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942425-68-5 (PHA-767491 (hydrochloride))

1

Identification

PHA-767491 (hydrochloride) PHA-767491 (hydrochloride)
Name PHA-767491 (hydrochloride)
Formula C12H12ClN3O
MW 249.7
CAS No. 942425-68-5
EINECS
Smiles O=C1C2=C(NC(C3=CC=NC=C3)=C2)CCN1.[H]Cl
Synonyms CAY-10572 hydrochloride; 2-(pyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one hydrochloride
InChI InChI=1S/C12H11N3O.ClH/c16-12-9-7-11(8-1-4-13-5-2-8)15-10(9)3-6-14-12;/h1-2,4-5,7,15H,3,6H2,(H,14,16);1H
2

Introduction

PHA-767491 (CAY10572) Hcl is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor with IC50 values of 10/34 nM.

Background Information

PHA-767491 hydrochloride is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor, which prevents initiation of DNA replication. It inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. It als ......by BOC Sciences
PHA-767491 is a potent and selective ATP-competitive dual cdc7/cdk9 inhibitor.  ......by BioVision, Inc.,
PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively. ......by MedChemexpress Co., Ltd.
PHA-767491, also known as CAY10572, is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. PHA-767491 in combination with 5-FU exhibited much stronger cytotoxicity and induced significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracted the 5-FU-induced phosphorylation of Chk1, a substrate of Cdc7; and decreased the expression of the anti-apoptotic protein myeloid leukemia cell 1, a downstream target of Cdk9. ......by MedKoo Biosciences, Inc.
PHA-767491 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. ......by Selleck Chemicals LLC
Potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 μM) and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2) (IC50 = 171 nM). ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000071830

Storage condition

4°C by MedChemexpress Co., Ltd.
Desiccate at RT by Tocris Bioscience Inc.

Solubility

100 mM in water ; 100 mM in DMSO ; by CHEMSCENE, LLC
100 mM in water ; 100 mM in DMSO ; by MedChemexpress Co., Ltd.
Soluble to 100 mM in water and to 100 mM in DMSO by Tocris Bioscience Inc.
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Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
PHA-767491 (hydrochloride) - Not Found
PHA-767491 (hydrochloride) - No Development Reported
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Safety Data of PHA-767491 (hydrochloride)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
Ark Pharm, Inc. USA
BLD Pharmatech
BOC Sciences
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD86();50mg/USD355() USA
MedChemexpress Co., Ltd. 10mg/USD86();50mg/USD355() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD86();50mg/USD355() China
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 942425-68-5

Name CAS No Formula MW
PHA-767491 845714-00-3 C12H11N3O 213.24

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

PHA-767491 (hydrochloride)

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