Torin 1
Synonym(s):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;mTOR Inhibitor XI, Torin1 - Calbiochem
- CAS NO.:1222998-36-8
- Empirical Formula: C35H28F3N5O2
- Molecular Weight: 607.62
- MDL number: MFCD18782653
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is Torin 1?
Description
Torin1 (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 properties
White Solid
The Uses of Torin 1
Torin 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.
What are the applications of Application
Torin 1 is a selective potent mTOR inhibitor, with over 100-fold selectivity for mTOR over kinases like PI3Kα, ATM, DNA-PK, hVps34, and 450 other proteins.
Definition
ChEBI: 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 Description
A 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 Actions
Cell permeable: yes
storage
Store at +4°C
References
References/Citations:
Properties of Torin 1
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 |
pka | 4.19±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 for Torin 1
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H320:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Torin 1
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