RAF1 kinase inhibitor (and others)
Catalog No. R01-900
Catalog No. | Pack Size | Price (USD) | |
---|---|---|---|
R01-900-10 | 10 mg | $60 | |
R01-900-50 | 50 mg | $240 | |
R01-900-BULK | BULK | Contact Us |
Overview:
Initially developed as a Raf kinase inhibitor, IC50 = 6 nM, but has been shown to inhibit many receptor tyrosine kinases including BRAF (IC50 = 22 nM); VEGFR-2 (IC50 = 90 nM); VEGFR-3 (IC50 = 20 nM); PDGFR-beta (IC50 = 57 nM); Flt3 (IC50 = 58 nM); c-KIT (IC50 = 68 nM); FGFR-1 (IC50 = 580 nM) (1). Paradoxically more potent in a cellular assay (IC50 = 20 nM) compared to an isolated enzyme assay (IC50 = 107 nM) for c-Fms (2). Inhibits activation of MAPK pathway and ERK phosphorylation (3). Induces caspase-independent apoptosis in melanoma cells (4). Clinically useful anticancer agent.
References:
1. SM Wilhelm et al. Cancer Res. 2004 64:7099
2. J Guo et al. Mol. Cancer Ther. 2006 5:1007
3. SM Wilhelm et al. Proc. Am. Assoc. Cancer Res. 2003 44:106609
4. DJ Panka et al. Cancer Res. 2006 66:1611
CAS Registry Number:
284461-73-0
Molecular Formula:
C21H16ClF3N4O3
Appearance:
Off-white powder
Melting Point:
204-206oC
Molecular Weight:
464.8
Purity:
>99% (TLC); NMR (Conforms)
Solubilization:
Soluble in DMSO (200 mg/ml); or Ethanol (3 mg/ml)
Aliases:
1. 4-(4-(3-(4-chloro-3 (trifluoromethyl) phenyl) ureido) phenoxy)-N-methylpicolinamide
2. BAY 43-9006
Storage and Stability:
Store desiccated as supplied at -20o for up to 2 years. Store solutions at -20oC for up to 1 month.
Molecular Structure:
Angiogenesis, Apoptosis/Autophagy, Cancer, Cardiovascular Disease, ERK/MAPK Pathway, Invasion/Metastasis, Neurobiology, Ser/Thr Kinases
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