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Formula | C23H18ClF2N3O3S |
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Molecular Weight | 489.92 | CAS No. | 918504-65-1 | |
Solubility (25°C)* | In vitro | DMSO | 97 mg/mL (197.99 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy. | |||||||||||
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In vitro | PLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. [1] In melanoma cell lines, the inhibitory effect by PLX4032 depends on B-RAF mutational status, because PLX4032 potently inhibits those harboring B-RAF V600 mutants, including V600E, V600D, V600K, and V600R, but not wildtype or other mutants. The IC50 values of PLX4032 on these cells, including MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058, ranges from 20 nM to 1 μM. In these cells, PLX4032 (0.1 μM to 30 μM) also inhibits the phosphorylation of both MEK1/2 and ERK1/2. [2] PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAFV600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAFV600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAFV600E inhibition by PLX4032 results in a rapid feedback EGFR activation, which compensates for the PLX4032-inhibited cell proliferation. [3] | |||||||||||
In vivo | In B-RAFV600E-mutant mice xenograft models, PLX4032 (6 mg/kg–20 mg/kg) inhibits tumor growth. [1] In mice xenograft models of LOX, Colo829, and A375 cells, PLX4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival. [2] | |||||||||||
Features | A novel and potent inhibitor of the B-RAFV600E oncoprotein. |
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Data from [Data independently produced by Nature, 2015, 520(7547), 368-72]
Data from [Data independently produced by Nature, 2015, 520(7547), 368-72]
Data from [Data independently produced by Oncogene, 2015, 10.1038/onc.2015.97]
Data from [Data independently produced by Nature, 2014, 508(7494), 118-22]
The ribotoxic stress response drives UV-mediated cell death [ Cell, 2024, 187(14):3652-3670.e40] | PubMed: 38843833 |
Proteostatic reactivation of the developmental transcription factor TBX3 drives BRAF/MAPK-mediated tumorigenesis [ Nat Commun, 2024, 15(1):4108] | PubMed: 38750011 |
Proteostatic reactivation of the developmental transcription factor TBX3 drives BRAF/MAPK-mediated tumorigenesis [ Nat Commun, 2024, 15(1):4108] | PubMed: 38750011 |
Mi-2β promotes immune evasion in melanoma by activating EZH2 methylation [ Nat Commun, 2024, 15(1):2163] | PubMed: 38461299 |
The CoREST repressor complex mediates phenotype switching and therapy resistance in melanoma [ J Clin Invest, 2024, 134(6)e171063] | PubMed: 38300709 |
Ubiquitin-specific protease 22 controls melanoma metastasis and vulnerability to ferroptosis through targeting SIRT1/PTEN/PI3K signaling [ MedComm (2020), 2024, 5(8):e684] | PubMed: 39135915 |
Genomic deletions explain the generation of alternative BRAF isoforms conferring resistance to MAPK inhibitors in melanoma [ Cell Rep, 2024, S2211-1247(24)00376-0] | PubMed: 38614086 |
ERK1/2 interaction with DHPS regulates eIF5A deoxyhypusination independently of ERK kinase activity [ Cell Rep, 2024, 43(10):114831] | PubMed: 39392755 |
Cell-specific models reveal conformation-specific RAF inhibitor combinations that synergistically inhibit ERK signaling in pancreatic cancer cells [ Cell Rep, 2024, 43(9):114710] | PubMed: 39240715 |
ZEB1 controls a lineage-specific transcriptional program essential for melanoma cell state transitions [ Oncogene, 2024, 43(20):1489-1505] | PubMed: 38519642 |
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