CPI-637

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Chemical Structure| 1884712-47-3 同义名 : -
CAS号 : 1884712-47-3
货号 : A788310
分子式 : C22H22N6O
纯度 : 99%+
分子量 : 386.45
MDL号 : MFCD30489741
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

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

DMSO: 9 mg/mL(23.29 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

    EP300, IC50:0.051 μM

    CBP, IC50:0.03 μM
描述 Mutations in the CBP/EP300 bromodomain are linked to the onset of neurological disorders and lymphomas. CPI-637 is a selective and cell-active CBP/EP300 bromodomain inhibitor with IC50 values of 0.03±0.01, 0.051±0.004, 11.0±0.6μM for CBP, EP300, and BRD4 BD-1, respectively. The EC50 value of CPI-637 for CBP is 0.3±0.1μM. CPI-637 inhibited the expression of MYC, a transcription factor in human cancers, with an EC50 value of 0.60μM[2]. In mice inoculated with Q165P-mutant prostate cancer cells, combined treatment with CPI-637 (30mg/kg) and JQ1 (50mg/kg) five days a week for three consecutive weeks significantly reduced tumor volume and suppressed the phosphorylation of AKT, the expression of androgen receptor and its downstream target genes[3].
作用机制 CPI-637 is a selective benzodiazepinone CBP/EP300 bromodomain inhibitor. The benzodiazepinone core of CPI-637 recapitulated the key hydrogen bonding interactions with the indazole substituents filling space above Pro1110 and the Pro/Arg cleft[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.88mL

5.18mL

2.59mL
参考文献

[1]aylor AM, Côte A, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor(CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6.

[2]Taylor AM, Côté A, Hewitt MC, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016;7(5):531-536. Published 2016 Mar 15. doi:10.1021/acsmedchemlett.6b00075

[3]Yan Y, Ma J, Wang D, et al. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019;11(11):e10659. doi:10.15252/emmm.201910659