Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(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.
AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (～1,000-fold) against PI3K isoforms and ATM/DNA-PK.
AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM; highly selective against multiple PI3K isoforms ((alpha)/(beta)/(gamma)/(delta)).
CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with >150-fold sensitivity over the related lipid kinase PI3K(alpha) (IC50=4 (mu)M).
ETP-46464 is a cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-K(alpha), and ATM (IC50= 0.6, 14, 36, 170, and 545 nM, respectively).
Everolimus (RAD001) is a mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3K(alpha) and other 266 kinases.
GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3K(alpha)/(beta)/(delta)/(gamma) with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively; also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.
GNE-317 is a potent PI3K/mTOR inhibitor that can cross the blood–brain barrier; shows potent suppression of the PI3K pathway in the brain of mice with intact BBB.
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3K(alpha), Kiapp is 21 nM for mTOR.
GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3K(alpha)/PI3K(beta)/PI3K(gamma)/PI3K(delta)/mTOR respectively.