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4401
Crizotinib
Activators & Inhibitors
Chemical Modulators

Crizotinib #4401

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Crizotinib: Image 1

Chemical structure of crizotinib.

Crizotinib: Image 2

Western blot analysis of extracts from KARPAS-299 cells, untreated or treated with crizotinib (1 hr) at the indicated concentrations, using Phospho-ALK (Tyr1604) Antibody #3341 (upper) or ALK (D5F3) XP® Rabbit mAb #3633 (lower).

Product Usage Information

Crizotinib is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 2.5 mg in 5.55 ml DMSO. Working concentrations and length of treatments vary depending on the desired effect, but it is typically used at 0.1-1 µM for 2-6 h. Soluble in DMSO at 25 mg/ml with warming; very poorly soluble in water with maximum solubility ~10-20 µM.

Storage

Store lyophilized or in solution at -20ºC, desiccated. 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 450.34 g/mol
Purity

>99%

Molecular Formula

C21H22Cl2FN5O

CAS 877399-52-5
Solubility Soluble in DMSO and EtOH at 25mg/ml.

Background

Crizotinib, also known as PF-02341066, is a novel, ATP-competitive receptor kinase inhibitor, showing high specificity for c-Met and anaplastic lymphoma kinase (ALK) over 120 other diverse kinases (1,2). Researchers have shown that crizotinib inhibits c-Met phosphorylation and c-Met-dependent proliferation, migration, and invasion of human tumor cells in vitro (IC50 values of 5–20 nM) (1). Crizotinib is effective against the constitutively active oncogenic fusion protein nucleophosmin (NPM)-ALK, inhibiting its phosphorylation (mean IC50 of 24 nM), inhibiting cell growth, and inducing G1-S phase cell cycle arrest and apoptosis in the ALK-positive ALCL (anaplastic large-cell lymphoma) cell lines KARPAS-299 and SU-DHL-1 (2).

  1. Zou, H.Y. et al. (2007) Cancer Res 67, 4408-17.
  2. Christensen, J.G. et al. (2007) Mol Cancer Ther 6, 3314-22.

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.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 4401S
Product # Size Price
4401S
2.5 mg N/A

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