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TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM[1]. | [in vivo]
TAK-448 acetate (0.01-3 mg/kg; given i.h.; dosings on day 0 and 28) has greater anti-tumor effects in VCaP xenograft model[2]. | Animal Model: | Rat VCaP xenograft androgen-sensitive prostate cancer model (7-week-old rats) | | Dosage: | 0.01, 0.03, 0.3, 3 mg/kg | | Administration: | Given i.h.; dosings on day 0 and 28 | | Result: | Had greater anti-tumor effects in VCaP xenograft model. |
| [References]
[1] Nishizawa N, et al. Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly PotentTestosterone-Suppressive Activity and Excellent Water Solubility. J Med Chem. 2016 Oct 13;59(19):8804-8811. DOI:10.1021/acs.jmedchem.6b00379
[2] Ishikawa K,et al. Usefulness of pharmacokinetic/efficacy analysis of an investigational kisspeptin analog, TAK-448, in quantitatively evaluating anti-tumor growth effect in the rat VCaP androgen-sensitiveprostate cancer model. Eur J Pharmacol. 2018 Jun 5;828:126-134. DOI:10.1016/j.ejphar.2018.03.032 |
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