|1,5,6,7-四氢-2-(4-吡啶基)-4H-吡咯并[3,2-c]吡啶-4-酮盐酸盐|CsnPharm

CAS No.: 942425-68-5

2-(Pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride Catalog No. CSN18614

Synonyms: CAY-10572 hydrochloride;CAY-10572 HCl;PHA-767491 (hydrochloride)

PHA-767491 HCl is a potent and ATP-competitive cyclin-dependent kinase (cdk) inhibitor with IC50 values of 10/34 nM for Cdc7/Cdk9.

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实验方案

技术信息

生物活性

描述Cdc7 is an essential kinase that promotes DNA replication by activating origins of replication. PHA-767491 is an effective, ATP-competitive, dual Cdc7/CDK9 inhibitor with IC₅₀s of 10 nM and 34 nM, respectively. Cell proliferation was inhibited in a panel of 61 human cell lines challenged with low micromolar concentrations of PHA-767491, with an average IC₅₀ value of 3.17 mM and less than 10 mM in all cases. In a smaller panel of 17 different cell types, using sub-G1 DNA content as a parameter of apoptosis, 24 h of exposure to either 5 or 10 mM PHA-767491 was sufficient to cause cell death. Importantly, PHA-767491 is capable of preventing duplication, and it can kill both p53-positive and p53-negative tumor cells of different origins. Treatment with 5 mM PHA-767491 for 6 to 9 hours in HeLa cells was necessary to observe a marked decrease in the number of bromodeoxyuridine (BrdU)-positive cells. After intravenous administration at two dose levels of 20 and 30 mg/kg twice a day for five consecutive days in nude mice carrying subcutaneous implanted tumors, a dose-dependent reduction in tumor volume with respect to vehicle-treated animals was observed^[3].
作用机制PHA-767491 competes with ATP for binding site, thus behaving as a pure ATP competitor.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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 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 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

更多
动物研究
剂量
Mice: 20 mg/kg, 30 mg/kg^[3] (i.v., BID); 25 mg/kg^[4] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg, 30 mg/kg^[3] (i.v., BID); 25 mg/kg^[4] (i.p.)
给药途径	i.v., i.p.

[1] Natoni A, Murillo LS, et al. Mechanisms of action of a dual Cdc7/Cdk9 kinase inhibitor against quiescent and proliferating CLL cells. Mol Cancer Ther. 2011 Sep;10(9):1624-34.
[2] Swords R, Mahalingam D, et al. Cdc7 kinase - a new target for drug development. Eur J Cancer. 2010 Jan;46(1):33-40.
[3] Montagnoli A, Valsasina B, Croci V, Menichincheri M, Rainoldi S, Marchesi V, Tibolla M, Tenca P, Brotherton D, Albanese C, Patton V, Alzani R, Ciavolella A, Sola F, Molinari A, Volpi D, Avanzi N, Fiorentini F, Cattoni M, Healy S, Ballinari D, Pesenti E, Isacchi A, Moll J, Bensimon A, Vanotti E, Santocanale C. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. doi: 10.1038/nchembio.90. Epub 2008 May 11. PMID: 18469809.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0048 mL
- 20.0240 mL
- 40.0481 mL
- 5 mM
- 0.8010 mL
- 4.0048 mL
- 8.0096 mL
- 10 mM
- 0.4005 mL
- 2.0024 mL
- 4.0048 mL

技术信息

CAS号

942425-68-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H12ClN3O

运输

蓝冰

分子量

249.70

别名

CAY-10572 hydrochloride;CAY-10572 HCl;PHA-767491 (hydrochloride);PHA-767491;CAY-10572

溶解度

DMSO	24.0 mg/mL (96.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+30% PEG 300+2% Tween 80+water

1 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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 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 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 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 HCT16 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HCT16 cells after 72 hrs by luciferase based assay, IC50=1 μM	19115845
human HeLa cells	5 μM	Function assay	24 h	Induction of apoptosis in human HeLa cells assessed as appearance of PARP at 5 uM after 24 hrs	18469809
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 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 K562 cells	-	Proliferation assay	72 h	Antiproliferative activity against p53 deficient human K562 cells after 72 hrs, IC50=5.87 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 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 NCI60 cells	-	Proliferation assay	-	Antiproliferative activity against human NCI60 cells, IC50=3.1 μM	18469809
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 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 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 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 SF268 cells	-	Proliferation assay	72 h	Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs, IC50=0.86 μM	18469809
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 SW403 cells	-	Proliferation assay	72 h	Antiproliferative activity against human SW403 cells after 72 hrs by luciferase based assay, IC50=1 μM	19115845
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 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 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
NHDF	5 μM	Function assay	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
U937 cells	-	Function assay	-	Inhibition of TNFalpha production in U937 cells, IC50=19 μM	17480064

2-(Pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride Catalog No. CSN18614

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