产品
编 号：F763017
分子式：C85H116F3N19O15
分子量：1700.94
分子式：C85H116F3N19O15
分子量：1700.94
产品类型
规格
价格
是否有货
500μg
询价
询价
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 3031514-44-7
产品详情
生物活性：
Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines.
体内研究：
Targefrin (50 mg/kg; i.v.; for 5 days) suppresses tumor growth when conjugated with Paclitaxel.Animal Model:Male nu/nu mice (injected with MIA PaCa-2 cells)
Dosage:50 mg/kg
Administration:i.v.; at day 1, 4, 8, 11 and 15
Result:Both Targefrin-Paclitaxel and Targefrin-dimer-Paclitaxel displayed a significant antitumor effect compared to both the untreated group and the Paclitaxel-treated group.
Animal Model:Balb/C mice
Dosage:50 mg/kg
Administration:IV via tail vein; single dosage
Result:Cmax ~650 ng/mL after 2 hours from the injection; estimated t1/2 ~15 hr.
体外研究：
Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells.Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration.
Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines.
体内研究：
Targefrin (50 mg/kg; i.v.; for 5 days) suppresses tumor growth when conjugated with Paclitaxel.Animal Model:Male nu/nu mice (injected with MIA PaCa-2 cells)
Dosage:50 mg/kg
Administration:i.v.; at day 1, 4, 8, 11 and 15
Result:Both Targefrin-Paclitaxel and Targefrin-dimer-Paclitaxel displayed a significant antitumor effect compared to both the untreated group and the Paclitaxel-treated group.
Animal Model:Balb/C mice
Dosage:50 mg/kg
Administration:IV via tail vein; single dosage
Result:Cmax ~650 ng/mL after 2 hours from the injection; estimated t1/2 ~15 hr.
体外研究：
Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells.Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration.
产品资料
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