475991

Torin1

≥99% (HPLC), powder, mTOR inhibitor, Calbiochem^®

• Sinônimo(s): mTOR Inhibitor XI, Torin1, 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
• Fórmula empírica (Notação de Hill): C₃₅H₂₈F₃N₅O₂
• Número CAS: 1222998-36-8
• Peso molecular: 607.62
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• product name: mTOR Inhibitor 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).
• Nível de qualidade: 100
• Ensaio: ≥99% (HPLC)
• forma: powder
• potência: 2 nM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow-white
• solubilidade: DMSO: 2 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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
• chave InChI: AKCRNFFTGXBONI-UHFFFAOYSA-N

Descrição

Descrição geral

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), 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 (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).

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).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
MTOR

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20&degC). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Liu, Q., et al. 2010. J Med Chem.53, 7146.
Thoreen, C., et al. 2009. J Biol Chem.284, 8023.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable