CFT-2718 | BRD4 PROTAC | Probechem Biochemicals

Chemical Structure : CFT-2718

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CFT-2718 (CFT2718)

货号: PC-72644Not For Human Use, Lab Use Only.

CFT-2718 (CFT2718) is a benzotriazoloazepine-based BRD4 degrader, rapidly and selectively degrade BRD4 in vitro in a CRBN-dependent manner (DC90=10 nM, 293T cells).

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生物&药学活性

CFT-2718 (CFT2718) is a benzotriazoloazepine-based BRD4 degrader, rapidly and selectively degrade BRD4 in vitro in a CRBN-dependent manner (DC90=10 nM, 293T cells).
CFT-2718 is more effective than dinaciclib in controlling cell growth and efficiently reduces BRD4 expression in vitro (H69 cell IC50: 0.02 versus 17.38 nM).
CFT-2718 is more effective than dinaciclib in control of PDX tumor models in vivo.
CFT-2718 selectively increased the expression of cleaved PARP, an indicator of apoptosis.
CFT-2718 caused rapid BRD4 degradation and reduced levels of total and pSer2 RPB1 protein.

物理化学性质&存储条件

分子量	811.388
分子式	C45H47ClN10O3
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	O=C(C(N(CC1=C2C=CC=C1N[C@H]3CN(CCCCCCN4N=CC(C5=CC=C(N6C(C7(CC7)N=C8C9=CC=C(Cl)C=C9)=NN=C6C)C8=C5)=C4)CC3)C2=O)CC%10)NC%10=O

参考文献

1. Sun D, et al. Mol Cancer Ther. 2021 Aug;20(8):1367-1377.

CFT-2718 (CFT2718)

生物&药学活性

物理化学性质&存储条件

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CFT-2718 (CFT2718)

生物&药学活性

物理化学性质&存储条件

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