Sorafenib Tosylate
CAS No. | 475207-59-1 | Cat. No. | BCP04089 |
Name | Sorafenib Tosylate | ||
Synonyms | BAY 439006 Tosylate ; BAY439006 Tosylate ; BAY-439006 Tosylate ; BAY 439006 Tosylate Salt; BAY 549085;4750207-59-1; | ||
Formula | C21H16ClF3N4O3.C7H8SO3 | M. Wt | 637.02 |
Description | Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib tosylate also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. Sorafenib tosylate weakly inhibits FGFR-1 with IC50 of 580 nM. Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. Sorafenib tosylate markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. Sorafenib tosylate potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. Sorafenib tosylate inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively.In addition to inhibition of the RAF/MEK/ERK signaling pathway, Sora | ||
Pathways | Angiogenesis/Protein Tyrosine Kinase MAPK Pathway | ||
Targets | PDGFR VEGFR c Kit FLT3 Raf |
Structure
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