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PHA 767491 HYDROCHLORIDE

PHA 767491 HYDROCHLORIDE Structure
CAS No.
845714-00-3
Chemical Name:
PHA 767491 HYDROCHLORIDE
Synonyms
CS-229;CAY10572;PHA-767491;PHA-767491HCL;CAY10572(PHA-767491);PHA 767491;PHA-767491;PHA-767491 (CAY10572);PHA 767491 HYDROCHLORIDE;PHA 767491 HYDROCHLORIDE USP/EP/BP;PHA-767491;CAY10572;PHA767491;PHA 767491
CBNumber:
CB02458643
Molecular Formula:
C12H11N3O
Molecular Weight:
213.24
MOL File:
845714-00-3.mol
MSDS File:
SDS
Modify Date:
2023/5/18 11:31:13

PHA 767491 HYDROCHLORIDE Properties

Density 1.287
storage temp. Desiccate at RT
solubility insoluble in H2O; insoluble in EtOH; ≥10.65 mg/mL in DMSO
form solid
Stability Hygroscopic
CAS DataBase Reference 845714-00-3

PHA 767491 HYDROCHLORIDE Chemical Properties,Uses,Production

Uses

Cdc7 kinase is a key regulator of the S-phase of the cell cycle. It is known to promote the activity of DNA replication origins in eukaryotic organisms. Inhibition of Cdc7 kinase causes blockade of DNA synthesis in human cell lines. Tumor cells are then funneled into the apoptotic pathway in a p53-independent manner. Pharmacological inhibition of Cdc7 kinase can be an effective strategy for the development of oncologic therapeutics useful for treatment of cancers. PHA 767491 HYDROCHLORIDE is a potent inhibitor of Cdc7 kinase with an IC50 value of 10 nM in the presence of 1.5 μM ATP. At 10 μM, PHA 767491 HYDROCHLORIDE induces apoptotic cell death in multiple cancer cell types. PHA 767491 HYDROCHLORIDE also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression, with an IC50 value of 34 nM.[Cayman Chemical]

Biological Activity

Potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC 50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines (IC 50 ~ 0.86 - 5.87 μ M) and induces apoptosis in a p53-independent manner in vivo . Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2) (IC 50 = 171 nM).

PHA 767491 HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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PHA 767491 HYDROCHLORIDE Spectrum

845714-00-3(PHA 767491 HYDROCHLORIDE)Related Search:

PHA-767491 CAY10572 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one PHA 767491 HYDROCHLORIDE 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-onehydrochloride 2-(pyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one 2-pyridin-4-yl-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one PHA-767491HCL PHA-767491;CAY10572;PHA767491;PHA 767491 PHA-767491 (CAY10572) PHA 767491;PHA-767491 CS-229 CAY10572(PHA-767491) 4H-Pyrrolo[3,2-c]pyridin-4-one, 1,5,6,7-tetrahydro-2-(4-pyridinyl)- PHA 767491 HYDROCHLORIDE USP/EP/BP PHA-767491 PHA767491 Dihydrochloride Salt 845714-00-3 C12H11N3OHCl Inhibitors