NEO2734 ( EP31670 )

产品货号. M22391 CAS No. 2081072-29-7

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

NEO2734
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

NEO2734 是一种口服活性、选择性的 p300/CBP 和 BET 溴结构域抑制剂（p300/CBP 和 BET 溴结构域的 IC50 均<30 nM）。
产品描述

NEO2734 is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).NEO2734, a novel dual inhibitor of BET and CBP/p300, is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo.
体外实验

Western Blot Analysis Cell Line:NUT carcinoma patient cell lines (TC-797 and PER-403).Concentration:1 μM.Incubation Time:6 h.Result:Results in greater loss of MYC protein.
体内实验

Animal Model:Mice (PER-403 and 14169 models).Dosage:5, 8, 10 mg/kg Administration:Orally, once daily for 28 days.Result:Two of the three mice treated with NEO2734 were alive by day 100.Provided markedly improved survival compared with EP, i-BET-762, and even iBET-762+EP by day 100 following initiation of treatment.
同义词

EP31670
通路

Chromatin/Epigenetic
靶点

Epigenetic Reader Domain
受体

p300/CBP|BET bromodomain
研究领域

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适应症

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1. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer.

计算器

产品手册

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