A multi-kinase inhibitor; inhibits ARK5

ON-123300 – 5 mg

Brand:
Cayman
CAS:
1357470-29-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

ON-123300 is a multi-kinase inhibitor.{43515,43516} It inhibits ARK5, Cdk4, and Cdk6 (IC50s = 3.87, 9.82, and 4.95 nM, respectively) as well as FYN, PDGFRβ, Abl, and PI3Kδ (IC50s = 11.09, 26, 53.32, and 144 nM, respectively) among others.{43516} It inhibits proliferation in a panel of 38 cancer cell lines (GI50s = 0.05-5 µM).{43516} ON-123300 also inhibits proliferation of U87 glioma cells (IC50 = 3.4 µM), decreases phosphorylation of Akt and activates ERK, as well as halts the cell cycle in the G2/M phase and induces apoptosis.{43515} When used in combination with the EGFR inhibitor gefitinib (Item No. 13166), it synergistically induces cytotoxicity of U87, U87 VIII, and U87 PTEN cells. ON-123300 reduces tumor growth in an MDA-MB-231 mouse xenograft model when administered at a dose of 50 mg/kg every other day.{43516}  

 

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Description

A multi-kinase inhibitor; inhibits ARK5, Cdk4, and Cdk6 (IC50s = 3.87, 9.82, and 4.95 nM, respectively); inhibits FYN, PDGFRβ, Abl, and PI3Kδ (IC50s = 11.09, 26, 53.32, and 144 nM, respectively) among others; inhibits proliferation in a panel of 38 cancer cell lines (GI50s = 0.05-5 µM); also inhibits proliferation of U87 glioma cells (IC50 = 3.4 µM); reduces tumor growth in an MDA-MB-231 mouse xenograft model at 50 mg/kg every other day

Formal name: 8-cyclopentyl-7,8-dihydro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-7-oxo-pyrido[2,3-d]pyrimidine-6-carbonitrile

Synonyms: 

Molecular weight: 429.5

CAS: 1357470-29-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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