Torin2 Inhibitor CAS No. 1223001-51-1

Cat. No.	Name	Size	Price
KI0617	Torin2	5 mg	$176
	Torin2	10 mg	$220
	Torin2	25 mg	$440
	Torin2	50 mg	$704

Chemical Characteristic

Product Name	Torin2
CAS No.	1223001-51-1
Molecular Weight	432
Formula	C₂₄H₁₅F₃N₄O
Chemical Name	9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one
Smiles	n1(c(=O)ccc2cnc3c(c12)cc(cc3)c1cnc(cc1)N)c1cc(ccc1)C(F)(F)F
Chemical Structure
Documents	HPLC MS COA

Biological activities

Torin 2 is a potent, selective and orally available mTOR inhibitor. The IC50 of torin 2 is 2.1, 0.25 and 200 nM against mTORC1, mTOR and PI3K, respectively. Torin 2 inhibits PI4Kβ, PI3K-C2α and PI3K-C2β with IC50 of 18.3, 28.1 and 24.5 nM, respectively. The IC50 of torin2 is 8.58 nM against hVPS34. Torin 2 suppresses p110α/p85α, p110β/p85α, p110γ with IC50 of 4.68, 17.5 and 5.67 nM, respectively. Torin2 inhibits DNA-PK with an IC50 of 0.5 nM.^[1] Torin 2 induces TFEB nuclear translocation more efficiently.^[2] Torin 2 inhibits mTORC1-dependent T389 phosphorylation on S6K (RPS6KB1) with an EC50 of 250 pM with approximately 800-fold selectivity for cellular mTOR versus PI3K. Torin 2 also exhibits potent biochemical and cellular activity against PIKK family kinases including ATM and ATR with IC50 of 28 and 35 nM, respectively. Torin 2 for 24 hours results in a prolonged block in negative feedback and consequent T308 phosphorylation on Akt.^[3] Torin2 has significantly improved bioavailability (54%), metabolic stability and plasma exposure.^[1]

Protocols

Torin2 is first dissolved at 25 mg/mL in 100% N-methyl-2-pyrrolidone and then diluted 1:4 with sterile 50% PEG400 prior to injection.^[1]

References

[1] Liu Q, et al. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J Med Chem. 2011, 54(5): 1473-1480. [2] Settembre C, et al. A lysosome-to-nucleus signalling mechanism senses and regulates the lysosome via mTOR and TFEB. EMBO J. 2012, 31(5): 1095-1108. [3] Liu Q, et al. Characterization of Torin2, an ATP-Competitive Inhibitor of mTOR, ATM, and ATR. Cancer Res. 2013, 73(8): 2574-2586.

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