Birabresib (OTX-015) | BET bromodomain inhibitor | Probechem Biochemicals

Chemical Structure : Birabresib

CAS No.: 202590-98-5

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Birabresib (OTX-015, MK-8628)

货号: PC-20573Not For Human Use, Lab Use Only.

Birabresib (OTX-015) is a potent, competitive inhibitor of BET bromodomain BRD2, BRD3, and BRD4 with EC50 of 10-19 nM, inhibits binding of BRD2, BRD3, and BRD4 to acetylated histone H4 (AcH4) with IC50 of 92-112 nM.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥2980	In stock
100 mg		Get quote

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生物&药学活性

Birabresib (OTX-015) is a potent, competitive inhibitor of BET bromodomain BRD2, BRD3, and BRD4 with EC50 of 10-19 nM, inhibits binding of BRD2, BRD3, and BRD4 to acetylated histone H4 (AcH4) with IC50 of 92-112 nM.
OTX015 inhibits cell growth of a variety of human cancer cell lines with IC50 of 60-200 nM for hematologic malignancies cells.
Oral administration of OTX015 significantly inhibited the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice, showing 79% TGI at 100 mg/kg qd and 61% TGI at 10 mg/kg bid.

物理化学性质&存储条件

分子量	491.99
分子式	C25H22ClN5O2S
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)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide

参考文献

1. J. Kay Noel, et al. Mol Cancer Ther (2013) 12 (11_Supplement): C244.

2. Klingbeil O, et al. Cell Death Dis. 2016 Sep 8;7(9):e2365.

Birabresib (OTX-015, MK-8628)

生物&药学活性

物理化学性质&存储条件

参考文献

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Birabresib (OTX-015, MK-8628)

生物&药学活性

物理化学性质&存储条件

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