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
Information
BS-181 HCl is a highly selectiveCDK7inhibitor withIC50of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
In vitro
BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.
In vivo
BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentration ~50 μM
Incubation Time：24 hours
Powder Purity:≥99%
规格
英文别名
N5-(6-aminohexyl)-N7-benzyl-3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diamine hydrochloride
规格或纯度
10mM in DMSO
英文名称
BS-181 HCl
生化机理
BS-181 HCl 是一种高选择性 CDK7 抑制剂，IC50 为 21 nM。它对 CDK7 的选择性是 CDK1、2、4、5、6 或 9 的 40 倍以上。
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=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCCCCCCN.Cl
关联CAS
分子量
416.99
Reaxy-Rn
26177980
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26177980&ln=
技术文档
高级数据
产品属性
| IC50 | CDK7, IC50: 21 nM |
|---|---|
| ALogP | 4.684 |
| hba_count | 2 |
| HBD Count | 3 |
| Rotatable Bond | 11 |
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 63 mg/mL (199.49 mM); Water: 63 mg/mL (199.49 mM); Ethanol: 1 mg/mL (3.16 mM);
DMSO(mg / mL) Max Solubility
83
DMSO(mM) Max Solubility
199.0455407
Water(mg / mL) Max Solubility
3
Water(mM) Max Solubility
7.194417132
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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