INK-128 | CAS:1224844-38-5

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Name:INK-128; Sapanisertib; MLN0128
Cat. No. :CS-0557
CAS No. :1224844-38-5
Formula:C15H15N7O
M. Wt. : 309.33
Solubility:10 mM in DMSO

INK-128 is a potent and selective mTOR inhibitor with IC50 of 1 nM, > 200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes.IC50 & Target: IC50: 1 nM (mTOR), 219 nM (PI3Kα), 5293 nM (PI3Kβ), 230 nM (PI3Kδ), 221 nM (PI3Kγ)[2]Ki: 1.4 nM (mTOR), 152 nM (PI3Kα), 4700 nM (PI3Kβ), 165 nM (PI3Kγ)[2]In Vitro: INK-128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1]. INK128 selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. INK128 decreases the invasive potential of PC3 prostate cancer cells. Furthermore, INK128 inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis[2]. In Vivo: In a ZR-75-1 breast cancer xenograft model, INK-128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day[1]. 4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. INK128 treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice[2].

Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61. Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.