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Chemical Structure : Entospletinib
CAS No.: 1229208-44-9
Catalog No.: PC-73180Not For Human Use, Lab Use Only.
Entospletinib (GS-9973) is a potent, selective and orally bioavailable Syk kinase inhibitor with IC50 of 7.7 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $238 | In stock | |
| 100 mg | Get quote |
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Entospletinib (GS-9973) is a potent, selective and orally bioavailable Syk kinase inhibitor with IC50 of 7.7 nM.
Entospletinib (GS-9973) also shows excellent selectivity for Syk, and potently inhibits BCR-mediated activation and proliferation of B-cells as well as immune-complex-stimulated cytokine production in monocytes.
Entospletinib (GS-9973) combined with Idelalisib synergistically inhibits CLL cell viability and further disrupts chemokine signaling.
Entospletinib (GS-9973) (1-10 mg/kg, p.o.) significantly inhibits ankle inflammation in a rat collagen-induced arthritis model, inhibits pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 of 1.2-3.9 mg/kg.
| M.Wt | 411.46 | |
| Formula | C23H21N7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
6-(1H-indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine |
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1. Currie KS, et al. J Med Chem. 2014 May 8;57(9):3856-73.
2. Burke RT, et al. Oncotarget. 2014 Feb 28;5(4):908-15.
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