NEO2734

产品说明书

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Chemical Structure| 2081072-29-7 同义名 : EP31670
CAS号 : 2081072-29-7
货号 : A1359463
分子式 : C22H24F3N3O3
纯度 : 99%+
分子量 : 435.44
MDL号 : MFCD32857168
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(241.14 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • p300/CBP

    p300/CBP, IC50:<30 nM

  • BET

    BET, IC50:<30 nM
描述 NEO2734 (EP31670) is an orally active inhibitor selectively targeting both p300/CBP and BET bromodomains, displaying IC50 values of less than 30 nM for each[1]. NEO2734 is effective in both SPOP mutant and wild-type prostate cancer[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.48mL

2.30mL

1.15mL

22.97mL

4.59mL

2.30mL
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.