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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

(±)-Nutlin-3

Cayman Chemical Item Number 10004372

(CAS 548472-68-0)

(±)-Nutlin-3 (CAS 548472-68-0)

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Sold under license from Hoffman-La Roche.

Description

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

1 El-Deiry, W.S. The p53 pathway and cancer therapy. Cancer J 11 229-236 (1998).

2 Lane, D.P., and Hupp, T.R. Drug discovery and p53. Drug Discov 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).

Formal Name (±)-​4-​[4,​5-​bis-​(4-​chlorophenyl)-​2-​(2-​isopropoxy-​4-​methoxy-​phenyl)-​4,​5-​dihydro-​imidazole-​1-​carbonyl]-​piperazin-​2-​one
CAS Number 548472-68-0
Molecular Formula C30H30Cl2N4O4
Formula Weight 581.5
Formulation A crystalline solid
Purity >98%
Stability 1 year
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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ClC(C=C1)​=CC=C1[C@H]​2[C@@H]​(C3=CC=C(Cl)​C=C3)​N(C(N4CCN([H]​)​C(C4)​=O)​=O)​C(C5=CC=C(OC)​C=C5OC(C)​C)​=N2

Background Reading

El-Deiry, W.S. The p53 pathway and cancer therapy. Cancer J 11 229-236 (1998).

Lane, D.P., and Hupp, T.R. Drug discovery and p53. Drug Discov Today 8(8) 347-355 (2003).

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).

(±)-Nutlin-3 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $23.00 $0.00
5 mg $104.00 $0.00
10 mg $184.00 $0.00
50 mg $403.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-10. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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Sold under license from Hoffman-La Roche.

Cayman Chemical is a manufacturer, supplier and vendor of biochemical reagents, assay kits, antibodies, and proteins.

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