Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC 50 s of 3 nM for both JAK2 and JAK2V617F kinase . Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3 , respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research In Vitro Fedratinib (TG101348) inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC 50 value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC 50 value of ～420 nM. ? Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. ? Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57Bl/6 mice induced by the JAK2V617F mutation Dosage: 60 mg/kg, 120 mg/kg Administration: Oral gavage; twice daily; for 42 days Result: Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis. Form:Solid IC50& Target:JAK2 3 nM (IC 50 ) JAK2(V617F) 3 nM (IC 50 ) Flt3 15 nM (IC 50 ) Ret 48 nM (IC 50 )
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Fedratinib hydrochloride hydrate
CAS number：1374744-69-0 molecular formula：C27H40Cl2N6O4S
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| Chinese alias | 盐酸菲德拉替尼水合物 | ||
| English alias | Fedratinib (hydrochloride hydrate) | TG101348(2ClH.H2O) | AKOS040759750 | FEDRATINIB HYDROCHLORIDE MONOHYDRATE [MI] | N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide hydrochloride hyd | ||
| CAS number | 1374744-69-0 | molecular formula | C27H40Cl2N6O4S |
| molecular weight | 615.6 g/mol | Exact mass | - |
| PSA | 118.000 Ų | logp | - |
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