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  3. GS-9901

GS-9901 

Cat. No.: HY-100694
Handling Instructions

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis.

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

GS-9901 Chemical Structure

GS-9901 Chemical Structure

CAS No. : 1640247-87-5

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Description

GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1].

IC50 & Target[1]

PI3Kδ

1 nM (IC50)

In Vivo

GS-9901 (0.3/1/3 mg/kg, orally, twice daily for 7 days) demonstrates efficacy in a rat model of arthritis and is predicted to be suitable for q.d. dosing in humans[1].

Animal Model: Female Lewis rats with established collagen-induced arthritis (CIA)[1].
Dosage: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg.
Administration: Orally, twice-daily for 7 days starting on the 10th day after the second collagen immunization.
Result: Demonstrated significant reduction in ankle swelling in rats treated with 0.3 mg/kg 35 (31% reduction), 1 mg/kg 35 (67%), and 3 mg/kg 35 (65%).
Plasma concentrations measured on day 7 (12 h after last dose) were consistent with maintaining approximately 60%, 80%, and >90% inhibition of PI3Kδ at 0.3, 1.0, and 3 mg/kg doses, respectively, at trough levels.
Clinical Trial
Molecular Weight

477.88

Formula

C₂₂H₁₇ClFN₉O

CAS No.

1640247-87-5

SMILES

NC1=NC(N)=NC(N[[email protected]](C2CC2)C(N3C4=CN=CC=C4)=NC5=C(F)C=CC(Cl)=C5C3=O)=C1C#N

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Room temperature in continental US; may vary elsewhere

Storage

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

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