Targefrin 是一种有效的靶向EphA2的试剂，作为拮抗剂发挥作用。Targefrin 结合 EphA2- LBD 的解离常数为 21 nM，IC50值为10.8 nM。Targefrin 在几种胰腺癌细胞系中诱导细胞受体内化和降解。
| 生物活性 | Targefrin is a potentEphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and anIC50value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreaticcancercell lines[1]. |
体外研究
(In Vitro) | Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells[1].
Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration[1].
Western Blot Analysis[1] | Cell Line: | BxPC3 cells (starved for 1 h and pre-treated with Targefrin for 20 min, followed by a combination treatment with 2 μg/mL ephrinA1-Fc for 3 h) | | Concentration: | 0.025, 0.25, 0.5, 1, 2.5, 5, 7.5 and 10 μM | | Incubation Time: | 20 min | | Result: | Effectively antagonized EphA2 degradation induced by the potent ephrinA1-Fc ligand, with an approximate EC50of ~1.6 μM. |
Cell Migration Assay[1] | Cell Line: | BxPC3 cells | | Concentration: | 2, 4, 5 and 10 μM | | Incubation Time: | 24 h | | Result: | Significantly inhibited pancreatic cancer cell migration. |
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体内研究
(In Vivo) | Targefrin (50 mg/kg; i.v.; for 5 days) suppresses tumor growth when conjugated withPaclitaxel[1].
| Animal Model: | Male nu/nu mice (injected with MIA PaCa-2 cells)[1] | | Dosage: | 50 mg/kg | | Administration: | i.v.; at day 1, 4, 8, 11 and 15 | | Result: | Both Targefrin-Paclitaxeland Targefrin-dimer-Paclitaxeldisplayed a significant antitumor effect compared to both the untreated group and thePaclitaxel-treated group. |
| Animal Model: | Balb/C mice[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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