ChemicalBook CAS DataBase List 837364-57-5

837364-57-5

Name	AG-024322
CAS	837364-57-5
Molecular Formula	C23H20F2N6
MDL Number	MFCD11100348
Molecular Weight	418.44
MOL File	837364-57-5.mol

Chemical Properties

Boiling point	668.4±65.0 °C(Predicted)
density	1.361±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
form	Solid
pka	7.84±0.30(Predicted)
color	White to off-white

Hazard Information

Uses

AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range[1]. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation?in vivo. AG-024322 induces cell apoptosis[3].

in vivo

AG-024322 (intravenous infusion; 2, 6, and 10 mg/kg; 5 days) exhibits no-adverse-effect at 2 mg/kg with mean plasma AUC (0-24.5) of 2.11 g.h/mL. At 6 mg/kg produces pancytic bone marrow hypocellularity, lymphoid depletion. And vascular injury at the injection site renal tubular degeneration occurs at 10 mg/kg^[1].AG-024322 (20 mg/kg) inhibits the growth of established human tumor xenografts of different origins with tumor growth inhibition (TGI) ranging from 32% to 86.4%.It also exhibits anti-tumor effects as a dose-pdependent manner^[3].AG-024322 (20 mg/kg) causes a 65% TGI in the MV522 tumor model. It results a 52% TGI at 1/2 of the maximum tolerated dose (MTD) and only slight anti-tumor activity at 1/4 of the MTD^[3].

Animal Model:	Male and female cynomolgus monkeys^[1]
Dosage:	2, 6, and 10 mg/kg (Toxicity analysis)
Administration:	Intravenous infusion; 5 days
Result:	Resulted in dose-dependent pancytic bone marrow hypocellularity and lymphoid depletion in lymph nodes, spleen, and/or thymus at >6 mg/kg.

IC 50

COX-1: 2.3 nM (Ki); COX-2: 3 nM (Ki); COX-4: 2.9 nM (Ki)

storage

Store at -20°C

References

[1] Brown AP, et al. Toxicity and toxicokinetics of the cyclin-dependent kinase inhibitor AG-024322 in cynomolgus monkeys following intravenous infusion.Cancer Chemother Pharmacol. 2008 Nov;62(6):1091-101. DOI:10.1007/s00280-008-0771-1
[2] Jessen BA,et al. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.J Appl Toxicol. 2007 Mar-Apr;27(2):133-42. DOI:10.1002/jat.1177
[3] Cathy C.?Zhang, et al. AG-024322 is a multi-targeted CDK inhibitor with potent antitumor activity?in vivo. Cellular and Molecular Biology 53: Cell Cycle Control and Cancer 1

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