CD161(Synonyms: NKR-P1A)

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CD161 (Synonyms: NKR-P1A)

CD161 (NKR-P1A) 是一种有效，选择性的且口服生物可利用的溴结构域和末端 (BET) 溴结构域抑制剂，对 BRD4 BD1 和 BRD4 BD2 的 IC50值 分别为 28.2 nM 和 7.2 nM。CD161 具有抗肿瘤活性。

CD161(Synonyms: NKR-P1A)

CD161 Chemical Structure

CAS No. : 1627716-22-6

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生物活性

CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity[1].

IC50 & Target

IC50: 28.2 nM (BRD4 BD1) and 7.2 nM (BRD4 BD2)[1]
体外研究
(In Vitro)

CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.

体内研究
(In Vivo)

CD161 (NKR-P1A) (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition[1].
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) [1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Dorsal side of severe combined immunodeficient (SCID) mice[1]
Dosage: 20, 40 mg/kg
Administration: Po; daily; 45 days
Result: Achieved essentially complete tumor growth inhibition.
Animal Model: Rat or mice[1]
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) [1].

分子量

435.48

Formula

C26H21N5O2
CAS 号

1627716-22-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhao Y, et al. Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. J Med Chem. 2017 May 11;60(9):3887-3901.

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