CDK7 and 9 inhibitor 14

Research use only, not for human use.

A potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively; displays >30-fold selectivity over CDK1/2/4, inhibits VEGFR2 with IC50 of 180 nM in a panel of non-CDK kinases.

A potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively; displays >30-fold selectivity over CDK1/2/4, inhibits VEGFR2 with IC50 of 180 nM in a panel of non-CDK kinases; demonstrates a broad spectrum of in vitro antitumor activity with average IC50 of 0.3 uM with no selectivity toward cell line types based on p53, p21, p16, or pRb status; significantly reduces phosphorylation of both Ser-2 and Ser-5 of the RNAP-II CTD, reduces antiapoptotic protein levels in cells, and selectively induces apoptosis in transformed cells, demonstrates antitumor activity in murine xenograft solid tumor models.

CDK7/9-IN-14

Angiogenesis

CDK

CDK

——

——

851439-14-0

382.49

C19H22N6OS

>98% (HPLC)

——

CC1=C(SC(=O)N1C)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCNCC4

3,4-dimethyl-5-[2-(4-piperazin-1-yl-phenylamino)-pyrimidin-4-yl]-3H-thiazol-2-one

(-20℃)

With Ice Pack

≥ 2 years