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编 号：F142349
分子式：C27H40Cl2N6O4S
分子量：615.62
分子式：C27H40Cl2N6O4S
分子量：615.62
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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100mg
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200mg
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500mg
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1g
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CAS No: 1374744-69-0
产品详情
生物活性：
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s 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.
体内研究：
Fedratinib hydrochloride hydrate (TG101348；60-120 mg/kg；口服强饲法；每天两次；42 天；C57Bl/6 小鼠) 处理显示处理动物的红细胞增多症呈剂量依赖性减少，脾肿大明显减少。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.
体外研究：
Fedratinib hydrochloride hydrate (TG101348) 抑制携带 JAK2V617F 突变的人成红细胞白血病 (HEL) 细胞系以及表达人 JAK2V617F 的小鼠前 B 细胞系 (Ba/F3 JAK2V617F) 的增殖，IC50 每条线的值约为 300 nM。亲代 Ba/F3 细胞的增殖被抑制到相当水平，IC50 值为 ~420 nM。将这些细胞暴露于 Fedratinib hydrochloride hydrate (TG101348) (0.1 μM、0.3 μM、1 μM、3 μM 和 10 μM) 降低 STAT5 磷酸化的浓度与抑制细胞增殖所需的浓度相当。 Fedratinib hydrochloride hydrate (TG101348) (0.1 μM、0.3 μM、1 μM、3 μM 和 10 μM) 以剂量依赖性方式诱导 HEL 和 Ba/F3 JAK2V617F 细胞凋亡。
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s 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.
体内研究：
Fedratinib hydrochloride hydrate (TG101348；60-120 mg/kg；口服强饲法；每天两次；42 天；C57Bl/6 小鼠) 处理显示处理动物的红细胞增多症呈剂量依赖性减少，脾肿大明显减少。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.
体外研究：
Fedratinib hydrochloride hydrate (TG101348) 抑制携带 JAK2V617F 突变的人成红细胞白血病 (HEL) 细胞系以及表达人 JAK2V617F 的小鼠前 B 细胞系 (Ba/F3 JAK2V617F) 的增殖，IC50 每条线的值约为 300 nM。亲代 Ba/F3 细胞的增殖被抑制到相当水平，IC50 值为 ~420 nM。将这些细胞暴露于 Fedratinib hydrochloride hydrate (TG101348) (0.1 μM、0.3 μM、1 μM、3 μM 和 10 μM) 降低 STAT5 磷酸化的浓度与抑制细胞增殖所需的浓度相当。 Fedratinib hydrochloride hydrate (TG101348) (0.1 μM、0.3 μM、1 μM、3 μM 和 10 μM) 以剂量依赖性方式诱导 HEL 和 Ba/F3 JAK2V617F 细胞凋亡。
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