
Deforolimus
CAS No. 572924-54-0
Deforolimus( AP-23573 | MK-8669 | Ridaforolimus )
Catalog No. M15090 CAS No. 572924-54-0
A potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line.
Purity : >98% (HPLC)






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Biological Information
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Product NameDeforolimus
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line.
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DescriptionA potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; displays significant antiproliferative activity a broad panel of cell lines with EC50 of 0.2-2.3 nM; potently and selectively inhibits VEGF production in a dose-dependent manner; exerts significant antitumor effects in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas) or A549 (lung) xenografts.Breast Cancer Phase 2 Clinical(In Vitro):Treatment of HT-1080 fibrosarcoma cells with Ridaforolimus results in a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50s of 0.2 and 5.6 nM, respectively, and EC50s of 0.2 and 1.0 nM, respectively. In HT-1080 cells, the EC50 for inhibition of cell proliferation (0.5 nM) is similar to the EC50s for inhibition of S6 and 4E-BP1 phosphorylation. Exposure to Ridaforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of Ridaforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Ridaforolimus exhibits a predominantly cytostatic mode of action, consistent with the findings for other mTOR inhibitors. Potent inhibitory effects on vascular endothelial growth factor secretion, endothelial cell growth, and glucose metabolism.(In Vivo):Ridaforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Ridaforolimus inhibits tumor growth in a dose-dependent manner, with 0.3 mg/kg being the lowest dose that inhibits tumor growth significantly and 3 and 10 mg/kg doses achieving maximum inhibition.
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In VitroTreatment of HT-1080 fibrosarcoma cells with Ridaforolimus results in a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50s of 0.2 and 5.6 nM, respectively, and EC50s of 0.2 and 1.0 nM, respectively. In HT-1080 cells, the EC50 for inhibition of cell proliferation (0.5 nM) is similar to the EC50s for inhibition of S6 and 4E-BP1 phosphorylation. Exposure to Ridaforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of Ridaforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Ridaforolimus exhibits a predominantly cytostatic mode of action, consistent with the findings for other mTOR inhibitors. Potent inhibitory effects on vascular endothelial growth factor secretion, endothelial cell growth, and glucose metabolism.
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In VivoRidaforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Ridaforolimus inhibits tumor growth in a dose-dependent manner, with 0.3 mg/kg being the lowest dose that inhibits tumor growth significantly and 3 and 10 mg/kg doses achieving maximum inhibition.
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SynonymsAP-23573 | MK-8669 | Ridaforolimus
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PathwayPI3K/Akt/mTOR signaling
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TargetmTOR
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RecptormTOR
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Research AreaCancer
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IndicationBreast Cancer
Chemical Information
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CAS Number572924-54-0
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Formula Weight990.2061
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Molecular FormulaC53H84NO14P
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 44 mg/mL
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SMILES[H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N1CCCC[C@@]1([H])C(=O)O[C@@H](CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]1CC[C@@H](OP(C)(C)=O)[C@@H](C1)OC |r,c:31,50,t:46,48|
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Chemical NameRapamycin, 42-(dimethylphosphinate) (9CI)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Rivera VM, et al. Mol Cancer Ther. 2011 Jun;10(6):1059-71.
2. Legrier ME, et al. Cancer Res. 2007 Dec 1;67(23):11300-8.
3. Becker MA, et al. BMC Cancer. 2016 Oct 20;16(1):814.
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