CD161 |CAS:1627716-22-6 Probechem Biochemicals

Chemical Structure : CD161

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CD161 (CD 161, CD-161, NKR-P1A)

货号: PC-61129Not For Human Use, Lab Use Only.

CD161 (NKR-P1A) is a potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.

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生物&药学活性

CD161 (NKR-P1A) is a potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.
CD161 shows high affinity for BRD2, BRD3, BRD4 and BRDT bromodomains, and liitle to no affintiy for other bromodomains (Ki>500 nM).
CD161 exhibits cytotoxicity against a panel of breast cancer cell lines (MDA-MB-231 IC50=244 nM).
CD161 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.

物理化学性质&存储条件

分子量	435.487
分子式	C26H21N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole

参考文献

1. Zhao Y, et al. J Med Chem. 2017 May 11;60(9):3887-3901.

CD161 (CD 161, CD-161, NKR-P1A)

生物&药学活性

物理化学性质&存储条件

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CD161 (CD 161, CD-161, NKR-P1A)

生物&药学活性

物理化学性质&存储条件

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