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Torin 2

Torin 2

Item no.	S2817-10000
Manufacturer	Selleckchem
CASRN	1223001-51-1
Amount	10 g
Category	Oncology Neuroscience Aging & Neurological Disorders Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Testicular & Prostate Cancer
Type	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1223001-51-1'
Similar products	Torin
Available
Administration	Intravenous or oral
Animal Models	male Swiss albino mice
Cell lines	MZ-CRC-1 and TT cells
Chemical Name	Benzo[h]-1, 6-naphthyridin-2(1H)-one, 9-(6-amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]-
Concentrations	50 nM
Description	Torin2 is a highly potent and selective mTOR inhibitor with IC50 of 0.25 nM.
Dosages	25 mg/kg
Formulation	first dissolve at 25 mg/mL in 100% N-methyl-2-pyrrolidone and then dilute 1:4 with sterile 50% PEG400 prior to injection
IC50	0.25 nM [1], 0.25 nM [1], 0.25 nM [1], 0.25 nM [1], 0.25 nM [1], 0.25 nM [1]
In vitro	Torin2 has the same binding mode as PI3Kgamma, V882 serves as a hinge binding point and in the inner hydrophobic pocket Y867, D841 and D964 provide three more hydrogen bonds with aminopyridine side chain analogous to Y2225, D2195 and D2357 of mTOR. [1] Torin2 inhibits mTORC1, thus activates TFEB by promoting its nuclear translocation with EC50 of 1.666 mM. [2] Torin 2(< 50 nM) causes a significant reduction in viability of both MZ-CRC-1 and TT cells. Torin 2 (100 nM) exerts a significant reduction of migration of both MZ-CRC-1 and TT cells. [3]
In vivo	Torin2 exhibits >95% pharmacodynamic response and half-time of 11.7 min in the mouse liver microsome stability study. Torin2 exhibits the best bioavailability (51%), short half-life (0.72 hours) and low clearance(19.6 mL/min/kg) in male Swiss albino mice following intravenous and oral administration. [1] Torin2(20mg/kg) ablates MYCN tumors with reduction in MYCN protein levels and induction of apoptosis in Th-MYCN mice. [4]
Incubation Time	3 days or 5 days
Kinase Assay	mTOR and PI3K Cellular Assays, Cellular IC50 values for mTOR are determined using p53 / MEFs. Cells are treated with vehicle or increasing concentrations of Torin2 for 1 h and then lyse. Phosphorylation of S6K1 Thr-389 is monitored by immunoblotting using a phospho-specific antibody. Meanwhile, cellular IC50 values for PI3Ka are determined based on phosphorylation of Akt Thr-308 in p53 / /mLST8 / MEFs or human PC3 cells expressing the S473D mutant of Akt1.
Method	For viability, MZ-CRC-1 and TT cells are seeded in quadruplicate in 96-well plates (1.0x104 cells per well) in culture media with 2.5% and 4% FBS, respectively. After 24 hours, cells are treated with Torin 2. At the indicated time point, cells are incubated for 3 hours with 10 uL of CellTiter96 AQueous One solution in 100 uL of culture media and absorbance is measured at 490 nm.
Molecular Weight (MW)	432, 4
Picture ChemicalStructure Description	Torin 2 Chemical Structure
Solubility (25C)	DMSO <1 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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