferative and anti-tumour activity and can be used in cancer research.
E1969New ADT-007 ADT-007 is a potent and orally active pan-RAS inhibitor. ADT-007 effectively targets and suppresses the proliferation of cancer cells harboring mutated or hyper-activated wild-type RAS isozymes. ADT-007 exhibits potent anti-cancer effects.
bioRxiv, 2024, 2024.10.04.616725
E4651New HRS-4642 HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo.
E1597New RMC-6236 RMC-6236 (RAS-IN-2) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS.
E4697New RGT-018 RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer.
E1856New ARS-1323 ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C.
E4700New ML-099 ML099(CID-888706) is a pan-activator of Ras-related GTPases. It enhances GTPase activity by increasing its affinity for guanine nucleotides through binding to an allosteric site between switch regions I and II.
E1962New RMC-9805 RMC-9805(KRAS G12D ON inhibitor) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation.
E1564New BI-2493 BI-2493, a structural analogue of BI-2865, is a highly selective inhibitor of pan-KRAS. BI-2493 attenuates tumor growth and can be used for cancer research.

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