| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:GS-9901
CAS:1640247-87-5
Purity:99.80% Package:1removed
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| | GS-9901 Basic information |
| Product Name: | GS-9901 | | Synonyms: | GS-9901;GS 9901,GS9901;5-Pyrimidinecarbonitrile, 2,4-diamino-6-[[(S)-[5-chloro-8-fluoro-3,4-dihydro-4-oxo-3-(3-pyridinyl)-2-quinazolinyl]cyclopropylmethyl]amino]- | | CAS: | 1640247-87-5 | | MF: | C22H17ClFN9O | | MW: | 477.88 | | EINECS: | | | Product Categories: | | | Mol File: | 1640247-87-5.mol |  |
| | GS-9901 Chemical Properties |
| 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 |
| | GS-9901 Usage And Synthesis |
| 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 |
| | GS-9901 Preparation Products And Raw materials |
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