CPI-455|1628208-23-0|-陌孚医药/Medlife

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CPI-455

目录号: PC10205 纯度: ≥98%

CAS No. :1628208-23-0

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PC10205-5mg	5mg	¥833.00	请登录
PC10205-25mg	25mg	¥3136.00	请登录

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中文名称

CPI-455

中文别名

6-异丙基-7-氧代-5-苯基-4,7-二氢吡唑并[1,5-a]嘧啶-3-腈;CPI-455

英文名称

CPI-455

英文别名

6-Isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile;CPI455;CPI-455;s8287;AK685833;CPI-455 hydrochloride

Cas No.

1628208-23-0

分子式

C₁₆H₁₅ClN₄O

分子量

314.77

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

CPI-455 is a specific, pan-KDM5 inhibitor with an IC₅₀ of 10 nM for KDM5A. CPI-455 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.

性状

Solid

IC50 & Target[1][2]

IC50: 10 nM (KDM5A)

体外研究(In Vitro)

CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
CPI-455, with high measured affinity for the target KDM5 proteins. Within 24 hours, increases in H3K4me3, are observed after exposure to either of the two active compounds, CPI-455 and CPI-766, in a dosedependent manner. IC₅₀ calculation for KDM5 Inhibitor CPI0455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Dual blockade of B7-H4 and KDM5B (CPI-455, 50/70 mg/kg, ip, daily) in mice elicits protective immunity.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old male C57BL/6 mice (One- to 2-mm fragments of P. gingivalis–positive PDXs were implanted subcutaneously into the flank region of humanized mice.)
Dosage:	50 mg/kg or 70 mg/kg (combined with anti–B7-H4).
Administration:	IP, daily, 14-28 days.
Result:	Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge. Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : ≥ 34 mg/mL (122.17 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5931 mL	17.9656 mL	35.9312 mL
5 mM	0.7186 mL	3.5931 mL	7.1862 mL
10 mM	0.3593 mL	1.7966 mL	3.5931 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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