mTOR

mTOR Inhibitors | Activators (36)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1039 Rapamycin (Sirolimus) Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
  • Nat Genet, 2014, 46(4):364-70
  • Cancer Cell, 2011, 19(6):792-804
  • Cell Res, 2012, 22(6):1003-21
S1120 Everolimus (RAD001) Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.
  • Cell, 2016, 164(1-2):293-309
  • Cell, 2016, 164(1-2):293-309
  • Cell, 2012, 149(3):656-70
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1.
  • Nat Med, 2015, 10.1038/nm.3855
  • Cancer Cell, 2015, 27(1):97-108
  • Cancer Cell, 2015, 27(4):533-46
S1044 Temsirolimus (CCI-779, NSC 683864) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.
  • Autophagy, 2011, 7(2):176-87
  • Cancer Res, 2014, 74(14):3947-58
  • Mol Oncol, 2014, 10.1016/j.molonc.2014.05.005
S1226 KU-0063794 KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.
  • Cell Stem Cell, 2012, 10(2):210-7
  • Circ Res, 2010, 107(10):1265-74
  • Oncogene, 2013, 10.1038/onc.2013.509
S7646 Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
S1009 BEZ235 (NVP-BEZ235, Dactolisib) BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.
  • Nature, 2012, 487(7408):505-9
  • Nat Med, 2015, 10.1038/nm.3855
  • Cancer Cell, 2012, 21(2):155-67
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
  • Cell, 2013, 153(4):840-54
  • Leukemia, 2013, 27(3):650-60
  • Leukemia, 2012, 26(5):927-33
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.
  • J Clin Invest, 2015, 10.1172/JCI78018
  • Nat Chem Biol, 2013, 9(11):708-14
  • Autophagy, 2012, 8(6):903-14
S5003 Tacrolimus (FK506) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.
  • Biomed Pharmacother, 2013, 67(6):469-73
  • Universidad de Cantabria, 2012, García Díaz
  • Biochim Biophys Acta, 2012, 1833(3):652-62
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1022 Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
  • J Lipid Res, 2014, 55(5):919-28
  • Mol Pharmaco, 2013, 84(1):104-13
  • Int J Oncol, 2014, 44(3):959-69
S2811 INK 128 (MLN0128) INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
  • Cancer Discov, 2014, 4(5):554-63
  • Cell Rep, 2015, 11(3):446-59
  • Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15
S1523 Voxtalisib (SAR245409, XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
  • Cell Rep, 2015, 11(3):446-59
  • Endocrinology, 2013, 154(3):1247-59
  • Mol Cancer Res, 2014, 12(5):703-13
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
  • Cancer Discov, 2016, 6(7):727-39
  • Elife, 2015, 4
  • Mol Cell Biol, 2014, 34(24):4474-84
S2658 Omipalisib (GSK2126458, GSK458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Phase 1.
  • Proc Natl Acad Sci USA, 2013, 110(10):4015-20
  • Mol Cancer Ther, 2015, 14(2):429-39
  • J Pharmacol Exp Ther, 2013, 347(3):669-80
S2624 OSI-027 OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
  • Cell Rep, 2015, 11(3):446-59
  • Eur J Cancer, 2013, 74:41-9
  • J Gen Virol, 2014, 10.1099/vir.0.066332-0
S2743 PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
  • Blood, 2015, 10.1182/blood-2014-11-610329
  • Cell Rep, 2015, 11(3):446-59
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S2696 Apitolisib (GDC-0980, RG7422) Apitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Phase 2.
  • Cancer Discov, 2014, 4(5):554-63
  • Mol Cancer Ther, 2015, 14(8):1928-38
  • Breast Cancer Res, 2014, 16(4):406
S1360 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
  • Nature, 2012, 486(7404):532-6
  • Nat Chem Biol, 2013, 9(11):708-14
  • Exp Mol Med, 2015, 47:e143
S1266 WYE-354 WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
  • Cancer Lett, 2015, 359(1):97-106
  • Mol Biol Cell, 2013, 24(23):3736-45
  • Mol Cancer Res, 2012, 10(6):821-33
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2628 Gedatolisib (PF-05212384, PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
  • Cell Rep, 2015, 11(3):446-59
  • Mol Cancer Ther, 2015, 14(2):429-39
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S2783 AZD2014 AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). Phase 2.
  • Cancer Lett, 2015, 357(2):468-75
  • Transl Res, 2014, 164(5):411-23
  • J Biol Chem, 2014, 289(44):30625-34
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively.
  • J Clin Invest, 2013, 124(2):742-54
  • Cell Rep, 2015, 11(3):446-59
  • Oncotarget, 2014, 5(20):10034-47
S2661 WYE-125132 (WYE-132) WYE-125132 (WYE-132) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
  • J Cell Sci, 2014, 127(Pt 4):788-800
  • PLoS One, 2014, 9(8):e105280
S2749 BGT226 (NVP-BGT226) BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
  • Mol Cancer Ther, 2015, 14(8):1928-38
  • Cancer Lett, 2014, 348(1-2):38-49
  • PLoS One, 2014, 9(3):e90746
S2238 Palomid 529 (P529) Palomid 529 (P529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6 but no effect observed on pMAPK or pAktT308. Phase 1.
  • Mol Cancer Res, 2015, 13(2):223-30
  • J Pharmacol Exp Ther, 2013, 347(3):669-80
  • Ann Surg Oncol, 2014, 10.1245/s10434-014-3824-1
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
  • Tumour Biol, 2014, 35(9):8659-64
  • Biochem Biophys Res Commun, 2015, 465(1):137-44
  • Int J Clin Exp Pathol, 2013, 6(10):2082-91
S2668 WYE-687 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
  • J Hepatol, 2015, 10.1016/j.jhep.2015.11.011
S2699 CH5132799 CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1.
  • Am J Transl Res, 2014, 6(5):471-493
  • Biochimie, 2014, 105:182-91
S2689 WAY-600 WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
  • Biochem Biophys Res Commun, , 474(2):330-7
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
S8040 GDC-0349 GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
  • Biochem Biophys Res Commun, 2016, 477(2):174-80
S7035 XL388 XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.
S2406 Chrysophanic Acid Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
S7091 Zotarolimus(ABT-578) Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
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All mTOR Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1039 Rapamycin (Sirolimus) <1 mg/mL 20 mg/mL <1 mg/mL
S1120 Everolimus (RAD001) <1 mg/mL 30 mg/mL 7 mg/mL
S1555 AZD8055 <1 mg/mL 50 mg/mL 3 mg/mL
S1044 Temsirolimus (CCI-779, NSC 683864) <1 mg/mL 75 mg/mL 75 mg/mL
S1226 KU-0063794 <1 mg/mL 16 mg/mL <1 mg/mL
S7646 Voxtalisib (XL765, SAR245409) <1 mg/mL 54 mg/mL <1 mg/mL
S1009 BEZ235 (NVP-BEZ235, Dactolisib) <1 mg/mL 0.01 mg/mL <1 mg/mL
S1038 PI-103 <1 mg/mL 24 mg/mL <1 mg/mL
S2218 Torkinib (PP242) <1 mg/mL 62 mg/mL 18 mg/mL
S5003 Tacrolimus (FK506) <1 mg/mL 94 mg/mL 83 mg/mL
S1022 Ridaforolimus (Deforolimus, MK-8669) <1 mg/mL 198 mg/mL <1 mg/mL
S2811 INK 128 (MLN0128) <1 mg/mL 62 mg/mL 2 mg/mL
S1523 Voxtalisib (SAR245409, XL765) Analogue <1 mg/mL 12 mg/mL <1 mg/mL
S2827 Torin 1 <1 mg/mL 2 mg/mL <1 mg/mL
S2658 Omipalisib (GSK2126458, GSK458) <1 mg/mL 100 mg/mL <1 mg/mL
S2624 OSI-027 <1 mg/mL 18 mg/mL <1 mg/mL
S2743 PF-04691502 <1 mg/mL 14 mg/mL <1 mg/mL
S2696 Apitolisib (GDC-0980, RG7422) <1 mg/mL 20 mg/mL <1 mg/mL
S1360 GSK1059615 <1 mg/mL 2 mg/mL <1 mg/mL
S1266 WYE-354 <1 mg/mL 99 mg/mL <1 mg/mL
S2628 Gedatolisib (PF-05212384, PKI-587) <1 mg/mL 2 mg/mL <1 mg/mL
S2783 AZD2014 <1 mg/mL 38 mg/mL <1 mg/mL
S2817 Torin 2 <1 mg/mL 20 mg/mL <1 mg/mL
S2661 WYE-125132 (WYE-132) <1 mg/mL 104 mg/mL <1 mg/mL
S2749 BGT226 (NVP-BGT226) <1 mg/mL 30 mg/mL <1 mg/mL
S2238 Palomid 529 (P529) <1 mg/mL 81 mg/mL <1 mg/mL
S2622 PP121 <1 mg/mL 64 mg/mL 2 mg/mL
S2668 WYE-687 <1 mg/mL 0.5 mg/mL <1 mg/mL
S2699 CH5132799 <1 mg/mL 12 mg/mL <1 mg/mL
S2689 WAY-600 <1 mg/mL 22 mg/mL 2 mg/mL
S8050 ETP-46464 <1 mg/mL 6 mg/mL <1 mg/mL
S8040 GDC-0349 <1 mg/mL 91 mg/mL 6 mg/mL
S7035 XL388 <1 mg/mL 23 mg/mL <1 mg/mL
S2406 Chrysophanic Acid <1 mg/mL 5 mg/mL <1 mg/mL
S7091 Zotarolimus(ABT-578) <1 mg/mL 100 mg/mL 100 mg/mL
S7811 MHY1485 <1 mg/mL 33 mg/mL <1 mg/mL
Tags: mTOR inhibition | mTOR cancer | mTOR activation | mTOR target | mTOR tumor | mTOR phosphorylation | mTOR activity | mTOR inhibitor drugs | mTOR kinase assay | mTOR inhibitor cancer | mTOR inhibitor therapy | mTOR signaling pathway | mTOR inhibitor review
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