1. Immunology/Inflammation
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  3. AG-024322

AG-024322 

Cat. No.: HY-15491
Handling Instructions

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. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis.

For research use only. We do not sell to patients.

AG-024322 Chemical Structure

AG-024322 Chemical Structure

CAS No. : 837364-57-5

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Description

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].

IC50 & Target[1]

COX-1

2.3 nM (Ki)

COX-2

3 nM (Ki)

COX-4

2.9 nM (Ki)

In Vitro

AG-024322 (0.1-30 μM; 24 hours) is less toxic at concentrations below 3 µM, the viability of human PBMCs as measured by ATP content with a TC50 value of 1.4 µM for human PBMCs[2].
AG-024322 (0-120 nM) exhibits growth inhibition effects on HCT-116 cells. It is slightly less potent in the functional cellular assay with an IC50 of 120 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

418.44

Formula

C₂₃H₂₀F₂N₆

CAS No.

837364-57-5

SMILES

CC1=C(CNCC)C=NC=C1C2=CC3=C(NN=C3C4=NC5=CC(F)=CC(F)=C5N4)C=C2

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AG-024322AG024322AG 024322COXCyclooxygenaseAnticancerMyelotoxicityVascularirritationnon-Hodgkin’slymphomaLeukopeniaMTDMV522Inhibitorinhibitorinhibit

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AG-024322
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HY-15491
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