CAS 1357470-29-1|ON-123300
Introduction：Basic information about CAS 1357470-29-1|ON-123300, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | ON-123300 | ||
|---|---|---|---|
| CAS Number | 1357470-29-1 | Molecular Weight | 429.51700 |
| Density | / | Boiling Point | / |
| Molecular Formula | C24H27N7O | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | on123300 |
|---|---|
| Synonym | More Synonyms |
ON-123300 BiologicalActivity
| Description | ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.IC50 value: 3.8 nM [1]Target: CDK4in vitro: ON123300 is a novel kinase inhibitor, inhibits CDK4/6 and PI3K-δ and exhibits potent activity against mantle cell lymphomas (MCLs). [1] ON123300 is a low molecular weight multi-kinase inhibitor identified through a series of screens that supported further analyses for brain tumor chemotherapy. Biochemical assays indicated ON123300 was a strong inhibitor of Ark5 and CDK4 as well as growth factor receptor tyrosine kinases such as Beta-type platelet-derived growth factor receptor [PDGFRβ]. ON123300 inhibited U87 glioma cell proliferation with an IC50 = 3.4 ± 0.1 μM and reduced phosphorylation of Akt, yet it also unexpectedly induced Erk activation; both in a dose- and time-dependent manner that subsequently was attributed to relieving Akt-mediated C-Raf S259 inactivation and activating a p70S6K initiated PI3K negative feedback loop. [3] |
|---|---|
| Related Catalog | Research Areas >>Cancer |
| Target | Cdk4/cyclin D1:3.87 nM (IC50) CDK6/cyclinD1:9.82 nM (IC50) ARK5:4.95 nM (IC50) FGFR1:26 nM (IC50) PDGFRβ:26 nM (IC50) PI3K-δ:144 nM (IC50) |
| References | [1]. Divakar SK, et al. Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas. Leukemia. 2016 Jan;30(1):86-93. [2]. Perumal D, et al. Dual Targeting of CDK4 and ARK5 Using a Novel Kinase Inhibitor ON123300 Exerts Potent Anticancer Activity against Multiple Myeloma. Cancer Res. 2016 Mar 1;76(5):1225-36. [3]. Zhang X, et al. Preclinical pharmacological evaluation of a novel multiple kinase inhibitor, ON123300, in brain tumor models. Mol Cancer Ther. 2014 May;13(5):1105-16. |
Chemical & Physical Properties
| Molecular Formula | C24H27N7O |
|---|---|
| Molecular Weight | 429.51700 |
| Exact Mass | 429.22800 |
| PSA | 90.08000 |
| LogP | 3.34958 |
| InChIKey | VADOZMZXXRBXNY-UHFFFAOYSA-N |
| SMILES | CN1CCN(c2ccc(Nc3ncc4cc(C#N)c(=O)n(C5CCCC5)c4n3)cc2)CC1 |
| Storage condition | -20℃ |
Synonyms
| 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile |
| 8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile |
