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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Deforolimus

HY-50908

(AP23573; MK-8669; Ridaforolimus; AP 23573; MK 8669; AP-23573; MK8669)

Deforolimus

Deforolimus Chemical Structure

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.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $85 In-stock
10 mg $77 In-stock
50 mg $296 In-stock
100 mg Get quote
200 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €83 In-stock
10 mg €75 In-stock
50 mg €290 In-stock
100 mg Get quote
200 mg Get quote

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Product name: Deforolimus
Cat. No.: HY-50908

Deforolimus Data Sheet

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    Purity: 97.83%

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Biological Activity of Deforolimus

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 [1]
Target: mTOR
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 [1]. 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 [2].
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 [1].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 990.21 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C53H84NO14P
CAS No 572924-54-0
Solvent & Solubility

DMSO ≥196mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

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

Clinical Information of Deforolimus

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

References on Deforolimus

Inhibitor Kit

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