BETd-246 | BET PROTAC | Probechem Biochemicals

Chemical Structure : BETd-246

CAS No.: 2140289-17-2

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BETd-246 (BETd 246, BETd246)

货号: PC-60931Not For Human Use, Lab Use Only.

BETd-246 (BETd246) is a potent, second-generation BET protein PROTAC degrader that exhibits superior selectivity, potency and antitumor activity.

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2 mg	￥2580	In stock
5 mg	￥4580	In stock
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25 mg		Get quote

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生物&药学活性

BETd-246 (BETd246) is a potent, second-generation BET protein PROTAC degrader that exhibits superior selectivity, potency and antitumor activity.
BETd-246 completely and selectively depletes BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
BETd-246 displays strong growth inhibition and apoptosis induction activity in TNBC cell lines with IC50 <1 uM, induces a rapid and time-dependent downregulation of MCL1 protein.
BETd-246 decreases BET proteins in xenograft breast tumors and suppress tumor growth in vivo without causing weight loss.

物理化学性质&存储条件

分子量	946.035
分子式	C48H55N11O10
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-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(3-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)propoxy)ethoxy)ethoxy)propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

参考文献

1. Bai L, et al. Cancer Res. 2017 May 1;77(9):2476-2487.

BETd-246 (BETd 246, BETd246)

生物&药学活性

物理化学性质&存储条件

参考文献

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BETd-246 (BETd 246, BETd246)

生物&药学活性

物理化学性质&存储条件

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