NEO2734

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

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）。

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.

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.

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.

EP31670

Chromatin/Epigenetic

Epigenetic Reader Domain

p300/CBP|BET bromodomain

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2081072-29-7

435.44

C22H24F3N3O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (229.65 mM)

Cc1cc(cn(C)c1=O)-c1ccc2nc(C3CCOCC3)n(CCOC(F)(F)F)c2c1

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(-20℃)

With Ice Pack

≥ 2 years