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12209
Nilotinib
Activators & Inhibitors
Chemical Modulators

Nilotinib #12209

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Nilotinib: Image 1

Chemical structure of nilotinib.

Nilotinib: Image 2

Western blot analysis of extracts from K562 cells untreated (-) or treated with Nilotinib (+) at 1uM for 24 hours, using Phospho-CrkL (Tyr207) Antibody #3181 (upper), CrkL (D4G7G) Rabbit mAb #38710 (middle) and B-Actin (D6A8) Rabbit mAb #8457 (lower).

Product Usage Information

Nilotinib is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 5 mg in 1.89 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 10-1000 nM for 2-72 hr. Nilotinib is soluble in DMSO at 50 mg/ml; very poorly soluble in ethanol and water with maximum solubility in water at ~10-20 µM.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 529.52 g/mol
Purity

>99%

Molecular Formula

C28H22F3N7O

CAS 641571-10-0
Solubility Soluble in DMSO at 50mg/ml.

Background

Nilotinib (AMN-107) is a novel tyrosine kinase inhibitor that potently inhibits Bcr-Abl. Nilotinib is more effective than imatinib at decreasing the proliferation and viability in cells expressing wild-type Bcr-Abl and is active against many imatinib-resistant Bcr-Abl mutants, with the exception of T315I (1-4). Nilotinib has been shown to inhibit Abl activity in cells expressing wild-type Abl and imatinib-resistant mutant Abl, with ~20-fold greater potency than imatinib. Nilotinib is similarly effective at inhibiting Abl autophosphorylation (3). Research studies have demonstrated that nilotinib treatment of Bcr-Abl-expressing K-562 cells attenuates Stat5 and CrkL phosphorylation, decreases Bcl-xL and c-Myc expression, induces p27 and Bim expression, and induces PARP cleavage. Many of these effects are enhanced by cotreatment with the histone deacetylase inhibitor LBH589 (5).

  1. Weisberg, E. et al. (2006) Br J Cancer 94, 1765-9.
  2. Golemovic, M. et al. (2005) Clin Cancer Res 11, 4941-7.
  3. O'Hare, T. et al. (2005) Cancer Res 65, 4500-5.
  4. Weisberg, E. et al. (2005) Cancer Cell 7, 129-41.
  5. Fiskus, W. et al. (2006) Blood 108, 645-52.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
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To Purchase # 12209S
Product # Size Price
12209S
5 mg $ 108