PHA-767491 HCl
别名: CAY10572, NMS 1116354
PHA-767491 (CAY10572, NMS 1116354) HCl是一种有效的，ATP竞争性的，双重Cdc7/CDK9抑制剂，无细胞试验中IC50分别为10 nM和34 nM，比作用于CDK1/2和GSK3-β选择性高20倍左右，比作用于MK2和CDK5选择性高50倍，比作用于PLK1和CHK2选择性高100倍。
PHA-767491 HCl Chemical Structure
CAS: 942425-68-5
产品质控
批次：
纯度：
99.96%
99.96
PHA-767491 HCl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human HeLa cells | Function assay | 5 μM | 24 h | Induction of apoptosis in human HeLa cells assessed as appearance of PARP at 5 uM after 24 hrs | 18469809 |
| NHDF | Function assay | 5 μM | 16 h | Induction of cell cycle arrest in thymidine deficient NHDF assessed as DNA synthesis in S-phase at 5 uM after 16hrs FACS analysis in presence of serum | 18469809 |
| human SF268 cells | Proliferation assay | 72 h | Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs, IC50=0.86 μM | 18469809 | |
| human HCT116 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=0.97 μM | 18469809 | |
| human HCT16 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT16 cells after 72 hrs by luciferase based assay, IC50=1 μM | 19115845 | |
| human SW403 cells | Proliferation assay | 72 h | Antiproliferative activity against human SW403 cells after 72 hrs by luciferase based assay, IC50=1 μM | 19115845 | |
| human A2780 cells | Proliferation assay | 72 h | Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=1.07 μM | 18469809 | |
| human SW48 cells | Proliferation assay | 72 h | Antiproliferative activity against human SW48 cells after 72 hrs by luciferase based assay, IC50=1.2 μM | 19115845 | |
| human MCF7 cells | Proliferation assay | 72 h | Antiproliferative activity against human MCF7 cells after 72 hrs by luciferase based assay, IC50=1.3 μM | 19115845 | |
| human U2OS cells | Proliferation assay | 72 h | Antiproliferative activity against human U2OS cells expressing p53 gene after 72 hrs by proliferative assay, IC50=1.49 μM | 18469809 | |
| human COLO205 cells | Proliferation assay | 72 h | Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay, IC50=1.5 μM | 19115845 | |
| human OVCAR8 cells | Proliferation assay | 72 h | Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay, IC50=1.56 μM | 18469809 | |
| human L363 cells | Proliferation assay | 72 h | Antiproliferative activity against human L363 cells after 72 hrs by luciferase based assay, IC50=1.6 μM | 19115845 | |
| human NHDF cells | Proliferation assay | 72 h | Antiproliferative activity against human NHDF cells after 72 hrs by luciferase based assay, IC50=1.6 μM | 19115845 | |
| human NCI-H929 cells | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H929 cells after 72 hrs by luciferase based assay, IC50=1.8 μM | 19115845 | |
| human SF539 cells | Proliferation assay | 72 h | Antiproliferative activity against human SF539 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=2.34 μM | 18469809 | |
| human SW480 cells | Proliferation assay | 72 h | Antiproliferative activity against p53 deficient human SW480 cells after 72 hrs by proliferative assay, IC50=2.67 μM | 18469809 | |
| human Jurkat cells | Proliferation assay | 72 h | Antiproliferative activity against p53 deficient human Jurkat cells after 72 hrs by proliferative assay, IC50=3.2 μM | 18469809 | |
| human HCT15 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay, IC50=3.81 μM | 18469809 | |
| human OPM2 cells | Proliferation assay | 72 h | Antiproliferative activity against human OPM2 cells after 72 hrs by luciferase based assay, IC50=4.5 μM | 19115845 | |
| human HT-29 cells | Proliferation assay | 72 h | Antiproliferative activity against human HT-29 cells after 72 hrs by luciferase based assay, IC50=5 μM | 19115845 | |
| human K562 cells | Proliferation assay | 72 h | Antiproliferative activity against p53 deficient human K562 cells after 72 hrs, IC50=5.87 μM | 18469809 | |
| human NCI60 cells | Proliferation assay | Antiproliferative activity against human NCI60 cells, IC50=3.1 μM | 18469809 | ||
| U937 cells | Function assay | Inhibition of TNFalpha production in U937 cells, IC50=19 μM | 17480064 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PHA-767491 (CAY10572, NMS 1116354) HCl是一种有效的，ATP竞争性的，双重Cdc7/CDK9抑制剂，无细胞试验中IC50分别为10 nM和34 nM，比作用于CDK1/2和GSK3-β选择性高20倍左右，比作用于MK2和CDK5选择性高50倍，比作用于PLK1和CHK2选择性高100倍。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | PHA-767491是第一个通过控制 DNA 复制起始而不是延伸阶段而影响机制的抑制剂。 | |||||||||||
| 靶点 |
|
化学信息&溶解度
| 分子量 | 249.7 | 分子式 | C12H11N3O.HCl |
| CAS号 | 942425-68-5 | SDF | Download PHA-767491 HCl SDF |
| Smiles | C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3.Cl | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 24 mg/mL ( (96.11 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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