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10004372 (±)-Nutlin-3
(CAS 548472-68-0)
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The protein p53, often called the 'guardian of the genome,' is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis.1,2 Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. Mdm2, a key negative regulator of p53 which is over-expressed in many human tumors, functions by binding to and targeting p53 for proteasomal degradation. Nutlin-3 inhibits p53-Mdm2 interaction with a IC50 of 0.09 µM.3 It induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells with mutated p53. Nutlin-3 also inhibits the growth of human tumor xenografts in nude mice by 90% at a dose of 200 mg/kg.3
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1
El-Deiry, W.S. The p53 pathway and cancer therapy. Cancer Journal 11 229-236 (1998).
2
Lane, D.P., Hupp, T.R. Drug discovery and p53. Drug Discovery Today 8(8) 347-355 (2003).
3
Vassilev, L.T., Vu, B.T., Graves, B., et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 303 844-848 (2004).
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Sold under license from Hoffman-La Roche.
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Pricing updated 2010-03-18.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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