S1460 |
SP600125
|
SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
-
Cancer Cell, 2024, 42(4):535-551.e8
-
Nat Commun, 2024, 15(1):2581
-
Nat Commun, 2024, 15(1):987
|
|
S1133 |
Alisertib (MLN8237)
|
Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3. |
-
Nat Commun, 2024, 15(1):1041
-
Cell Rep Med, 2024, 5(3):101471
-
Redox Biol, 2024, 72:103137
|
|
S1147 |
Barasertib (AZD1152-HQPA)
|
Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1. |
-
Gastroenterology, 2024, S0016-5085(24)00062-3
-
Nat Commun, 2024, 15(1):1041
-
J Exp Clin Cancer Res, 2024, 43(1):234
|
|
S1048 |
Tozasertib (VX-680)
|
Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2. |
-
Cell Death Dis, 2024, 15(1):56
-
Cell Rep, 2024, 43(9):114739
-
Elife, 2024, 12RP92324
|
|
S1103 |
ZM 447439
|
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. |
-
Nat Commun, 2024, 15(1):8754
-
Nat Commun, 2024, 15(1):1041
-
Cell Rep, 2024, 43(9):114739
|
|
S1100 |
MLN8054
|
MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1. |
-
Nat Commun, 2024, 15(1):1041
-
Nat Commun, 2023, 14(1):5317
-
Mol Biol Cell, 2023, 34(5):ar47
|
|
S1107 |
Danusertib (PHA-739358)
|
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2. |
-
Elife, 2024, 12RP92324
-
Sci Rep, 2024, 14(1):4303
-
Environ Mol Mutagen, 2024, 10.1002/em.22604
|
|
S1529 |
Hesperadin
|
Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo. |
-
Cell Rep, 2024, 43(9):114739
-
Environ Mol Mutagen, 2024, 10.1002/em.22604
-
Oncogene, 2022, 10.1038/s41388-022-02328-4
|
|
S2770 |
MK-5108
|
MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1. |
-
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
-
Sci Rep, 2024, 14(1):4303
-
Biosensors (Basel), 2022, 12(4)196
|
|
S1451 |
TCS7010 (Aurora A Inhibitor I)
|
TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway. |
-
Int J Mol Sci, 2022, 23(24)15573
-
Int J Mol Sci, 2022, 23(24)15573
-
Biochim Biophys Acta Mol Cell Res, 2022, 1869(12):119361
|
|
S1134 |
AT9283
|
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
-
J Transl Med, 2024, 22(1):209
-
Int J Mol Sci, 2024, 25(5)2956
-
Sci Rep, 2024, 14(1):8200
|
|
S1249 |
JNJ-7706621
|
JNJ-7706621 is a pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1. |
-
Microbiol Spectr, 2023, 11(1):e0194322
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Curr Biol, 2022, 32(19):4314-4324.e7
|
|
S2719 |
AMG-900
|
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1. |
-
Cell Chem Biol, 2023, 30(8):987-998.e24
-
Cancer Cell, 2022, 40(7):754-767.e6
-
Int J Mol Sci, 2022, 23(24)15573
|
|
S1454 |
PHA-680632
|
PHA-680632 is a potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3. |
-
Sci Rep, 2024, 14(1):12470
-
Heliyon, 2023, 9(7):e17386
-
Heliyon, 2023, 9(7):e17386
|
|
S2158 |
KW-2449
|
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1. |
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Cell Rep Med, 2022, 3(1):100492
-
Cancer Res, 2022, 82(11):2141-2155
|
|
S7588 |
Reversine
|
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 400 nM/500 nM/400 nM, respectively. Also used for stem cell dedifferentiation.
|
-
Nat Commun, 2023, 14(1):3364
-
Commun Biol, 2023, 6(1):1271
-
Heliyon, 2023, 9(9):e20182
|
|
S1154 |
SNS-314
|
SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1. |
-
Cell Chem Biol, 2023, 30(8):987-998.e24
-
Res Sq, 2023, rs.3.rs-2570204
-
Haematologica, 2022, 10.3324/haematol.2022.280884
|
|
S1181 |
ENMD-2076
|
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. |
-
Cell, 2021, 184(2):334-351.e20
-
Sci Adv, 2021, 7(4)eabd7851
-
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S2740 |
GSK1070916
|
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1. |
-
PLoS One, 2024, 19(1):e0295629
-
Cell Chem Biol, 2023, 30(8):987-998.e24
-
Cancer Cell, 2021, S1535-6108(21)00383-4
|
|
S2744 |
CCT137690
|
CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel. |
-
Cancer Lett, 2024, 604:217258
-
Sci Rep, 2024, 14(1):8200
-
Cell Chem Biol, 2023, 30(8):987-998.e24
|
|
S1171 |
CYC116
|
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1. |
-
Sci Rep, 2024, 14(1):4303
-
Cell Chem Biol, 2023, 30(8):987-998.e24
-
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
|
|
S2718 |
TAK-901
|
TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1. |
-
Sci Rep, 2024, 14(1):8200
-
Cell Chem Biol, 2023, 30(8):987-998.e24
-
Microbiol Spectr, 2023, 11(1):e0194322
|
|
S7843 |
BI-847325
|
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1. |
-
Nat Commun, 2023, 14(1):478
-
Cancer Res Commun, 2023, 3(10):2170-2181
-
Cancer Res Commun, 2023, 3(10):2170-2181
|
|
S1519 |
CCT129202
|
CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc. |
-
Aging (Albany NY), 2020, 7;12(9):8221-8240
-
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
-
PLoS One, 2014, 9(7):e102741
|
|
S8699 |
SNS-314 Mesylate
|
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. |
-
Haematologica, 2022, 10.3324/haematol.2022.280884
-
Cancers (Basel), 2021, 13(6)1205
-
Front Pharmacol, 2020, 30;11:543
|
|
S8782 |
LY3295668
|
LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively. |
-
J Natl Cancer Inst, 2024, djae091
-
Med Oncol, 2024, 41(6):142
-
EBioMedicine, 2023, 95:104752
|
|
S9658 |
SP-96
|
SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC). |
-
Cell Chem Biol, 2023, 30(8):987-998.e24
|
|
S7065 |
MK-8745
|
MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B. |
|
|
S2018 |
ENMD-2076 L-(+)-Tartaric acid
|
ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2. |
|
|
S9741 |
TAS-119
|
TAS-119 is a potent, selective, and orally active inhibitor of Aurora A, including Aurora B with an IC50 of 1.0 nM and 95 nM, respectively. It exhibits antitumor activities. |
|
|
E0338 |
AKI603
|
AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation. |
|
|
E0342 |
Aurora kinase Inhibitor II
|
Aurora kinase inhibitor II, an anilinoquinazoline that is both a potent and selective ATP-competitive inhibitor of Aurora kinase (ARK), has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division. |
|
|
E0616 |
Chiauranib
|
Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |
|
|
S2931 |
Aurora Kinase Inhibitor III
|
Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). |
|
|
S6214 |
H-1152 dihydrochloride
|
H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. |
|
|
E1651New |
CD532
|
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. It breaks the native conformation of Aurora-A, drives the degradation of N-Myc in N-Myc-driven cancers, and also exhibits anti-proliferative effects. |
|
|
S1272 |
XL228
|
XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively. |
|
|
E1435New |
Tinengotinib
|
Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
|
|
S1460 |
SP600125
|
SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
- Cancer Cell, 2024, 42(4):535-551.e8
- Nat Commun, 2024, 15(1):2581
- Nat Commun, 2024, 15(1):987
|
|
S1133 |
Alisertib (MLN8237)
|
Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3. |
- Nat Commun, 2024, 15(1):1041
- Cell Rep Med, 2024, 5(3):101471
- Redox Biol, 2024, 72:103137
|
|
S1147 |
Barasertib (AZD1152-HQPA)
|
Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1. |
- Gastroenterology, 2024, S0016-5085(24)00062-3
- Nat Commun, 2024, 15(1):1041
- J Exp Clin Cancer Res, 2024, 43(1):234
|
|
S1048 |
Tozasertib (VX-680)
|
Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2. |
- Cell Death Dis, 2024, 15(1):56
- Cell Rep, 2024, 43(9):114739
- Elife, 2024, 12RP92324
|
|
S1103 |
ZM 447439
|
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. |
- Nat Commun, 2024, 15(1):8754
- Nat Commun, 2024, 15(1):1041
- Cell Rep, 2024, 43(9):114739
|
|
S1100 |
MLN8054
|
MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1. |
- Nat Commun, 2024, 15(1):1041
- Nat Commun, 2023, 14(1):5317
- Mol Biol Cell, 2023, 34(5):ar47
|
|
S1107 |
Danusertib (PHA-739358)
|
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2. |
- Elife, 2024, 12RP92324
- Sci Rep, 2024, 14(1):4303
- Environ Mol Mutagen, 2024, 10.1002/em.22604
|
|
S1529 |
Hesperadin
|
Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo. |
- Cell Rep, 2024, 43(9):114739
- Environ Mol Mutagen, 2024, 10.1002/em.22604
- Oncogene, 2022, 10.1038/s41388-022-02328-4
|
|
S2770 |
MK-5108
|
MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1. |
- Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
- Sci Rep, 2024, 14(1):4303
- Biosensors (Basel), 2022, 12(4)196
|
|
S1451 |
TCS7010 (Aurora A Inhibitor I)
|
TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway. |
- Int J Mol Sci, 2022, 23(24)15573
- Int J Mol Sci, 2022, 23(24)15573
- Biochim Biophys Acta Mol Cell Res, 2022, 1869(12):119361
|
|
S1134 |
AT9283
|
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
- J Transl Med, 2024, 22(1):209
- Int J Mol Sci, 2024, 25(5)2956
- Sci Rep, 2024, 14(1):8200
|
|
S1249 |
JNJ-7706621
|
JNJ-7706621 is a pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1. |
- Microbiol Spectr, 2023, 11(1):e0194322
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Curr Biol, 2022, 32(19):4314-4324.e7
|
|
S2719 |
AMG-900
|
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1. |
- Cell Chem Biol, 2023, 30(8):987-998.e24
- Cancer Cell, 2022, 40(7):754-767.e6
- Int J Mol Sci, 2022, 23(24)15573
|
|
S1454 |
PHA-680632
|
PHA-680632 is a potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3. |
- Sci Rep, 2024, 14(1):12470
- Heliyon, 2023, 9(7):e17386
- Heliyon, 2023, 9(7):e17386
|
|
S2158 |
KW-2449
|
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Cell Rep Med, 2022, 3(1):100492
- Cancer Res, 2022, 82(11):2141-2155
|
|
S7588 |
Reversine
|
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 400 nM/500 nM/400 nM, respectively. Also used for stem cell dedifferentiation.
|
- Nat Commun, 2023, 14(1):3364
- Commun Biol, 2023, 6(1):1271
- Heliyon, 2023, 9(9):e20182
|
|
S1154 |
SNS-314
|
SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1. |
- Cell Chem Biol, 2023, 30(8):987-998.e24
- Res Sq, 2023, rs.3.rs-2570204
- Haematologica, 2022, 10.3324/haematol.2022.280884
|
|
S1181 |
ENMD-2076
|
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. |
- Cell, 2021, 184(2):334-351.e20
- Sci Adv, 2021, 7(4)eabd7851
- J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S2740 |
GSK1070916
|
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1. |
- PLoS One, 2024, 19(1):e0295629
- Cell Chem Biol, 2023, 30(8):987-998.e24
- Cancer Cell, 2021, S1535-6108(21)00383-4
|
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S2744 |
CCT137690
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CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel. |
- Cancer Lett, 2024, 604:217258
- Sci Rep, 2024, 14(1):8200
- Cell Chem Biol, 2023, 30(8):987-998.e24
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S1171 |
CYC116
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CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1. |
- Sci Rep, 2024, 14(1):4303
- Cell Chem Biol, 2023, 30(8):987-998.e24
- Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
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S2718 |
TAK-901
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TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1. |
- Sci Rep, 2024, 14(1):8200
- Cell Chem Biol, 2023, 30(8):987-998.e24
- Microbiol Spectr, 2023, 11(1):e0194322
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S7843 |
BI-847325
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BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1. |
- Nat Commun, 2023, 14(1):478
- Cancer Res Commun, 2023, 3(10):2170-2181
- Cancer Res Commun, 2023, 3(10):2170-2181
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S1519 |
CCT129202
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CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc. |
- Aging (Albany NY), 2020, 7;12(9):8221-8240
- J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
- PLoS One, 2014, 9(7):e102741
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S8699 |
SNS-314 Mesylate
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SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. |
- Haematologica, 2022, 10.3324/haematol.2022.280884
- Cancers (Basel), 2021, 13(6)1205
- Front Pharmacol, 2020, 30;11:543
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S8782 |
LY3295668
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LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively. |
- J Natl Cancer Inst, 2024, djae091
- Med Oncol, 2024, 41(6):142
- EBioMedicine, 2023, 95:104752
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S9658 |
SP-96
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SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC). |
- Cell Chem Biol, 2023, 30(8):987-998.e24
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S7065 |
MK-8745
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MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B. |
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S2018 |
ENMD-2076 L-(+)-Tartaric acid
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ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2. |
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S9741 |
TAS-119
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TAS-119 is a potent, selective, and orally active inhibitor of Aurora A, including Aurora B with an IC50 of 1.0 nM and 95 nM, respectively. It exhibits antitumor activities. |
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E0338 |
AKI603
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AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation. |
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E0342 |
Aurora kinase Inhibitor II
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Aurora kinase inhibitor II, an anilinoquinazoline that is both a potent and selective ATP-competitive inhibitor of Aurora kinase (ARK), has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division. |
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E0616 |
Chiauranib
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Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |
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S2931 |
Aurora Kinase Inhibitor III
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Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). |
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S6214 |
H-1152 dihydrochloride
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H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. |
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E1651New |
CD532
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CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. It breaks the native conformation of Aurora-A, drives the degradation of N-Myc in N-Myc-driven cancers, and also exhibits anti-proliferative effects. |
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S1272 |
XL228
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XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively. |
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E1435New |
Tinengotinib
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Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
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