Deforolimus (Ridaforolimus) Chemical Structure
BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.
PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.
Rapamycin also known as Sirolimus & Rapamune is an mTOR inhibitor. Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated pathways.
Temsirolimus (Torisel) is a mTOR inhibitor.
Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress and Afinitorm is an mTOR inhibitor available at Selleck with IC50 of 0.63 nM.
Ku-0063794 is an mTOR inhibitor, IC50 ~10 nM for mTORC1 and mTORC2, respectively.
WYE-354 is an mTOR inhibitor with an IC50 of 5 nM.
GSK1059615 is a pan-PI3K reversible inhibitor,IC50:PI3Kα(0.4 nM), β (0.6 nM),γ (5 nM),δ (2 nM) and mTOR(12 nM).
XL765 is a mixed mTOR/PI3k inhibitor with IC50 of 157, 39, 113, 9 and 43 nM for mTOR, p110α, β, γ and δ, respectively.
AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM.
Deforolimus (Ridaforolimus) is a small-molecule inhibitor of mTOR. It is an immunosuppressant for the treatment of certain cancers. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis. [1]
| Molecular Weight (WM): | 990.21 |
|---|---|
| Formula: | C53H84NO14P |
| CAS No.: | 572924-54-0 |
| Synonyms: |
AP23573, MK-8669
|
| Dissolve in (25°C): | DMSO ≥198mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

Concentration-time profile in rat serum following administration of deforolimus formulations(10mg/kg) intravenously to rats (mean + SEM)
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Concentration-time profile in rat serum following administration of deforolimus formulations(10mg/kg) intravenously to rats (mean + SEM)
Data independently produced by Dr Neal M. Davies of Washington State University Deforolimus (Ridaforolimus) purchased from Selleck

Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
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Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
Data independently produced by Dr Zhang of Tianjin Medical University Deforolimus (Ridaforolimus) purchased from Selleck
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