Torin 1

Torin-1 is a potent and selective mTOR inhibitor. The apoptosis-inducing mTOR inhibitor Torin-1 hindered growth, motility, invasion, and survival of CoCSCs in vitro, and suppressed tumor growth in vivo with a concomitant reduction in vessel formation. Torin-1 also affected the expression of markers for cell proliferation, angio-/lympho-genesis, and stemness in vivo, including Ki67, DLL1, DLL4, Notch, Lgr5, and CD44. Importantly, Torin-1 did not affect the survival of normal colon stem cells in vivo, suggesting its selectivity towards cancer cells.

Product information

CAS Number: 1222998-36-8

Molecular Weight: 607.62

Formula: C35H28F3N5O2

Synonym:

Torin 1

Torin-1

Torin1

Chemical Name:  1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one

Smiles: CCC(=O)N1CCN(CC1)C1=CC=C(C=C1C(F)(F)F)N1C2=C(C=CC1=O)C=NC1=CC=C(C=C12)C1=CC2=CC=CC=C2N=C1

InChiKey: AKCRNFFTGXBONI-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Torin1 (250 nM) completely inhibits proliferation and causes a G1/S cell cycle arrest, and decreases cell size to a greater degree than 50 nM rapamycin in wild-type MEFs. Torin1 has more than 800-fold selectivity between mTOR and PI3Kis, and is very selective relative to other PIKK family kinases with the exception of DNA-PK.

In Vivo:

Torin1 (20 mg/kg, i.p.) is efficacious in a U87MG xenograft model, and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues.

References:

1. Francipane MG, Lagasse E. Selective targeting of human colon cancer stem-like cells by the mTOR inhibitor Torin-1. Oncotarget. 2013 Nov;4(11):1948-62. PubMed PMID: 24185040; PubMed Central PMCID: PMC3875761.
2. Vogel KR, Ainslie GR, Jansen EE, Salomons GS, Gibson KM. Torin 1 partially corrects vigabatrin-induced mitochondrial increase in mouse. Ann Clin Transl Neurol. 2015 Jun;2(6):699-706. doi: 10.1002/acn3.200. Epub 2015 Apr 17. PubMed PMID: 26125044; PubMed Central PMCID: PMC4479529.
3. Cheng NT, Guo A, Meng H. The protective role of autophagy in experimental osteoarthritis, and the therapeutic effects of Torin 1 on osteoarthritis by activating autophagy. BMC Musculoskelet Disord. 2016 Apr 6;17(1):150. doi: 10.1186/s12891-016-0995-x. PubMed PMID: 27052304; PubMed Central PMCID: PMC4823842.

Products are for research use only. Not for human use.