mTOR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	mTOR	mTORC1	mTORC2	Other Targets
A10133	Dactolisib	***			p110α,p110γ,p110δ
A10782	Rapamycin	****
A10374	Everolimus	***
A10114	AZD8055	****			DNA-PK,PI3Kδ,PI3Kα
A10906	Temsirolimus	*
A10726	PI-103	*			p110α,p110δ,p110β
A10505	KU-0063794		**	**
A10746	Torkinib	**			p110δ,PDGFR,DNA-PK
A10295	Ridaforolimus	****
A11461	INK 128	****			PI3Kα,PI3Kγ,PI3Kδ
A10997	Voxtalisib Analogue	*			PI3Kγ,PI3Kα,PI3Kδ
A11587	Torin 1	***	***	**	DNA-PK,p110γ,C2α
A11035	Omipalisib		****	****	p110α,p110δ,p110γ
A11056	OSI-027	***	*	*	PI3Kγ,DNA-PK,PI3Kα
A11024	PF-04691502	**			PI3Kδ,PI3Kα,PI3Kγ
A11023	Apitolisib	*			p110α,p110δ,p110γ
A10438	GSK1059615	**			PI3Kα,PI3Kβ,PI3Kδ
A11079	Gedatolisib	****			PI3Kα,PI3Kγ
A10989	WYE-354	***			PI3Kα,PI3Kγ
A11303	Vistusertib	***			P-Akt (S473),pS6 (S235/236)
A11586	Torin 2	****			ATM,ATR,DNA-PK
A11038	WYE-125132	****
A11207	PP121	**			PDGFR,Hck,VEGFR
A11187	WYE-687	***			PI3Kα,PI3Kγ,p38α
A11169	CH5132799	*			PI3Kα,PI3Kγ,PI3Kβ
A11188	WAY-600	**			PI3Kα,PI3Kγ
A13328	ETP-46464	****			ATR,DNA-PK,PI3Kα
A11443	GDC-0349	***			PI3Kα
A12395	XL388	**	**	*	CYP2C9,CYP3A4
A13078	CC-223	**			cFMS,FLT4,DNA-PK
A16276	Voxtalisib	*			PI3Kγ,PI3Kα,PI3Kδ
A11950	Zotarolimus	***
A10389	Tacrolimus
A11162	BGT226				PI3Kα,PI3Kγ,PI3Kβ
A10693	Palomid 529
A10210	Chrysophanic Acid				EGFR
A11537	QL-IX-55
A12480	VS-5584	****			PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ
A12704	SF1126				PI3K
A12935	PF-04979064	****			PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ, Akt
A14432	GNE-493	***			PI3Kα, PI3Kδ, PI3Kγ, PI3Kβ
A15175	mTOR inhibitor (mTOR-IN-1)	***
A15508	MHY1485
A16126	LY3023414				PI3Kα, Akt1, DNA-PK

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No.	Product Name	Application	Product Information
A11035 SALE	GSK2126458 (Omipalisib)	mTOR/PI3K Inhibitor,	GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
A15175	mTOR inhibitor (mTOR-IN-1)	mTOR inhibitor	mTOR inhibitor is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 1.5 nM.
A11024 SALE	PF-04691502	PI3K/mTOR Inhibitor	PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.
A11023 SALE	GDC-0980 (Apitolisib, RG7422)	mTOR/PI3K Inhibitor	GDC-0980 (RG7422) is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms, respectively.
A15508 SALE	MHY1485	mTOR inhibitor	MHY1485 is a mTOR activator; inhibits the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes.
A12480 SALE	VS-5584	PI3K/mTOR inhibitor	VS-5584 is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
A11537	QL-IX-55	mTORC1/2 inhibitor	QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.
A16126	LY3023414	PI3K/mTOR Dual Inhibitor	LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242). Product Citations (1) Zou Y, .et al. Targeting PI3K-AKT-mTOR by LY3023414 inhibits human skin squamous cell carcinoma cell growth in vitro and in vivo, Biochem Biophys Res Commun, 2017, Aug 19;490(2):385-392 PMID: 28623128
A16276	SAR245409 (XL765, Voxtalisib)	PI3K/mTOR dual inhibitor	SAR245409 is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity.
A10133 SALE	BEZ235 (NVP-BEZ235, Dactolisib)	PI3K/mTOR Inhibitor	BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Product Citations (2) Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246 Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
A12935	PF-04979064	PI3K/mTOR Dual Inhibitor	PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor.
A13328	ETP-46464	ATR inhibitor	ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
A12395 SALE	XL388	mTOR inhibitor	XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR).
A11587 SALE	Torin 1	mTOR inhibitor	Torin1 is a potent inhibitor of mTOR with IC50 of 2-10 nM. Product Citations (2) Ashyad Rayhan, .et al. Using genetic buffering relationships identified in fission yeast to reveal susceptibilities in cells lacking hamartin or tuberin function, Biol Open, 2018, Jan 15; 7(1): bio031302 PMID: 29343513 Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
A11586	Torin 2	mTOR inhibitor	Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).
A11950 SALE	Zotarolimus	mTOR inhibitor	Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier.
A11443 SALE	GDC-0349	mTOR inhibitor	GDC-0349 is under evaluating the Safety and Tolerability in Patients with locally advanced or metastatic solid tumors or non hodgkin's lymphoma.
A14114	GNE 477	PI3K/mTOR inhibitor	GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
A14432	GNE-493	Dual Pan PI3k/mTOR inhibitor	GNE-493 is potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitor with potential anticancer activity.
A13519	AP1903	-	AP1903 is a lipid-permeable tacrolimus analogue with homodimerizing activity. Dimerizer drug AP1903 homodimerizes an analogue of human protein FKBP12 (Fv) which contains a single acid substitution (Phe36Val) so that AP1903 binds to wild-type FKBP12 with 1000-fold lower affinity.
A10900	Desmethyl-VS-5584	PI3K/mTOR inhibitor	Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
A15147	LY 303511	PI3K inhibitor	LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K.
A15779	CC-115	mTOR/DNA-PK inhibitor	CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
A13078	CC-223	mTOR Inhibitor	CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with >150-fold sensitivity over the related lipid kinase PI3K-alpha (IC50=4uM).
A11461 SALE	INK 128 (MLN0128)	mTOR inhibitor	INK 128 is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
A11303 SALE	AZD2014 (Vistusertib)	mTORC1/2 inhibitor	AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor. Product Citations (1) James T. Lynch, etc. Identification of differential PI3K pathway target dependencies in T-cell acute lymphoblastic leukemia through a large cancer cell panel screen. Oncotarget. 2016 Apr 19; 7(16): 22128–22139.
A10389 SALE	FK-506 (Tacrolimus)	mTOR inhibitor	FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells. Product Citations (2) Ogawa Y, .et al. Inhibition of astrocytic adenosine receptor A2A attenuates microglial activation in a mouse model of Sandhoff disease, Neurobiol Dis, 2018, Oct;118:142-154 PMID: 30026035 Yuko Okamoto, .et al. In vivo drug delivery efficiency of albumin-encapsulated liposomes as hydrophobic drug carriers, J Drug Deliv Sci Technol, 2018, 47: 62-66
A10693 SALE	Palomid 529 (P529)	AKT Inhibitor	Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation.
A10746 SALE	PP242 (Torkinib)	mTOR Inhibitor	PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2. Product Citations (2) Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
A10505 SALE	KU-0063794	mTOR Inhibitor	KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively).
A10374 SALE	Everolimus (RAD001)	mTOR inhibitor	Everolimus (RAD-001) is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an mTOR inhibitor. Product Citations (4) Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 Nachi Namatame, .et al. Antitumor profile of the PI3K inhibitor ZSTK474 in human sarcoma cell lines, Oncotarget, 2018, Oct 12; 9(80): 35141-35161 PMID: 30416685 Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168 Rieko Ohki, .et al. PHLDA3 is a novel tumor suppressor of pancreatic neuroendocrine tumors, Proc Natl Acad Sci U S A., 2014, 111(23): E2404-E2413. PMID: 24912192
A10438 SALE	GSK1059615	mTOR/PI3K Inhibitor	GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM). Product Citations (1) Jing Xie, .et al. GSK1059615 kills head and neck squamous cell carcinoma cells possibly via activating mitochondrial programmed necrosis pathway, Oncotarget, 2017, Aug 1; 8(31): 50814-50823 PMID: 28881606
A10726 SALE	PI-103	PI3K Inhibitor	PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR. Product Citations (1) Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
A10782 SALE	Rapamycin (Sirolimus)	mTOR Inhibitors	Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2). Product Citations (2) Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435 Ya-Hui Chen, .et al. The Different Effects of Atorvastatin and Pravastatin on Cell Death and PARP Activity in Pancreatic NIT-1 Cells, J Diabetes Res, 2016, 2016: 1828071 PMID: 28004006
A10906 SALE	Temsirolimus (Torisel)	mTOR inhibitor	Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells.
A11038 SALE	WYE-125132 (WYE-132)	mTOR Inhibitor	WYE-125132 is an ATP-competitive and specific inhibitor of mTORC1 and mTORC2 (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks).
A10997 SALE	XL765	PI3K inhibitor	XL765 is a PI3K/mTOR dual kinase inhibitor and it is more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.
A11056	OSI-027	mTOR inhibitor	OSI-027 is a potent, selective and orally bioavailable mTOR kinase inhibitor that inhibits the kinase activity associated with both the TORC1 and TORC2 complexes of mTOR.
A10295	Deforolimus (Ridaforolimus)	mTOR Inhibitor	Deforolimus (Ridaforolimus) is an investigational targeted and small-molecule inhibitor of the protein mTOR. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.
A10989 SALE	WYE-354	mTOR Inhibitor	WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of PI3K α (IC50 = 1026 nM) and other kinases. Product Citations (1) H Weber ,etc. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Oncotarget, 2015, 6(31), 31877.
A11207 SALE	PP121	PI3K Inhibitor	PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).
A11188	WAY-600	mTOR inhibitor	WAY-600 is a single digit nanomolar inhibitor of the mTOR kinases, with significant selectivity for these enzymes over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold).
A11187	WYE-687	mTOR Inhibitor	WYE-687 is a novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin(mTOR).
A11169 SALE	CH5132799	PI3K inhibitor	CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM).
A11162 SALE	NVP-BGT226	PI3K inhibitor	NVP-BGT226, novel phosphoinositide 3-kinase/mTOR dual inhibitor, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.
A11079 SALE	PKI-587 ( Gedatolisib )	PI3K/mTOR inhibitor	PKI-587 is a highly potent PI3K/mTOR kinase inhibitor that inhibits PI3K-α,β,γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively.
A10114 SALE	AZD8055	mTOR Inhibitor	AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. Product Citations (2) Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877-31888 PMID: 26397134 Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380

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A11035 SALE

A15175

A11024 SALE

A11023 SALE

A15508 SALE

A12480 SALE

A11537

A16126

A16276

A10133 SALE

A12935

A13328

A12395 SALE

A11587 SALE

A11586

A11950 SALE

A11443 SALE

A14114

A14432

A13519

A10900

A15147

A15779

A13078

A11461 SALE

A11303 SALE

A10389 SALE

A10693 SALE

A10746 SALE

A10505 SALE

A10374 SALE

A10438 SALE

A10726 SALE

A10782 SALE

A10906 SALE

A11038 SALE

A10997 SALE

A11056

A10295

A10989 SALE

A11207 SALE

A11188

A11187

A11169 SALE

A11162 SALE

A11079 SALE

A10114 SALE

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