产品
编 号：F132872
分子式：C25H26N6O2
分子量：442.51
分子式：C25H26N6O2
分子量：442.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1353644-70-8
产品详情
生物活性：
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of75% at the end of study, and with a dose response.Animal Model:NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)
Dosage:2 mg/kg, 5 mg/kg, 15 mg/kg
Administration:Oral administration;daily; for 21 days
Result:Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.
体外研究：
Theliatinib 显着抑制 A431 细胞中的 EGFR 磷酸化，IC50 为 7 nM。Theliatinib 还抑制 A431、H292 和 FaDu 细胞存活，IC50 值分别为 80 nM、58 nM 和 354 nM。
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of75% at the end of study, and with a dose response.Animal Model:NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)
Dosage:2 mg/kg, 5 mg/kg, 15 mg/kg
Administration:Oral administration;daily; for 21 days
Result:Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.
体外研究：
Theliatinib 显着抑制 A431 细胞中的 EGFR 磷酸化，IC50 为 7 nM。Theliatinib 还抑制 A431、H292 和 FaDu 细胞存活，IC50 值分别为 80 nM、58 nM 和 354 nM。
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