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T-8040 Temsirolimus, >99%       Prices Reduced (May 2010)

[CCI-779] [Torisel] [42-(3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoyl)-rapamycin]

M.W. 1030.29

C56H87NO16

[162635-04-3]

M.I. 14:  9142

Storage:  Store at or below -20 ºC. Solubility:  Soluble in DMSO at 200 mg/mL; soluble in ethanol at 200 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Temsirolimus, a rapamycin (sirolimus) derivative, also known as CCI-779, is an mTOR inhibitor with anti-cancer activity.  Wan, X., et al.  "CCI-779 Inhibits Rhabdomyosarcoma Xenograft Growth by an Antiangiogenic Mechanism Linked to the Targeting of mTOR/Hif-1α/VEGF Signaling."  Neoplasia 8:  394-401 (2006).

• Antiangiogenic effects may contribute to the antitumor activity of temsirolimus observed in breast cancer.  Del Bufalo, D., et al.  "Antiangiogenic potential of the Mammalian target of rapamycin inhibitor temsirolimus."  Cancer Res. 66:  5549-5554 (2006).

• Temsirolimus showed synergistic in vivo antimyeloma effects in combination with dexamethasone in a xenograft model.  Yan, H., et al.  "Mechanism by Which Mammalian Target of Rapamycin Inhibitors Sensitize Multiple Myeloma Cells to Dexamethasone-Induced Apoptosis."  Cancer Res. 66:  2305-2313 (2006).

• In lymphoblasts from adult patients with acute lymphoblastic leukemia (ALL), cells treated with sirolimus showed an increase in apoptotic cells and a dramatic decrease in cell proliferation compared to untreated cells.  Mice bearing NOD/SCID xenografts treated with temsirolimus showed a decrease in splenomegaly and in peripheral-blood blasts.  On the other hand, untreated mice continued to show expansion of human ALL.  Temsirolimus also down-regulated the mTOR signaling intermediate phospho-S6 in xenografted human ALL.  Teachey, D.T., et al.  "The mTOR inhibitor CCI-779 induces apoptosis and inhibits growth in preclinical models of primary adult human ALL."  Blood 107:  1149-1155 (2006).

• Temsirolimus is able to reverse cisplatin resistance in small cell lung cancer cell lines selected for cisplatin resistance and in cell lines derived from patients who failed cisplatin therapy.  Wu, C., et al.  "Overcoming cisplatin resistance by mTOR inhibitor in lung cancer."  Mol. Cancer 4:  25-34 (2005).

• Temsirolimus is the active ingredient in the drug sold under the trade name Torisel®.  This drug has been approved in at least one country for use in patients with advanced renal (kidney) cell carcinoma.  NOTE:  The temsirolimus sold by LC Laboratories is NOT Torisel®, and is NOT for human use.

• Sold for laboratory or manufacturing purposes only; not for human, 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.

• Please see also our other standard immunosuppressant products:

  A-1040   Ascomycin

  C-1377   CP-690550, Free Base

  C-6000   Cyclosporin A

  E-4040   Everolimus

  F-4633   Fingolimod, Hydrochloride Salt

  F-4900   FK-506

  M-7800   Mycophenolic Acid, Free Acid

  P-6040   Pimecrolimus

  R-5000   Rapamycin

  Z-9040   Zotarolimus