BD-9136 | BRD4 degrader | Probechem Biochemicals

Chemical Structure : BD-9136

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BD-9136 (BD9136)

货号: PC-24551Not For Human Use, Lab Use Only.

BD-9136 is a potent, highly selective PROTAC degrader of BRD4 with DC50 of 1.2 nM (MV-4-11 cell, 4 h), Dmax=99%, displays >1000-fold selective over BRD2 and BRD3 proteins.

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25 mg		Get quote

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生物&药学活性

BD-9136 is a potent, highly selective PROTAC degrader of BRD4 with DC50 of 1.2 nM (MV-4-11 cell, 4 h), Dmax=99%, displays >1000-fold selective over BRD2 and BRD3 proteins.
BD-9136 is very potent and effective in inducing BRD4 degradation and achieves DC50 values of 0.1-4.7 nM and Dmax of >90% in 8 cancer cell lines.
BD-9136 potently inhibits cell growth inhibition in leukemia and breast cancer cell lines with IC50 of 5.1-80.9 nM.
BD-9136 significantly reduces only the level of BRD4 protein in the MDA-MB-231 cell line and does not significantly reduce any of the other >5,700 proteins, including BRD2 and BRD3 proteins.
BD-9136 effectively reduces the level of BRD4 protein in both the MV4;11 and MDA-MB-231 xenograft tumor tissues.
BD-9136 effectively inhibits tumor growth without adverse effects on mice and is more efficacious than the corresponding pan BET inhibitor.

物理化学性质&存储条件

分子量	824.96
分子式	C44H44N10O5S
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	1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[3-[4-[2-[9-methyl-3-(phenylmethyl)-4H,6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]oxazepin-2-yl]ethynyl]-1H-pyrazol-1-yl]-3-[2-(4-methyl-1-piperazinyl)ethyl]-1-azetidinyl]-

参考文献

1. Hu J, et al. J Med Chem. 2023 Jun 22;66(12):8222-8237.

BD-9136 (BD9136)

生物&药学活性

物理化学性质&存储条件

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BD-9136 (BD9136)

生物&药学活性

物理化学性质&存储条件

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