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I-BET762(GSK525762),BETInhibitor

品牌：Xcessbio

貨號：M60154-2s

規(guī)格：2mg solid

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I-BET762(GSK525762),BETInhibitor

商品詳情參考文獻(xiàn) 相關(guān)資料

Product Information

Molecular Weight:	423.90
Formula:	C₂₂H₂₂ClN₅O₂
Purity:	≥98%
CAS#:	1260907-17-2
Solubility:	DMSO up to 50 mM
Chemical Name:	(S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide
Storage:	Powder: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 1 year.

Biological Activity:

I-BET762 (GSK525762) is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC₅₀?of ~35 nM. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation. It is highly selective over other bromodomain-containing proteins. In vivo studies using I-BET762 have demonstrated efficacy in a range of oncology and immunoinflammatory models. I-BET762 is currently in clinical development for oncology indication.?

How to Use:?

In vitro:? I-BET762 was used at 0.5-1 μM final concentration in various in vitro assays.
In vivo:?I-BET762 could be dosed to the mice by oral administration at 10-30 mg/kg once per day.?

Reference:

1. Mirguet O, et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. (2013) J Med Chem. 56(19):7501-15.
2. Zhao Y, et al. The making of I-BET762, a BET bromodomain inhibitor now in clinical development. (2013) J Med Chem. 56(19):7498-500.?

Products are for research use only. Not for human use.

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