PLX-7904

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 BRaf 抑制剂，在突变 RAS 表达细胞中针对 BRaf V600E 的 IC50 为 5 nM。

A potent and selective BRaf inhibitor with IC50 of 5 nM against BRaf V600E in mutant RAS expressing cells; inhibits the growth of A375, COLO829, COLO205 that expresses BRAFV600E with IC50 values of 0.17 uM, 0.53 uM, and 0.16 uM, respectively; inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells.

PLX7904 inhibits the in vitro growth of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 that expresses BRAFV600E with IC50 values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, on a par with vemurafenib IC50 values in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively). PLX7904 and PLX8394 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 and PLX8394 treatment at 1 μM concentration reduce colony formation and viability in parental cells to a similar level as PLX4720. PPLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells. PPLX7904 inhibits ERK1/2 in PLX470-resistant cell lines. PPLX7904 treatment promotes apoptosis and inhibits anchorage-independent growth of vemurafenib resistant cells.

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PLX-7904

MAPK/ERK Signaling

Raf

B-Raf(V600E)

Cancer

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1393465-84-3

512.5317

C24H22F2N6O3S

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(C1=CNC2=NC=C(C3=CN=C(C4CC4)N=C3)C=C21)C5=C(F)C=CC(NS(=O)(N(CC)C)=O)=C5F

Sulfamide, N'-[3-[[5-(2-cyclopropyl-5-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-N-ethyl-N-methyl-

(-20℃)

With Ice Pack

≥ 2 years