GS-9901

Research use only, not for human use.

GS-9901 is a selective, orally active and potent PI3Kδ inhibitor (IC50: 1 nM) for the study of non-Hodgkin's lymphoma and chronic lymphocytic leukemia.

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

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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.Animal Model:Female Lewis rats with established collagen-induced arthritis (CIA).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.

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PI3K/Akt/mTOR signaling

PI3K

PI3K

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1640247-87-5

477.88

C22H17ClFN9O

>98% (HPLC)

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[C@@H](NC=1C(C#N)=C(N)N=C(N)N1)(C=2N(C(=O)C=3C(N2)=C(F)C=CC3Cl)C=4C=CC=NC4)C5CC5

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(-20℃)

With Ice Pack

≥ 2 years