BRAF inhibitor 13

Research use only, not for human use.

A potent and selective B-Raf inhibitor with IC50 of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.

A potent and selective B-Raf inhibitor with IC50 of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively; induces proliferation and hyperplasia in normal tissues of mice.

Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers.

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BRAF-IN-13

MAPK/ERK Signaling

Raf

B-Raf

Cancer

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1093100-40-3

478.944

C26H19ClN8

>98% (HPLC)

DMSO: ≥53 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CC1=C(C2=C(C=C1)C(=NC=C2)NC3=CC=C(C=C3)Cl)NC4=C(C=CC=N4)C5=C6C(=NC=N5)N=CN6

N5-(3-(9H-purin-6-yl)pyridin-2-yl)-N1-(4-chlorophenyl)-6-methylisoquinoline-1,5-diamine

(-20℃)

With Ice Pack

≥ 2 years