| Identification | Back Directory | [Name]
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide hydrochloride hydrate (1:2:1) | [CAS]
1374744-69-0 | [Synonyms]
CL121
TG101348(2ClH.H2O)
Fedratinib hydrochloride hydrate
TG-101348 dihydrochloride hydrate
N-(tert-Butyl)-3-((5-methyl-2-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)amino)pyrimidin-4-yl)amino)benzenesulfonamide dihydrochloride hydrate
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide hydrochloride hydrate
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide hydrochloride hydrate (1:2:1) | [Molecular Formula]
C27H40Cl2N6O4S | [MDL Number]
MFCD28137677 | [MOL File]
1374744-69-0.mol | [Molecular Weight]
615.615 |
| Hazard Information | Back Directory | [Uses]
A potent, highly selective and ATP-competitive JAK2 inhibitor with an IC50 of 3 nM for JAK2 and JAK2V617F. | [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[1]. | Animal Model: | C57Bl/6 mice induced by the JAK2V617F mutation[1] | | 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.
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| [IC 50]
JAK2: 3 nM (IC50); JAK2(V617F): 3 nM (IC50); Flt3: 15 nM (IC50); Ret: 48 nM (IC50) |
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