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R-7040 Ridaforolimus, >99%       Prices Reduced (September 2011)

[9CI] [AP 23573] [Deforolimus] [MK-8669] [AP-23573] [AP23573] [MK 8669] [MK8669]

M.W. 990.21

C53H84NO14P

[572924-54-0]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

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• Ridaforolimus (the name has been changed from "deforolimus") is an immunosuppressant and a novel small-molecule inhibitor of the protein mammalian target of rapamycin (mTOR).  Ridaforolimus inhibits cancer cell growth, cell division, metabolism, and angiogenesis by blocking mTOR.  Mahalingam, D., et al.  "Targeting the mTOR pathway using deforolimus in cancer therapy."  Future Oncol. 5:  291-303 (2009).

• Ridaforolimus had an antitumor activity in >85% of patients with advanced solid tumors.  Rivera, V.M., et al.  "Pharmacodynamic study of skin biopsy specimens in patients (pts) with refractory or advanced malignancies following administration of AP23573, an mTOR inhibitor."  J. Clin. Oncol. 23:  3033 (2005).

• Ridaforolimus has low toxicity profiles and promising clinical efficacy in patients with advanced sarcomas.  Chawla, S.P., et al.  "Updated results of a phase II trial of AP23573, a novel mTOR inhibitor, in patients (pts) with advanced soft tissue or bone sarcomas."  J. Clin. Oncol. 24:  9505 (2006).

• The level of phosphorylated S6 ribosomal protein expression was a marker of early tumor response to ridaforolimus.  Iwenofu, O.H., et al.  "Phospho-S6 ribosomal protein: a potential new predictive sarcoma marker for targeted mTOR therapy."  Mod. Pathol. 21:  231-237 (2008).

• MEK inhibitors in combination with the mTOR inhibitor, rapamycin or its analogue ridaforolimus, exhibited synergism in human lung cancer cell lines by inhibiting proliferation rather than promoting cell death.  Legrier, M.E., et al.  "Targeting protein translation in human non small cell lung cancer via combined MEK and mammalian target of rapamycin suppression."  Cancer Res. 67:  11300-11308 (2007).

• Another CAS number previously assigned to ridaforolimus, 697252-87-2, has been deleted by CAS and is no longer in use.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.