NEO2734
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。
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包装价格促销价数量
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5mg￥2962.002370.00- +
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10mg￥4862.003890.00- +
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50mg￥13712.0010970.00- +
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100mg￥21187.0016950.00- +
- 货号: ajcx11564
- CAS: 2081072-29-7
- 别名: EP31670
- 分子式: C??H??F?N?O?
- 分子量: 435.44
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: 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].
Reference:
[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.
