BI-1347

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

BI-1347 是一种有效的、选择性的 CDK8/cyclinC 抑制剂，IC50 为 1 nM。

BI-1347 is a potent, selective inhibitor of CDK8/cyclinC with IC50 of 1 nM; BI-1347 shows tumor growth inhibition in an in vivo xenograft model, BI-1347 is an excellent small molecule tool inhibitor for testing biological hypotheses in vitro and in vivo.

BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells.BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells.Western Blot Analysis Cell Line:Mouse splenic NK cells Concentration:150 nM Incubation Time:44 hours Result:Increased the proportion of granzyme B-positive NK cells by approximately 4-fold.Western Blot Analysis Cell Line:Human NK92MI cells Concentration:0.1 nM-10 μM Incubation Time:24 hours Result:Increased perforin levels with an EC50 value of 7.2 nM.

BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity in vivo.BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model. Animal Model:B16-F10-luc2 syngeneic melanoma model Dosage:10 mg/kg Administration:Oral gavage; 10 mg/kg; once daily; 30 d Result:Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%.Showed minimal effect on body weight at 10 mg/kg.Showed lower tumor burden both on day 23 and 29, compared to the control group.

BI1347

Angiogenesis

CDK

CDK8

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2163056-91-3

356.429

C22H20N4O

>98% (HPLC)

DMSO: 120 mg/mL (336.68 mM), Need ultrasonic and warming （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1

2-(4-(4-(isoquinolin-4-yl)phenyl)-1H-pyrazol-1-yl)-N,N-dimethylacetamide

(-20℃)

With Ice Pack

≥ 2 years