SB590885

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01889CAS No. ：405554-55-4Purity：98%

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CAS No.	405554-55-4	Cat. No.	BCP01889
Name	SB590885
Synonyms	SB-590885;GSK-2118436;GSK2118436;GSK 2118436;SB 590885;
SMILES
Chemical Name
Formula	C27H27N5O2	M. Wt	453.54
Purity	98%	Storage	Store at 4-8°C
Description	SB590885 displays significant selectivity for B-Raf over c-Raf with Ki of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (Ki = 38 nM for mutant B-Raf, 6 nM for c-Raf). SB590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, SB590885 treatment potently inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. SB590885 displays high affinity for B-Raf with Kd of 0.3 nM.Most of the melanoma cell lines that harbor the BRAF V600E mutation