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GS-9973 is an imidazopyrazine inhibitor of Syk that is currently in clinical trials as a potential treatment for chronic lymphocytic leukemia (CLL). GS-9973 exhibits anticancer chemotherapeutic activity. In vitro, this compound decreases survival of CLL cells, inhibits cell growth, and disrupts chemokine signaling.
| Cas No. | 1229208-44-9 |
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| Purity | ≥98% |
| Formula | C23H21N7O |
| Formula Wt. | 411.46 |
| IUPAC Name | 6-(1H-Indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo[1,2-a]pyrazin-8-amine |
| Synonym | GS9973, Entospletinib |
| Solubility | DMSO 26 mg/mL warmed (63.18 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Yellow to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet |
Sharman J, Hawkins M, Kolibaba K, et al. An open-label phase 2 trial of entospletinib (GS-9973), a selective Syk inhibitor, in chronic lymphocytic leukemia. Blood. 2015 Feb 18. Epub ahead of print]. PMID: 25696919.
Currie KS, Kropf JE, Lee T, et al. Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. J Med Chem. 2014 May 8;57(9):3856-73. PMID: 24779514.
Burke RT, Meadows S, Loriaux MM, et al. A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor. Oncotarget. 2014 Feb 28;5(4):908-15. PMID: 24659719.