Torin 1

Torin 1 Basic information
Product Name:Torin 1
Synonyms:TORIN-1;TORIN 1;CS-1958;mTOR Inhibitor XI, Torin1 - Calbiochem;1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one;1-[4-(4-PROPANOYLPIPERAZIN-1-YL)-3-(TRIFLUOROMETHYL)PHENYL]-9-QUINOLIN-3-YLBENZO[H][1,6]NAPHTHYRIDIN-2-ONE;Torin 1;Benzo[h]-1,6-naphthyridin-2(1H)-one, 1-[4-[4-(1-oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)-;1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)benzo[h]-1,6-naphthyridin-2(1H)-one Torin 1
CAS:1222998-36-8
MF:C35H28F3N5O2
MW:607.62
EINECS:
Product Categories:Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals;PI3K/Akt/mTOR;Inhibitors;Akt;mTOR;PI3K
Mol File:1222998-36-8.mol
Torin 1 Structure
Torin 1 Chemical Properties
Melting point >223°C (dec.)
Boiling point 817.2±65.0 °C(Predicted)
density 1.362
storage temp. +2C to +8C
solubility Soluble in DMSO (up to 8 mg/ml).
form Yellowish-white powder
pka4.19±0.20(Predicted)
color White or off-white
Stability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Safety Information
Safety Statements 24/25
HS Code 29334900
MSDS Information
Torin 1 Usage And Synthesis
DescriptionTorin1 (1222998-36-8) is a potent and selective ATP-competitive mTOR inhibitor, IC50=2 and 10 nM for mTORC1 and mTORC2 respectively.1,2 Active in vivo at inhibition of mTOR-mediated effects in mice (20 mg/kg).2 Induces autophagy.3 Torin 1-mediated enhancement of TFEB-mediated autophagy alleviates neuronal death in oxidative stress-induced disease models.4 Downregulates NGF expression in RSC96 cells.5
Chemical PropertiesWhite Solid
UsesTorin 1 is a potent and selective mTOR inhibitor (IC50 = 2 - 10 nM for mTORC1 and mTORC2). Displays 200-fold selectivity for mTOR over DNA-PK, ATM and hVps34.
DefinitionChEBI: Torin 1 is a member of the class of pyridoquinolines that is 9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2-one bearing an additional 4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl substituent at position 1. It is a potent inhibitor of mTOR and exhibits anti-cancer properties. It has a role as a mTOR inhibitor and an antineoplastic agent. It is a N-acylpiperazine, a N-arylpiperazine, an organofluorine compound, a pyridoquinoline and a member of quinolines.
General 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).
Biochem/physiol ActionsCell permeable: yes
storageStore at +4°C
ReferencesReferences/Citations:
Torin 1 Preparation Products And Raw materials
Rapamycin AC480 (BMS-599626) Brivanib alaninate CUDC-101 RO4929097 Acalabrutinib Avagacestat (BMS-708163) Telaprevir Pictilisib KU-0063794 Torin 2 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid Tariquidar CCT 137690 3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol PP242 Everolimus

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