Senexin B

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

Senexin B (SNX2-1-165) 是一种高效、选择性、口服的 CDK8/CDK19 抑制剂，IC50 为 24-50 nM。

Senexin B (SNX2-1-165) is a highly potent, selective and orally available CDK8/CDK19 inhibitor with IC50 of 24-50 nM; exhibits selectivity for CDK8 and CDK19 with Kd of 140 nM and 80 nM, respectively; significantly suppresses tumor growth in ER-positive breast cancer xenografts.

Senexin B inhibits CDK8/19 in low nanomolar range. Senexin B is a newly optimized derivative of Senexin A. It has the same high selectivity for CDK8/19 and is more potent than Senexin A. Senexin B strongly reduces the emergence of estrogen independent cells. Senexin B shows synergy with fulvestrant in MCF7, T47D-ER/Luc and BT474.

Pretreatment of tumor-free mice with Senexin B significantly inhibits the growth of triple-negative breast cancer (TNBC) cells inoculated into mice subsequently to Senexin B administration, indicating a general chemopreventive effect on the normal tissue “soil”. Senexin B potentiates the tumor-suppressive effect of doxorubicin on established TNBC xenografts; this effect is associated with the suppression of NFκB-mediated transcriptional induction of tumor-promoting cytokines. Senexin B inhibits invasive growth into the muscle layer in an orthotopic xenograft model of MDA-MB-468 TNBC cells. In a spleen-to-liver colon cancer metastasis model of syngeneic mouse CT26 tumors, Senexin B treatment of mice have the same effect as CDK8 knockdown in tumor cells: suppression of metastatic growth in the liver without a significant effect on primary tumor growth in the spleen. Senexin B suppresses tumor growth and augmentes the effects of fulvestrant in ER-positive breast cancer xenografts.

SNX2-1-165

Angiogenesis

CDK

CDK

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1449228-40-3

450.53

C27H26N6O

>98% (HPLC)

10 mM in DMSO

O=C(C1=CC2=CC=C(CCNC3=C4C(C=CC(C#N)=C4)=NC=N3)C=C2C=C1)N5CCN(C)CC5

4-((2-(6-(4-Methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years