| Chemical Properties | Back Directory | [Boiling point ]
862.7±75.0 °C(Predicted) | [density ]
1.71±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
3.94±0.12(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1]. | [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.
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| [IC 50]
PI3Kδ: 1 nM (IC50) | [References]
[1] Patel L, et al. Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability. J Med Chem. 2016 Oct 13;59(19):9228-9242. DOI:10.1021/acs.jmedchem.6b01169 |
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| Company Name: |
Enzo Biochem Inc
|
| Tel: |
Enzo Biochem Inc. 13797054060 |
| Website: |
www.enzo.com |
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