NHWD-870 (NHWD870)

Chemical Structure : NHWD-870

CAS No.: 2115742-03-3

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货号: PC-27038Not For Human Use, Lab Use Only.

NHWD-870 is a potent BET inhibitor with IC50 of 2.7 nM for BRD4 bromodomain, inhibits BRD4 activation and c-MYC expression.

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5 mg	￥2980	In stock
10 mg	￥4580	In stock
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生物&药学活性

NHWD-870 is a potent BET inhibitor with IC50 of 2.7 nM for BRD4 bromodomain, inhibits BRD4 activation and c-MYC expression.
NHWD-870 shows potent BET inhibition in cellular assays using A375 melanoma cells with IC50 of 2.46 nM, which is about 23-fold more potent than I-BET151 (IC50 = 55.5 nM), and about 14-fold more potent than two clinical stage inhibitors GSK-525762 (IC50 = 35.6 nM) or OTX015 (IC50=34.8 nM).
NHWD-870 suppresses the growth of multiple solid tumor cell lines, inhibits BRD4 phosphorylation and c-MYC expression.
NHWD-870 strongly suppresses the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo.
NHWD-870 reduced the proliferation of TAMs in vivo, by inhibiting CSF1R signaling.

物理化学性质&存储条件

分子量	491.60
分子式	C29H29N7O
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	(S)-7-(1,4-Dimethyl-1H-1,2,3-triazol-5-yl)-1-methyl-9-(phenyl(tetrahydro-2H-pyran-4-yl)methyl)-1,9-dihydropyrido[2',3':4,5]pyrrolo[3,2-f]indazole

参考文献

1. Yin M, et al. Nat Commun. 2020 Apr 14;11(1):1833.

NHWD-870 (NHWD870)

生物&药学活性

物理化学性质&存储条件

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NHWD-870 (NHWD870)

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