JR-AB2-011 - mTORC2-抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJR-AB2-011Cat. No.: HY-122022分式: CHClFNOS分量: 398.28作靶點(diǎn): mTOR作通路: PI3K/Akt/mTOR儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 62.5 mg/mL (156.92 mM; Need ultrasonic)H2O

2、 : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.22 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.22 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 JR-AB2-011種選擇性 mTORC2 抑制劑，IC50 值為 0.36 M。JR-AB2-011 通過(guò)阻斷 Rict

3、or-mTOR 聯(lián)合體 (Ki: 0.19 M) 抑制 mTORC2 活性。JR-AB2-011 具有抗多形性膠質(zhì)母細(xì)胞瘤 (GBM) 的活性 1。IC50 & Target mTORC20.36 M (IC50)體外研究 JR-AB2-011 (1 M; 24 hours) has good anti-GBM properties, blocks mTORC2 signaling and Rictor associationwith mTOR 1.JR-AB2-011 (0.5-2 M; 48 hours) displays the least toxicity to normal neur

4、ons with no significant cytotoxiceffects for concentrations up to 10 mM compared to CID613034 1.Apoptosis Analysis 1Cell Line: U87 GBM cells; LN229 GBM cellsConcentration: 1 MIncubation Time: 24 hoursResult: Had good anti-GBM properties and blocked mTORC2 signaling and Rictor association withmTOR.Ce

5、ll Cytotoxicity Assay 1Cell Line: Normal mature human neuronsConcentration: 0.5, 1, 2 MIncubation Time: 48 hoursResult: Displayed the least toxicity to normal neurons with no significant cytotoxic effects forconcentrations up to 10 mM.體內(nèi)研究 Mice receiving JR-AB2-011 (4 mg/kg; daily i.p. for 10 days;

6、20 mg/kg; daily i.p. for 10 days) at either dosingregimen display marked inhibition of tumor growth rate (JR-AB2-011 at 4 mg/kg/d; 74% inhibition at end ofdosing period; tumor growth delay 10.0 days; JR-AB2-011 at 20 mg/kg/d; 80% inhibition at end of dosingperiod; tumor growth delay 12.0 days) as co

7、mpared to mice receiving vehicle alone 1.Animal Model: LN229 cells in female C.B.-17-scid (Taconic) mice 1Dosage: 4 mg/kg; 20 mg/kgAdministration: Daily i.p.; 10 daysResult: Either dosing regimen displayed marked inhibition of tumor growth rate as compared tomice receiving vehicle alone.REFERENCES2/

8、3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Benavides-Serrato A, et al. Correction: Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxicinglioblastoma. PLoS One. 2019 Feb 6;14(2):e0212160.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo