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2225868-19-7

2225868-19-7 Structure

2225868-19-7 Structure
IdentificationBack Directory
[Name]

123B9
[CAS]

2225868-19-7
[Synonyms]

123B9
[Molecular Formula]

C58H82ClFN12O20
[MOL File]

2225868-19-7.mol
[Molecular Weight]

1321.79
Chemical PropertiesBack Directory
[Boiling point ]

1748.4±65.0 °C(predicted)
[density ]

1.401±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
[form ]

Solid
[pka]

4.20±0.10(predicted)
[color ]

White to off-white
[Sequence]

{2-(3-chloro-4-fluorophenoxy)acetic acid}-Ser-Ala-Tyr-Pro-Asp-Ser-Val-Pro-{Nle}-{Hsr}-Ser-NH2
Hazard InformationBack Directory
[Uses]

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].
[in vivo]

In mice, the mean plasma concentration over time following 123B9 IV administration (30 mg/kg) indicated that the compound is detectable in vivo at each time point tested (30 min, 1 hr, 2 hr, 4 hr) with a mean concentration in plasma of 447 ng/mL and 569 ng/mL still detectable at 2 hr and 4 hr, respectively[1].

[References]

[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. DOI:10.1016/j.chembiol.2015.06.011
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