PHA 767491 HYDROCHLORIDE

Product Name: PHA 767491 HYDROCHLORIDE
CAS No.: 845714-00-3
Chemical Name: PHA 767491 HYDROCHLORIDE
Synonyms: CS-229;CAY10572;PHA-767491;PHA-767491HCL;Cdc7/Cdk9 Inhibitor;CAY10572(PHA-767491);PHA 767491;PHA-767491;PHA-767491 (CAY10572);PHA 767491 HYDROCHLORIDE;PHA-767491, 10 mM in DMSO
CBNumber: CB02458643
Molecular Formula: C12H11N3O
Formula Weight: 213.24
MOL File: 845714-00-3.mol

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PHA 767491 HYDROCHLORIDE Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 18218
Product name: PHA-767491
Purity: ≥98%
Packaging: 5mg
Price: $35
Updated: 2021/12/16

Cayman Chemical

Product number: 18218
Product name: PHA-767491
Purity: ≥98%
Packaging: 10mg
Price: $60
Updated: 2021/12/16

Cayman Chemical

Product number: 18218
Product name: PHA-767491
Purity: ≥98%
Packaging: 25mg
Price: $140
Updated: 2021/12/16

Cayman Chemical

Product number: 18218
Product name: PHA-767491
Purity: ≥98%
Packaging: 50mg
Price: $245
Updated: 2021/12/16

Tocris

Product number: 3140
Product name: PHA 767491 hydrochloride
Purity: ≥99%(HPLC)
Packaging: 50
Price: $635
Updated: 2021/12/16

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PHA 767491 HYDROCHLORIDE Chemical Properties,Usage,Production

Uses

PHA 767491 is a potent and selective ATP-competitive dual inhibitor cdc7/cdk9. It blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2).

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]

Definition

ChEBI: 2-pyridin-4-yl-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one is a pyrrolopyridine.

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).

in vivo

PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts^[2].

target

cdc7

IC 50

CDK9: 34 nM (IC₅₀); CDK2: 240 nM (IC₅₀); CDK1: 250 nM (IC₅₀); CDK5: 460 nM (IC₅₀); GSK3-β: 220 nM (IC₅₀); Mk2: 470 nM (IC₅₀); Plk1: 980 nM (IC₅₀); Chk2: 1100 nM (IC₅₀)

PHA 767491 HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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PHA 767491 HYDROCHLORIDE Suppliers

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View Lastest Price from PHA 767491 HYDROCHLORIDE manufacturers

Career Henan Chemical Co

Product: PHA 767491 HYDROCHLORIDE 845714-00-3
Price: US $9.80/KG
Min. Order: 1g
Purity: ≥99%
Supply Ability: 100kg
Release date: 2019-12-25

845714-00-3, PHA 767491 HYDROCHLORIDERelated Search:

Selumetinib Alectinib Saracatinib Dabrafenib LDC000067 Roscovitine

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

PHA-767491, 10 mM in DMSO

Cdc7/Cdk9 Inhibitor

845714-00-3

C12H11N3OHCl

Inhibitors