(S)-crizotinib - CAS 1374356-45-2
Catalog number: 1374356-45-2
Category: Inhibitor
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Molecular Formula:
C21H22Cl2FN5O
Molecular Weight:
450.34
COA:
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Targets:
MTH1
Description:
(S)-crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single-strand breaks, and activates DNA repair in human colon carcinoma cells.
Purity:
>98%
MSDS:
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InChIKey:
KTEIFNKAUNYNJU-LBPRGKRZSA-N
InChI:
InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m0/s1
Canonical SMILES:
CC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N
1.Safety profiles of first-line therapies for metastatic non-squamous non-small-cell lung cancer.
Losanno T1, Gridelli C2. Expert Opin Drug Saf. 2016 Apr 12:1-15. [Epub ahead of print]
INTRODUCTION: Lung cancer still represents the leading cause of death for cancer. About the 70% of diagnosis are in advanced-stage. Non-small-cell lung cancer (NSCLC) represents the 85% of all diagnosed lung cancers and non-squamous histology represents the 40% of all NSCLC. First-line therapies increase survival, control symptoms and improve quality of life, compared with best supportive care. It is crucial to choose a treatment with a low impact on patient's life considering the related toxicities. Areas covered: Adverse events (AEs) of first-line therapies for non-squamous NSCLC are here reviewed and discussed, from evidences in clinical trials conducting to drugs approval. Expert opinion: For advanced disease, palliation and preserving patients QoL are still the primary goal of treatment. Therefore, differing toxicity profiles are often a deciding factor in first-line and also maintenance setting for non-squamous NSCLC. Special attention is necessary to renal function and drugs' nephrotoxicity.
2.Metastatic EML4-ALK fusion detected by circulating DNA genotyping in an EGFR-mutated NSCLC patient and successful management by adding ALK inhibitors: a case report.
Liang W1,2, He Q3,4, Chen Y5,6, Chuai S7, Yin W8,9, Wang W10,11, Peng G12,13, Zhou C14,15,16, He J17,18. BMC Cancer. 2016 Feb 5;16:62. doi: 10.1186/s12885-016-2088-5.
BACKGROUND: Rebiopsy is highly recommended to identify the mechanism of acquired resistance to EGFR-TKIs in advanced lung cancer. Recent advances in multiplex genotyping based on circulating tumor DNA (ctDNA) provide a strong and non-invasive alternative for detection of the resistance mechanism.
3.Re-Evaluating Progression in an Era of Progress: A Review of First- and Second-Line Treatment Options in Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer.
Castellanos EH1, Horn L2. Oncologist. 2016 Apr 6. pii: theoncologist.2015-0396. [Epub ahead of print]
: The advent of crizotinib, the first small molecule inhibitor against anaplastic lymphoma kinase (ALK), has led to impressive advances in the care of patients with advanced ALK-rearranged non-small cell lung cancer. The development of second-generation ALK inhibitors, starting with the recent U.S. Food and Drug Administration approval of ceritinib, promises to expand the therapeutic landscape for this cohort of patients. With increasing use of molecularly targeted therapy options, it has been observed that disease progression in patients receiving targeted agents has a heterogeneous biology, manifesting as either oligoprogressive or widely progressive disease, which may require development of innovative treatment strategies. This review discusses the first- and second-generation ALK inhibitors approved or in clinical development, as well as the novel challenges and approaches to disease progression in patients on targeted agents.
4.Crizotinib Response in a Late Relapse of ALK-positive Lung Adenocarcinoma.
Zito Marino F1, Morabito A, Gridelli C, Rocco G, Liguori G, De Rosa N, Botti G, Franco R. Appl Immunohistochem Mol Morphol. 2016 Mar 17. [Epub ahead of print]
Anaplastic lymphoma kinase (ALK) rearrangement is a therapeutic target in non-small cell lung cancer. To date, few reports have been provided related to ALK-rearranged late recurrence and sensitivity to the treatment with specific ALK inhibitors. We report a case of a 35-year-old man who underwent a right lower lobe lobectomy for lung adenocarcinoma, and treated with the platinum-based chemotherapy regimen. After 10 healthy years, he developed a lung nodule in the same site as the previous. Cytopathologic diagnosis was lung adenocarcinoma. Furthermore, the pulmonary nodule was considered a late recurrence in relation to the lymph node involvement, the same histotype and the site, ALK fluorescence in situ hybridization test and epidermal growth factor receptor analysis were performed on the formalin-fixed paraffin-embedded specimens of the previous resected tumor, because of inadequacity cytologic sample. Being positive for ALK rearrangement, the patient was treated with crizotinib with a good response.
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CAS 1374356-45-2 (S)-crizotinib

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