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You are here:Home-Inhibitors & Agonists-PI3K/Akt/mTOR Pathway-mTOR

Request The Product List ofmTOR mTOR

mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. mTOR belongs to the phosphatidylinositol 3-kinase-related kinase protein family. mTOR integrates the input from upstream pathways, including growth factors and amino acids. mTOR also senses cellular nutrient, oxygen, and energy levels. The mTOR pathway is dysregulated in human diseases, such as diabetes, obesity, depression, and certain cancers. Rapamycin inhibits mTOR by associating with its intracellular receptor FKBP12. The FKBP12-rapamycin complex binds directly to the FKBP12-Rapamycin Binding (FRB) domain of mTOR, inhibiting its activity.

Cat. No. Product Name CAS No. Information
GY02657

NV-128

154447-38-8

NV-128 (LY-303511) is a novel isoflavone derivative that inhibits mTOR and promotes caspase-independent cell death; induce significant cell death in both paclitaxel-resistant and carboplatin-resistant EOC cells with GI50 of 1-5 ug/mL; significantly depresses mitochondrial function by decrease in ATP, Cox-I, and Cox-IV levels, and by increase in mitochondrial superoxide and hydrogen peroxide.

GY02545

CZ-415

1429639-50-8

A potent, highly selective, ATP-competitive and orally bioavailable mTOR inhibitor with pKd of 8.2; displays >100-fold selectivity over PI3Ks; inhibit downstream targets phosphorylation of pS6RP (S240/244) and pAkt (S473) in HEK293T cells with IC50 of 14.5 nM and 14.8 nM, inhibits IFNγ production in stimulated human whole blood with IC50 of 226 nM; shows efficacy in a semitherapeutic collagen induced arthritis (CIA) mouse model.

GY07021

AZD 3147

1101810-02-9

AZD 3147 is a potent, selective dual mTORC1 and mTORC2 inhibitor with enzyme IC50 of 1.5 nM; weakly inhibits PI3K isoforms with IC50 of 1-10 uM, potently inhibits pAKT at Ser473 with pIC50 of 8.25; has exellentphysicochemical and pharmacokinetic properties.

GY10528

MTI-31

1567915-38-1

MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR), displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G; showed an IC50 value 39 nM in LANCE® assay of mTOR substrate phosphorylation; dose-dependently inhibits of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473) tumor cell lines harboring mTOR pathway dysregulation with IC50 of <0.12 uM; potently inhibited cell proliferation (IC50 <1 mmol/L) and in vivo tumor growth in multiple NSCLC models of EGFR/T790M, EML4-ALK, c-Met or KRAS (MED <10 mg/kg), also suppressed programmed death ligand 1 (PD-L1) in EGFR- and ALK-driven NSCLC, mediated in part by mTORC2/AKT/GSK3β-dependent proteasomal degradation.

GY02355

CC-115 hydrochloride

1300118-55-1

A novel dual inhibitor of mTOR and DNA-PK with IC50 of 21 nM and 13 nM, respectively; blocks both mTORC1(pS6) and mTORC2(pAktS473) signaling in PC-3 cancer cells, in vitro and in vivo; exhibits dose-dependent efficacy in tumor xenograft models.

GY02272

CC-223

1228013-30-6

A potent, selective, and orally bioavailable inhibitor of mTOR kinase with IC50 of 16 nM; displays >200-fold selectivity over the related PI3K-α (IC50=4.0 uM), shows no significant inhibition of ATR or SMG1 and weakly inhibits DNA-PK (IC50=0.84 uM); inhibits mTORC1 (pS6RP and p4EBP1) and mTORC2 [pAKT(S473)] in cellular systems, exhibits growth inhibitory activity in hematologic and solid tumor cell lines; demonstrates tumor growth inhibition in multiple solid tumor xenografts.

GY02271

CC-115

1228013-15-7

A novel dual inhibitor of mTOR and DNA-PK with IC50 of 21 nM and 13 nM, respectively; blocks both mTORC1(pS6) and mTORC2(pAktS473) signaling in PC-3 cancer cells, in vitro and in vivo; exhibits dose-dependent efficacy in tumor xenograft models.

GY02241

mTOR-IN-1

1207358-59-5

A potent and selective mTOR inhibitor with Ki of 1.5 nM; >500-fold selectivity over closely related PI3 kinases; exhibits suitable mouse PK and demenstrates active in an NCI-PC3prostate cancer model; orally bioavailable.

GY01914

WYE-354

1062169-56-5

WYE-354 is a potent, selective and ATP-competitive inhibitor of mTOR with IC50 of 5 nM (recombinant mTOR ), displays >100-fold selectivity over PI3K isofoms; acutely blocks substrate phosphorylation by mTORC1 and mTORC2 in vitro and in cells in response to growth factor, amino acids, and hyperactive PI3K/AKT, reduces AKT downstream function and inhibits proliferation of diverse cancer cell lines; inhibits mTORC1 and mTORC2 and displayed robust antitumor activity in PTEN-null tumors.

GY03055

Zotarolimus

221877-54-9

Zotarolimus (ABT-578, A 179578) is a semi-synthetic analogue of rapamycin, inhibits FKBP-12 binding with IC50 of 2.8 nM and shows less potent systemic immunosuppression than rapamycin; effectively inhibits both smooth muscle cell and endothelial cell proliferation, with IC50 values of 2.9 nM and 2.6 nM, respectively; exhibits high-affinity binding to the immunophilin FKBP12, inhibiting in vitro proliferation of both human and rat T cells; inhibits Con A-induced human T cells with IC50 of 7.0 nM; reduce early complications and improve late clinical outcomes in patients needing

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