1640247-87-5
1640247-87-5 structure
- Name: GS-9901
- Chemical Name: GS-9901
- CAS Number: 1640247-87-5
- Molecular Formula: C22H17ClFN9O
- Molecular Weight: 477.88
- Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
- Create Date: 2019-08-03 23:54:58
- Modify Date: 2024-01-11 10:19:51
-
GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1].
| Name | GS-9901 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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. |
| References |
| Molecular Formula | C22H17ClFN9O |
|---|---|
| Molecular Weight | 477.88 |