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TAK-448 acetate

Names

[ CAS No. ]:
1470374-22-1

[ Name ]:
TAK-448 acetate

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

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

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C60H84N16O16

[ Molecular Weight ]:
1285.41

[ Storage condition ]:
2-8℃

Related Compounds