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Submit ReviewCrizotinib is a potent inhibitor of c-MET and anaplastic lymphoma kinase (ALK) (cell IC50 values are 8.0 and 20 nM respectively). Selective for c-MET and ALK against >120 different kinases. Displays antitumor efficacy in multiple tumor models; inhibits c-MET-dependent proliferation, migration and invasion of human tumor cells in vitro. Orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc.
分子量 | 450.34 |
公式 | C21H22Cl2FN5O |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 877399-52-5 |
PubChem ID | 11626560 |
InChI Key | KTEIFNKAUNYNJU-GFCCVEGCSA-N |
Smiles | ClC1=[C@@]([C@H](OC2=C(N)N=CC(C3=CN(C4CCNCC4)N=C3)=C2)C)C(Cl)=CC=C1F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 4.5 | 10 | |
2eq.HCl | 45.03 | 100 |
以下数据基于产品分子量 450.34。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.22 mL | 11.1 mL | 22.21 mL |
5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
参考文献是支持产品生物活性的出版物。
Christensen et al (2007) Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol.Cancer Ther. 6 3314 PMID: 18089725
Zou et al (2007) An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 67 4408 PMID: 17483355
Cui et al (2011) Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J.Med.Chem. 54 6342 PMID: 21812414
If you know of a relevant reference for Crizotinib, please let us know.
关键词: Crizotinib, Crizotinib supplier, c-MET, alk, anaplastic, lymphoma, kinases, antitumor, selective, potent, PF2341066, PF02341066, PF, 02341066, 2341066, MET, Receptors, ALK, 4368, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Crizotinib 的部分引用包括:
Zhu et al (2016) Crosstalk between bone marrow-derived myofibroblasts and gastric cancer cells regulates cancer stemness and promotes tumorigenesis. Oncogene 35 5388 PMID: 27109105
Qi et al (2011) Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors. Cancer Res 71 1081 PMID: 21266357
Alan M et al (2020) Synergistic activity of agents targeting growth factor receptors, CDKs and downstream signaling molecules in a panel of pancreatic cancer cell lines and the identification of antagonistic combinations: Implications for future clinical trials in pancreatic Oncol Rep 44 2581-2594 PMID: 33125153
Gimenez-Xavier et al (2017) Genomic and Molecular Screenings Identify Different Mechanisms for Acquired Resistance to MET Inhibitors in Lung Cancer Cells. Mol Cancer Ther 16 1366 PMID: 28396363
Gimenez-Xavier et al (2018) Deep analysis of acquired resistance to FGFR1 inhibitor identifies MET and AKT activation and an expansion of AKT1 mutant cells. Oncotarget 9 31549 PMID: 30140389
Jan et al (2021) The tyrosine kinase inhibitor crizotinib influences blood glucose and mRNA expression of GLUT4 and PPARs in the heart of rats with experimental diabetes. Can J Physiol Pharmacol 99 635-643 PMID: 33201727
Maru et al (2019) Establishment and characterization of patient-derived organoids from a young patient with cervical clear cell carcinoma. Cancer Sci PMID: 31265190
Ayoub (2017) Crizotinib, a MET inhibitor, inhibits growth, migration, and invasion of breast cancer cells in vitro and synergizes with chemotherapeutic agents. Onco Targets Ther 10 4869 PMID: 29042798
Sullivan et al (2012) ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53. FASEB J 8 646 PMID: 22660439
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