ON123300

ON123300, a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. ON123300 inhibits CDK6 with an IC50 of 9.82 nM.

Product information

CAS Number: 1357470-29-1

Molecular Weight: 429.52

Formula: C24H27N7O

Chemical Name: 8-cyclopentyl-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-7-oxo-7H,8H-pyrido[2,3-d]pyrimidine-6-carbonitrile

Smiles: CN1CCN(CC1)C1C=CC(=CC=1)NC1N=C2C(C=C(C#N)C(=O)N2C2CCCC2)=CN=1

InChiKey: VADOZMZXXRBXNY-UHFFFAOYSA-N

InChi: InChI=1S/C24H27N7O/c1-29-10-12-30(13-11-29)20-8-6-19(7-9-20)27-24-26-16-18-14-17(15-25)23(32)31(22(18)28-24)21-4-2-3-5-21/h6-9,14,16,21H,2-5,10-13H2,1H3,(H,26,27,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 16.67 mg/mL (38.81 mM; ultrasonic and warming and heat to 60°C).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ON123300 inhibits U87 glioma cell proliferation with an IC50 of 3.4±0.1 μM.ON123300 (1 and 10 μM) inhibits cell proliferation in a panel of 11 glioma models including a patient-derived model (GBM10). ON123300 (6.3 μM; 1 h) reduces phosphorylation of Akt and its downstream signaling components, P70S6K, 40S rpS6 and Rb S780, yet ON123300 induces Erk activation in U87 cells; both in a dose- and time-dependent manner.ON123300 inhibits PI3Kδ with the IC50 of 144nM.

In Vivo:

ON123300 decreases p-Akt expression and increases p-Erk activity in brain tumors upon administration at both IV doses of 5 mg/kg and 25 mg/kg in U87 brain tumor-bearing mouse. The half-life (T1/2) is 1.5 h for 5 mg/kg and 25 mg/kg in plasma.

Products are for research use only. Not for human use.