CD 161

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、选择性的、口服生物可利用的 BET 溴结构域抑制剂，对于 BRD4 BD2 和 BRD4 BD1 的 IC50 分别为 7.2 和 28.2 nM。

A potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively; shows high affinity for BRD2, BRD3, BRD4 and BRDT bromodomains, and liitle to no affintiy for other bromodomains (Ki>500 nM); exhibits cytotoxicity against a panel of breast cancer cell lines (MDA-MB-231 IC50=244 nM), demonstrates significant antitumor activity in the MV4;11 leukemia and MDA-MB-231 triple-negative breast cancer xenograft models in mice, has excellent microsomal stability and good oral pharmacokinetics in rats and mice.

CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner. Western Blot Analysis Cell Line:MV4;11 leukemia cells.Concentration:30, 100, 300, 1000, 3000 nM.Incubation Time:1 hours Result:Induced rapid down-regulation of c-Myc at as early as the 1 hours time point and in a dose-dependent manner.

CD161 (NKR-P1A) (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition.CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the Cmax of 7333 ng/mL (po) for rat. The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) . Animal Model:Dorsal side of severe combined immunodeficient (SCID) mice Dosage:20, 40 mg/kg Administration:Po; daily; 45 days Result:Achieved essentially complete tumor growth inhibition.Animal Model:Rat or mice Dosage:5 mg/kg (iv), 25 mg/kg (po) for rat and mice (Pharmacokinetic Study) Administration:Iv and po; 0, 5, 15, 30 mins, and 1, 2, 4, 6, 8, 24 hours Result:The t1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the Cmaxof rat is 7333 ng/mL (po). The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) .

CD161 | CD-161

Chromatin/Epigenetic

Bromodomain

Bromodomain

Cancer

——

1627716-22-6

435.487

C26H21N5O2

>98% (HPLC)

——

CC1=C(C2=CC3=C(C=C2OC)C4=C(C5=CC=NC6=CC=CC=C56)N=C(C)N=C4N3)C(C)=NO1

4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole

(-20℃)

With Ice Pack

≥ 2 years