推荐产品
product name
mTOR抑制剂XI，Torin1, mTOR Inhibitor XI, Torin1, CAS 1222998-36-8, is a cell-permeable, highly potent, ATP-competitive inhibitor of mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively).
品質等級
化驗
≥99% (HPLC)
形狀
powder
效力
2 nM IC50
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
yellow-white
溶解度
DMSO: 2 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
InChI
1S/C35H28F3N5O2/c1-2-32(44)42-15-13-41(14-16-42)31-11-9-26(19-28(31)35(36,37)38)43-33(45)12-8-24-20-40-30-10-7-22(18-27(30)34(24)43)25-17-23-5-3-4-6-29(23)39-21-25/h3-12,17-21H,2,13-16H2,1H3
InChI 密鑰
AKCRNFFTGXBONI-UHFFFAOYSA-N
一般說明
一种可渗透细胞的吡啶酮喹啉衍生物，可作为mTOR和DNA-PK的高效，ATP竞争性抑制剂（IC50分别为4.32和6.34 nM），同时仅在更高的浓度下抑制PI 3-K（IC50=171至533 nM）。有效抑制体外MEF中mTORC1介导的S6K1磷酸化（IC50=2 nM），以及体内鼠肺和肝中mTORC2介导的Akt 和mTORC1依赖性S6磷酸化（单次腹腔内注射剂量20 mg/kg后长达6小时）。尽管其体内稳定性差（小鼠中T1/2 =4.52 h；10 mg/kg i.p.），但据报告，Torin1通过每日200 mg/kg的高剂量i.p.给药可完全抑制U87MG衍生的小鼠肿瘤扩张。还报告了可有效抑制已知对雷帕霉素具有抗性的细胞mTORC1功能（目录号 553210、553211和553212）。
一种可渗透细胞的吡啶酮喹啉衍生物，可作为针对mTOR和DNA-PK的高效，ATP竞争性抑制剂（在无细胞激酶测定中，IC50分别为4.32和6.34 nM），仅在更高的浓度下抑制I类（P110γ，P110α/P85α，和P110δ/P85α的IC50分别为171，250和564 nM），II类（C2α和C2β的IC50分别为176和564 nM）和III类（hVPS34的IC50=533 nM）PI 3-K。有效抑制体外MEF培养物中mTORC1介导的S6K1 Thr389磷酸化（IC50=2 nM），以及体内鼠肺和肝中mTORC2介导的Akt Ser473和mTORC1依赖性S6 Ser235/236磷酸化（单次腹腔内注射剂量为20 mg/kg后长达6小时）。尽管其体内稳定性差（小鼠中T1/2 =4.52 h；10 mg/kg i.p.），但据报告，Torin1通过每日200 mg/kg的高剂量i.p.给药可完全抑制U87MG衍生的小鼠肿瘤扩张。还报告了可有效抑制已知对雷帕霉素具有抗性的细胞mTORC1功能（目录号 553210、553211和553212）。
生化／生理作用
主要靶标
MTOR
MTOR
可逆性：是
细胞可渗透性：具有
包裝
用惰性气体包装
警告
毒性：标准处理（A）
重構
复溶后，等分并冷冻保存（-20&C）。贮备液在-20°C下可稳定保存至多3个月。
其他說明
Liu, Q., et al. 2010.J Med Chem.53, 7146.
Thoreen, C., et al. 2009.J Biol Chem.284, 8023.
Thoreen, C., et al. 2009.J Biol Chem.284, 8023.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 2
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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