Dual BET-Kinase inhibitor 3

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

一种有效的双重 BET 溴结构域激酶抑制剂，对 BRD4 BD1、JAK2 和 FLT-3 的 IC50 分别为 34、1.1 和 1.1 nM。

A potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively; also significantly inhibits NTRK3 (IC50=5 nM), ROS1 (IC50=11 nM), PDGFRβ (IC50=16 nM) and FGFR1 (IC50=43 nM), shows equal activity against the first and second bromodomains of BRD4 and shows only slightly reduced activity against BRDT-1; inhibits cell growth of MM and AML cell lines with IC50 of <1 uM, reduces c-MYC and p-STAT3 levels and induces G1 arrest, display differential activity across cancer cell lineages.

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BRD4-Kinases-IN-3 | BRD4 Kinases IN 3 | BRD4KinasesIN3 | BRD4 kinases inhibitor 3

Chromatin/Epigenetic

Bromodomain

Bromodomain

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1877286-69-5

527.663

C26H34FN7O2S

>98% (HPLC)

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CC(S(=O)(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C(F)=C3)=NC=C2C)=C1)=O)(C)C

N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-methylpyrimidin-4-yl)amino)phenyl)-2-methylpropane-2-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years