1234319-68-6

1234319-68-6 structure

Name: TAK-448
Chemical Name: YO029HR229
CAS Number: 1234319-68-6
Molecular Formula: C₅₈H₈₀N₁₆O₁₄
Molecular Weight: 1225.36
Catalog: Research Areas Cancer
Create Date: 2018-07-13 20:01:21
Modify Date: 2024-01-09 19:05:26
TAK-448 (MVT-602) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM[1].

Name	YO029HR229
Synonyms	YO029HR229

Description	TAK-448 (MVT-602) 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 (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.
References	[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.