Description
Cas:1222998-36-8
Product Information:
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.
Chemical Formula: C35H28F3N5O2
Exact Mass: 607.2195
Molecular Weight: 607.6372
Elemental Analysis: C, 69.18; H, 4.64; F, 9.38; N, 11.53; O, 5.27
Synonym:
Torin-1
Torin1
Torin 1
Chemical Name: 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one
InChi Key:
AKCRNFFTGXBONI-UHFFFAOYSA-N
InChi Code: 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
Smiles Code:
O=C1N(C2=CC=C(N3CCN(C(CC)=O)CC3)C(C(F)(F)F)=C2)C4=C(C=NC5=CC=C(C6=CC7=CC=CC=C7N=C6)C=C54)C=C1
Technical Data:
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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:
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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.
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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.
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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.
Products are for research use only. Not for human use.
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