Bioactivity | 123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a Kd value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors[1]. |
Target | Kd: 4.0 μM (EphA2) |
In Vivo | 在小鼠中,静脉注射 123B9(30 mg/kg)后随时间推移的平均血浆浓度表明,该化合物在每个测试时间点(30 分钟、1 小时、2 小时、4 小时)在体内均可检测到,血浆中平均浓度分别为 447 ng/mL 和 569 ng/mL,在 2 小时和 4 小时仍可检测到[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 2225868-19-7 |
Sequence | {2-(3-chloro-4-fluorophenoxy)acetic acid}-Ser-Ala-Tyr-Pro-Asp-Ser-Val-Pro-{Nle}-{Hsr}-Ser-NH2 |
Shortening | {2-(3-chloro-4-fluorophenoxy)acetic acid}-SAYPDSVP-{Nle}-{Hsr}-S-NH2 |
Formula | C58H82ClFN12O20 |
Molar Mass | 1321.79 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Bainan Wu, et al. Design and Characterization of Novel EphA2 Agonists for Targeted Delivery of Chemotherapy to Cancer Cells. Chem Biol. 2015 Jul 23;22(7):876-887. |