Product Data?SheetSapanisertibCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-133281224844-38-5C??H??N?O309.33mTOR; AutophagyPI3K/Akt/mTOR; AutophagyPowderIn solvent-20°C4°C-80°C-20°C3 years2 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 83.3 mg/mL (269.29 mM)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM3.2328 mL0.6466 mL0.3233 mL16.1640 mL3.2328 mL1.6164 mL32.3279 mL6.4656 mL3.2328 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；?旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (8.08 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-CD in saline)Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solutionPage 1 of 2 www.MedChemExpress.cn
此?案可获得 ≥ 2.5 mg/mL (8.08 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合均匀。BIOLOGICAL ACTIVITY?物活性Sapanisertib (INK-128; MLN0128; TAK-228) 是?种?服有效的 ATP依赖性的 mTOR1/2 抑制剂，抑制 mTOR 激酶的IC50 值为 1 nM。IC?? & TargetmTOR1 nM (IC50)PI3Kγ221 nM (IC50)mTORC1?PI3Kδ230 nM (IC50)mTORC2?PI3Kβ5.293 μM (IC50)PI3Kα219 nM (IC50)Autophagy?体外研究Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1]. Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) 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].体内研究In a ZR-75-1 breast cancer xenograft model, Sapanisertib (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. Sapanisertib (INK-128) 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].PROTOCOLCell Assay [2]PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of Sapanisertib (INK-128) necessary to achieve inhibition of cell growth by 50% (IC50) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve).MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration [2]Nude mice are inoculated subcutaneously in the right subscapular region with 5×106?MDA-MB-361 cells. After tumours reach a size of 150-200 mm3, mice are randomLy assigned into vehicle control or treatment groups. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, 80% water and administered by oral gavage at 0.3 mg/kg?and 1 mg/kg?daily.MCE has not independently confirmed the accuracy of these methods. They are for reference only.客户使?本产品发表的科研?献????Nature. 2016 Dec 1;540(7631):119-123.????Cell Stem Cell. 2024 Mar 1;22(3):369-383.e8.????Sci Transl Med. 2024 Jul 18;10(450). pii: eaaq1093.Page 2 of 3 www.MedChemExpress.cn
????Nat Commun. 2017 Jun 8;8:15617.????Dev Cell.?2024 Jan 27;52(2):236-250.e7.?
See more customer validations on www.MedChemExpress.cnREFERENCES
[1].?Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.
[2].?Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61.
McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
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