NEO2734 (EP31670) 是一种口服有效的双重 p300/CBP 和 BET 溴结构域选择性抑制剂，对 p300/CBP 和 BET 溴结构域的 IC50 值均<30 nm。 neo2734 在 spop 突变型和野生型前列腺癌中具有活性。
货号:ajcx11564
CAS:2081072-29-7
分子式:C??H??F?N?O?
分子量：435.44
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2].

NEO2734 (1 μM) induces differentiation and G1-phase cell cycle arrest[1].
NEO2734 (1 μM) rapidly induces squamous differentiation in NMC cell lines, and expression of the terminal squamous differentiation marker, involucrin, or keratins[1].
NEO2734 is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo[2].

参考文献:
[1]. Chevaun D Morrison-Smit, et al. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 Jul;19(7):1406-1414.
[2]. Yuqian Yan, et al. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019 Nov 7;11(11):e10659.