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(AP23573; MK-8669; Ridaforolimus; AP 23573; MK 8669; AP-23573; MK8669)
Deforolimus Chemical Structure
|Product name: Deforolimus|
|Cat. No.: HY-50908|
Deforolimus(AP23573; MK-8669; Ridaforolimus) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin.
IC50 value: 0.2 nM 
in vitro: Treatment of HT-1080 cells with Deforolimus induces a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50 of 0.2 nM and 5.6 nM, respectively, and leads to a decrease in cell size, an increase in the proportion of cells in the G1 phase of the cell cycle, and inhibition of glucose uptake. Deforolimus displays significant antiproliferative activity a broad panel of cell lines with EC50 of 0.2-2.3 nM. Deforolimus potently and selectively inhibits VEGF production in a dose-dependent manner . Deforolimus treatment significantly induces growth suppression in human NSCLC cell lines with IC30 values of 2.45-8.83 nM, with the exception of H157 with IC30 of >20 nM. Deforolimus treatment (2.8-5.9 nM) significantly dephosphorylates p70S6KThr389 in A549, H1703 and H157 cells, except H1666 that may express a resistant variant of mTORC1, and causes increased phosphorylation of pAKTser473 and pAKTThr308 in A549 and H1703 cells. Deforolimus in combination with the MEK inhibitors, CI-1040 or PD0325901 exhibits dose-dependent synergism in lung cancer cell lines, which is associated with the suppression of proliferation rather than enhancement of cell death, involving the inhibition of ribosomal biogenesis by 40% within 24 hours and a decreased polysome/monosome ratio .
in vivo: Administration of Deforolimus exerts significant antitumor effects in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas) or A549 (lung) xenografts in a dose-dependent manner, and inhibits mTOR signaling in in SK-LMS-1 xenograft model associated with inhibition of tumor growth .
|M.Wt||990.21||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥196mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.0099 mL||5.0494 mL||10.0989 mL|
|5 mM||0.2020 mL||1.0099 mL||2.0198 mL|
|10 mM||0.1010 mL||0.5049 mL||1.0099 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Deforolimus||Rajavithi Hospital||Cholangiocarcinoma||31-JAN-12||30-JUN-14||Phase 2||11-SEP-13|
|Merck & Co Inc||Metastatic breast cancer||31-JUL-12||31-JAN-15||Phase 2||08-OCT-13|
|Merck & Co Inc||Sarcoma||31-OCT-07||31-DEC-12||Phase 3||22-FEB-13|
|Merck & Co Inc||Bone tumor||31-OCT-07||31-DEC-12||Phase 3||22-FEB-13|
|Merck & Co Inc||Metastatic breast cancer||30-SEP-10||31-OCT-13||Phase 2||07-NOV-13|
|Memorial Sloan-Kettering Cancer Center||Renal cell carcinoma||31-JUL-11||31-JUL-14||Phase 2||23-SEP-13|
. Rivera VM, et al. Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens. Mol Cancer Ther, 2011, 10(6), 1059-1071.
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