1357470-29-1
1357470-29-1 structure
- Name: ON-123300
- Chemical Name: on123300
- CAS Number: 1357470-29-1
- Molecular Formula: C24H27N7O
- Molecular Weight: 429.51700
- Catalog: Research Areas Cancer
- Create Date: 2018-05-23 14:25:12
- Modify Date: 2024-01-03 23:07:01
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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]
| Name | on123300 |
|---|---|
| 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 |
| 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 | |
| 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 |
| Molecular Formula | C24H27N7O |
|---|---|
| Molecular Weight | 429.51700 |
| Exact Mass | 429.22800 |
| PSA | 90.08000 |
| LogP | 3.34958 |
| Storage condition | -20℃ |