TAK-448

TAK-448 (MVT-602) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

IC50: 460 pM (KISS1R)[1] EC50: 632 pM (KISS1R)[1]

TAK-448 (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 mg/kg, 0.03 mg/kg, 0.3 mg/kg, 3 mg/kg Administration: Given i.h.; dosings on day 0 and 28 Result: Had greater anti-tumor effects in VCaP xenograft model.

[1]. 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.

[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.