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

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

Safety Statements 

24/25

HS Code 

29334900

Torin 1 Usage And Synthesis

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

Uses

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.

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 (T_1/2 = 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:

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