计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
CPI-455 is a specific, pan- KDM5 inhibitor with an IC 50 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
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. ?\nCPI-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. IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dual blockade of B7-H4 and KDM5B (CPI-455, 50/70 mg/kg, ip, daily) in mice elicits protective immunity. MCE 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.
IC50& Target:KDM5
规格
规格或纯度
10mM in DMSO
英文名称
CPI-455
生化机理
CPI-455 是一种特异性泛 KDM5 抑制剂，对 KDM5A 的 IC50 为 10 nM。CPI-455 可介导 KDM5 抑制作用，提高 H3K4me3 的整体水平，并在多个癌细胞系模型中减少耐药顽固癌细胞的数量。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)C1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3
分子量
278.31
Reaxy-Rn
32509184
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=32509184&ln=
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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技术文档和文章
溶液计算器
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