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ON123300

Cat. No. M7557
ON123300  Structure
Size Price Availability Quantity
5mg USD 145 In stock
10mg USD 220 In stock
25mg USD 440 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: ON123300 is a novel kinase inhibitor, inhibits CDK4/6 and PI3K-δ and exhibits potent activity against mantle cell lymphomas (MCLs). 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.

Protocol
Cell Experiment
Cell lines MM1.S and NCI-H929 cells
Preparation method MM1.S and NCI-H929 cells were treated with ON123300/PD-0332991 for 24 hours. Approximately 106 cells of each cell line were harvested (along with untreated controls) after 24 hours of treatment in 12-well plates. Cells were washed with PBS and resuspended in appropriate volume of Annexin binding buffer and then stained with Annexin V Pacific Blue/PI.
Concentrations 50 nmol/L
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 429.52
Formula C24H27N7O
CAS Number 1357470-29-1
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

Dual Targeting of CDK4 and ARK5 Using a Novel Kinase Inhibitor ON123300 Exerts Potent Anticancer Activity against Multiple Myeloma.
Perumal D, et al. Cancer Res. 2016 Mar 1;76(5):1225-36. PMID: 26873845.

Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas.
Divakar SK, et al. Leukemia. 2016 Jan;30(1):86-93. PMID: 26174628.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ON123300 supplier, CDK, inhibitors

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