C-7900 Crizotinib, Free Base, >99%

Synonyms : [PF-02341066] [PF-1066] [PF-2341066]

Related Terms : [Xalkori]

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  • M.W. 450.34
  • C21H22Cl2FN5O
  • [877399-52-5]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 25 mg/mL with warming; soluble in ethanol at 25 mg/mL with warming; 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 aqueo. Disposal: A.

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  • Crizotinib, also known as PF-02341066, is a potent ATP-competitive, recombinant human c-Met kinase inhibitor (Ki = 4 nM). In cell-based assays, it inhibited hepatocyte growth factor (HGF)-stimulated or constitutive total tyrosine phosphorylation of wild-type c-Met in a panel of human tumor and endothelial cell lines. It showed activity against c-Met phosphorylation in mIMCD3 mouse (IC50 = 5 nM) or MDCK canine (IC50 = 20 nM) epithelial cells. Crizotinib inhibited human GTL-16 gastric carcinoma cell growth (IC50 = 9.7 nM), induced apoptosis in GTL-16 cells (IC50 = 8.4 nM), inhibited HGF-stimulated human NCI-H441 lung carcinoma cell migration and invasion (IC50s of 11 and 6.1 nM, respectively), and inhibited MDCK cell scattering (IC50 = 16 nM). Crizotinib also inhibited HGF-stimulated c-Met phosphorylation (IC50 = 11 nM), cell survival (IC50 = 14 nM), and Matrigel invasion (IC50 = 35 nM) in human umbilical vascular endothelial cells. In addition, it inhibited serum-stimulated human dermal microvascular endothelial cell branching tubulogenesis (formation of vascular tubes) in fibrin gels. Crizotinib showed antitumor effects in vivo in c-Met-dependent human xenograft models including GTL-16 human gastric carcinoma, U87MG human glioblastoma, NCI-H441 NSCLC, Caki-1 RCC, and PC-3 prostate carcinoma. Zou, H.Y., et al. "An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms." Cancer Res. 67: 4408-4417 (2007).
  • The EC90 (167 ng/ml) for the inhibition of cMet phosphorylation in athymic mice bearing GTL16 tumors corresponded to the EC50 (213 ng/ml) for the GTL16 tumor growth inhibition, indicating that near-complete inhibition of cMet phosphorylation (>90%) is required to significantly inhibit tumor growth (>50%). Yamazaki, S., et al. "Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse models." Drug Metab. Dispos. 36: 1267-1274 (2008)
  • Crizotinib showed gender-related differences in pharmacokinetics in rats, with at least 2-fold higher crizotinib plasma concentrations in males than females when administered at the same dose. In male rat liver S9 incubation oxidation was the major metabolic pathway, whereas in females sulfoconjugation predominanted. Zhong, W.Z., et al. "Gender specific drug metabolism of PF-02341066 in rats--role of sulfoconjugation." Curr. Drug Metab. 11: 296-306 (2010).
  • 76 patients with non-small cell lung cancer harboring anaplastic lymphoma kinase (ALK) fusion were recruited for a phase II clinical trial of crizotinib. The median half-life was about 53 hours. 50 patients were evaluable for response. The overall response rate was 64% and the disease control rate was 90%. Gastrointestinal toxicities (nausea and vomiting) were the most frequent adverse events. Bang, Y., et al. "Clinical activity of the oral ALK inhibitor PF-02341066 in ALK-positive patients with non-small cell lung cancer (NSCLC)." J. Clin. Oncol. 28: 3 (2010).
  • This crizotinib product is the free base, whose CAS number is given above. The CAS number of the acetate salt is 877399-53-6.
  • Another CAS number previously assigned to crizotinib, namely 912279-98-2, has been deleted by CAS and is no longer in use.
  • Crizotinib is the active ingredient in the drug product sold under the trade name Xalkori®. This drug is currently approved in at least one country for use in patients with locally advanced or metastatic non-small cell lung cancer that is anaplastic lymphoma kinase-positive.  NOTE: THE CRIZOTINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT XALKORI®, 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.