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PHA-767491 HCl

別名: CAY10572, NMS 1116354

PHA-767491 (CAY10572, NMS 1116354) HCl是一種有效的，ATP競爭性的，雙重Cdc7/CDK9抑制劑，無細胞試驗中IC50分別為10 nM和34 nM，比作用于CDK1/2和GSK3-β選擇性高20倍左右，比作用于MK2和CDK5選擇性高50倍，比作用于PLK1和CHK2選擇性高100倍。

PHA-767491 HCl Chemical Structure

PHA-767491 HCl Chemical Structure

CAS: 942425-68-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 984.14 現(xiàn)貨
10mg 735.92 現(xiàn)貨
50mg 3015.12 現(xiàn)貨
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PHA-767491 HCl相關產(chǎn)品

相關信號通路圖

CDK Signaling Pathways

CDK信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 PHA-767491 (CAY10572, NMS 1116354) HCl是一種有效的，ATP競爭性的，雙重Cdc7/CDK9抑制劑，無細胞試驗中IC50分別為10 nM和34 nM，比作用于CDK1/2和GSK3-β選擇性高20倍左右，比作用于MK2和CDK5選擇性高50倍，比作用于PLK1和CHK2選擇性高100倍。
特性 PHA-767491是第一個通過控制 DNA 復制起始而不是延伸階段而影響機制的抑制劑。
靶點
Cdc7 [1]
(Cell-free assay)		 CDK9 [1]
(Cell-free assay)		 GSK-3β [1]
(Cell-free assay)		 CDK2 [1]
(Cell-free assay)		 CDK1 [1]
(Cell-free assay)		 點擊更多
10 nM 34 nM 220 nM 240 nM 250 nM

化學信息&溶解度

分子量 249.7 分子式

C12H11N3O.HCl
CAS號 942425-68-5 SDF Download PHA-767491 HCl SDF
Smiles C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3.Cl
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 24 mg/mL ( (96.11 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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