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475991 mTOR Inhibitor XI, Torin1 - Calbiochem

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).

mTOR Inhibitor XI, Torin1 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

同义词: 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII

475991
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概述

Replacement Information

Products

产品目录编号包装 数量 / 包装
475991-10MGCN 玻璃瓶 10 mg
Description
OverviewA cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively), while inhibiting PI 3-K only at much higher concentrations (IC50 =171 to 533 nM). Effectively inhibits mTORC1-mediated S6K1 phosphorylation in MEF (IC50 = 2 nM) in vitro, as well as mTORC2-mediated Akt and mTORC1-dependent S6 phosphorylations in murine lung and liver in vivo (up to 6 h post single 20 mg/kg i.p. dose). Despite its poor in vivo stability (T1/2 = 4.52 h in mice; 10 mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200 mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant (Cat. Nos. 553210, 553211, and 553212).
Catalogue Number475991
Brand Family Calbiochem®
Synonyms1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII
References
ReferencesLiu, Q., et al. 2010. J Med Chem. 53, 7146.
Thoreen, C., et al. 2009. J Biol Chem. 284, 8023.
Product Information
CAS number1222998-36-8
FormYellowish-white powder
Hill FormulaC₃₅H₂₈F₃N₅O₂
Chemical formulaC₃₅H₂₈F₃N₅O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationmTOR 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).
Biological Information
Primary TargetMTOR
Primary Target IC<sub>50</sub>2 nM
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
产品目录编号 GTIN
475991-10MGCN 04055977184433

Documentation

mTOR Inhibitor XI, Torin1 - Calbiochem MSDS

职位

物料安全数据表 (MSDS) 

mTOR Inhibitor XI, Torin1 - Calbiochem 分析证书

标题批号
475991

参考

参考信息概述
Liu, Q., et al. 2010. J Med Chem. 53, 7146.
Thoreen, C., et al. 2009. J Biol Chem. 284, 8023.
数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision04-July-2013 JSW
Synonyms1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII
DescriptionA cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34 nM, respectively, in cell-free kinase assays), inhibiting class I (IC50 =171, 250, and 564 nM, respectively, against P110γ, P110α/P85α, and P110δ/P85α, respectively), class II (IC50 =176 and 564 nM, respectively, against C2α, and C2β, respectively), and class III (IC50 = 533 nM against hVPS34) PI 3-K only at much higher concentrations. Effectively inhibits mTORC1-mediated S6K1 Thr389 phosphorylation in MEF cultures (IC50 = 2 nM) in vitro, as well as mTORC2-mediated Akt Ser473 and mTORC1-dependent S6 Ser235/236 phosphorylations in murine lung and liver in vivo (up to 6 h after single i.p. dose at 20 mg/kg). Despite its poor in vivo stability (T1/2 = 4.52 h in mice; 10 mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200 mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant (Cat. Nos. 553210, 553211, and 553212).
FormYellowish-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1222998-36-8
Chemical formulaC₃₅H₂₈F₃N₅O₂
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (2 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesLiu, Q., et al. 2010. J Med Chem. 53, 7146.
Thoreen, C., et al. 2009. J Biol Chem. 284, 8023.