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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
AZD7762, 丝氨酸/苏氨酸蛋白激酶 Chk1 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，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
AZD7762是Chk1的抑制剂，IC50为5 nM，对Chk2的抑制性与Chk1相近，但对CAM，Yes，Fyn，Lyn，Hck和Lck的抑制性较弱。
Information
AZD7762 is a potent and selective inhibitor ofChk1withIC50of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.
In vitro
AZD7762, a more selective Chk1 inhibitor, inhibits Chk1 phosphorylation of a cdc25C peptide by reversibly binding to the ATP-binding site of Chk1, with IC50 of 5 nM and Ki of 3.6 nM. AZD7762 induces cell arrest with EC50 of 0.620 μM, and significantly abrogates the camptothecin induced G2 arrest with an EC50 of 10 nM, by blocking the chk1 dependent degradation of Cdc25A and activation of Cyclin A. AZD7762 (300 nM) enhances the antitumor efficacy of gemcitabine against SW620 and topotecan against MDA-MB-231 by reducing the GI50 values from 24.1 nM and 2.25 μM to 1.08 nM and 0.15 μM, respectively. AZD7762 shows cytotoxicity against a variety of neuroblastoma cell lines bearing p53 wild type, p53 mutation, Mdm2 amplification or p14 deletion with IC50 values ranging from 82.6-505.9 nM.
In vivo
AZD7762 alone at 25 mg/kg shows little antitumor activity in the H460-DNp53 xenograft mice and SW620 xenograft mice, but when administrated in combination with gemcitabine (60 mg/kg), AZD7762 shows significant antitumor efficacy in the two xenografts mice with a log cell kill of 0.9 or percent treated/control (%T/C) of 26 even at low dose of 12.5 mg. Dosing of AZD7762 in combination with gemcitabine (10 mg/kg) in the H460-DNp53 xenograft rat inhibits the tumor volume in a dose-dependent manner with the %T/C values of 48 and 32 for 10 and 20 mg/kg AZD7762, respectively. AZD7762 (25 mg/kg) in combination with irinotecan (25 or 50 mg/kg) causes complete tumor regression in the SW620 xenograft mice with the %T/C increasing significantly to -66% and -67%, respectively.
Cell Data
cell lines：EpoBa/F3 JAK2V617F, Ba/F3p210, HEL, and K562
Concentrations：Dissolved in DMSO, final concentration ~12.5 μM
Incubation Time：20 or 48 hours
Powder Purity:≥97%
规格
英文别名
1-(2-((S)-piperidin-3-ylcarbamoyl)-5-(3-fluorophenyl)thiophen-3-yl)urea
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AZD7762
生化机理
AZD7762 是一种强效的 Chk1 选择性抑制剂，在无细胞试验中的 IC50 为 5 nM。它对 Chk2 同样有效，而对 CAM、Yes、Fyn、Lyn、Hck 和 Lck 的抑制作用较弱。第 1 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
丝氨酸/苏氨酸蛋白激酶 Chk1 抑制剂
名称和识别符
EC号
804-400-3
分子类型
小分子
Isomeric SMILES
C1C[C@@H](CNC1)NC(=O)C2=C(C=C(S2)C3=CC(=CC=C3)F)NC(=O)N
分子量
362.42
Reaxy-Rn
26001216
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26001216&ln=
技术文档
高级数据
产品属性
| ALogP | 2.3 |
|---|
关联靶点（人）
RET
Tclin
原癌基因酪氨酸蛋白激酶受体 Ret(Proto-oncogene tyrosine-protein kinase receptor Ret)
(1 活性数据)
SIK2
Tchem
丝氨酸/苏氨酸蛋白激酶SIK2(Serine/threonine-protein kinase SIK2)
(1 活性数据)
BCR
Tclin
断点簇区域蛋白质(Breakpoint cluster region protein)
(1 活性数据)
Tchem
未表征蛋白 FLJ45252(Uncharacterized protein FLJ45252)
(1 活性数据)
PRKAG2
Tchem
5'-AMP活化蛋白激酶亚基γ-2(5'-AMP-activated protein kinase subunit gamma-2)
(1 活性数据)
CHEK1
Tchem
丝氨酸/苏氨酸蛋白激酶 Chk1(Serine/threonine-protein kinase Chk1)
(7 活性数据)
CHEK2
Tchem
丝氨酸/苏氨酸蛋白激酶 Chk2(Serine/threonine-protein kinase Chk2)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 49 mg/mL (201.07 mM); Ethanol: 49 mg/mL (201.07 mM); Water: Insoluble;
安全和危险性（GHS）
信号词
危险
危险声明
H302: 吞食有害
H318: 造成严重的眼睛损伤
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:
技术文档和文章
溶液计算器
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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