Home Cell Cycle CDK inhibitor PHA-767491 HCl For research use only.

PHA-767491 HCl

Synonyms: CAY10572, NMS 1116354

PHA-767491 (CAY10572, NMS 1116354) HCl is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2.

PHA-767491 HCl Chemical Structure

PHA-767491 HCl Chemical Structure

CAS No. 942425-68-5

Purity & Quality Control

PHA-767491 HCl Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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 NCI60 cells Proliferation assay Antiproliferative activity against human NCI60 cells, IC50=3.1 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
U937 cells Function assay Inhibition of TNFalpha production in U937 cells, IC50=19 μM 17480064
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
Click to View More Cell Line Experimental Data

Biological Activity

Description PHA-767491 (CAY10572, NMS 1116354) HCl is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2.
Features The first inhibitor that directly affects the mechanisms controlling initiation as opposed to elongation in DNA replication.
Targets
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)		 Click to View More Targets
10 nM 34 nM 220 nM 240 nM 250 nM

Chemical Information & Solubility

Molecular Weight 249.7 Formula

C12H11N3O.HCl
CAS No. 942425-68-5 SDF Download PHA-767491 HCl SDF
Smiles C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 24 mg/mL ( (96.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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