6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride

Modify Date: 2024-04-06 18:20:45

6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride Structure
6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride structure
Common Name 6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride
CAS Number 2095432-28-1 Molecular Weight 314.770
Density N/A Boiling Point N/A
Molecular Formula C16H15ClN4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride


CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].

 Names

Name CPI-455 Hydrochloride
Synonym More Synonyms

  Biological Activity

Description CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].
Related Catalog
Target

KDM5

In Vitro CPI-455 hydrochloride 介导 KDM5 抑制,提高 H3K4 三甲基化 (H3K4me3) 的总体水平,并减少使用标准化疗或靶向药物治疗的多种癌细胞系模型中的 DTP 数量[1]。 CPI-455 盐酸盐,对目标 KDM5 蛋白具有高亲和力。在 24 小时内,在暴露于两种活性化合物 CPI-455 和 CPI-766 中的任何一种后,观察到 H3K4me3 以剂量依赖性方式增加。 KDM5 Inhibitor CPI0455 在 3 种管腔乳腺癌细胞系 MCF-7、T-47 和 EFM-19 中的 IC50 计算值分别为 35.4、26.19 和 16.13 μM[2]。
In Vivo 在小鼠体内双重阻断 B7-H4 和 KDM5B(CPI-455 hydrochloride,50/70 mg/kg,腹腔注射,每日)可引发保护性免疫[2]。
References

[1]. Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8.  

[2]. Benjamin R. Leadem. NOVEL HISTONE DEMETHYLASE INHIBITORS SYNERGISTICALLY

[3]. Xiang Yuan, et al. Blockade of Immune-Checkpoint B7-H4 and Lysine Demethylase 5B in Esophageal Squamous Cell Carcinoma Confers Protective Immunity against P. gingivalis Infection. Cancer Immunol Res. 2019 Sep;7(9):1440-1456.  

 Chemical & Physical Properties

Molecular Formula C16H15ClN4O
Molecular Weight 314.770
Exact Mass 314.093445
Storage condition Inert atmosphere,2-8°C

 Synonyms

6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride (1:1)
Pyrazolo[1,5-a]pyrimidine-3-carbonitrile, 4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl-, hydrochloride (1:1)