ALK inhibitor 1 - CAS 761436-81-1
Catalog number: 761436-81-1
Category: Inhibitor
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Molecular Formula:
C23H28BrN7O3S
Molecular Weight:
562.48
COA:
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Targets:
ALK
Description:
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
Purity:
>98%
Synonyms:
Benzenesulfonamide, 2-[[5-bromo-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-
MSDS:
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InChIKey:
FTSDLONCFCQDGA-UHFFFAOYSA-N
InChI:
InChI=1S/C23H28BrN7O3S/c1-25-35(32,33)21-7-5-4-6-19(21)27-22-17(24)15-26-23(29-22)28-18-9-8-16(14-20(18)34-3)31-12-10-30(2)11-13-31/h4-9,14-15,25H,10-13H2,1-3H3,(H2,26,27,28,29)
Canonical SMILES:
CNS(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Br)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC
1.Successful treatment of hepatic oligometastases with stereotactic ablative radiotherapy and radiofrequency ablation in an anaplastic lymphoma kinase fusion-positive lung cancer patient.
Weber B1, Liu M2, Sobkin P3, Morris SW4, Hout D4, van der Westhuizen N5, Tonseth RP6, Saltman DL7. J Med Radiat Sci. 2016 Mar;63(1):67-70. doi: 10.1002/jmrs.144. Epub 2015 Oct 3.
Local ablative therapy with stereotactic ablative radiotherapy may improve survival in oncogene-addicted lung cancer patients with extracranial oligometastatic disease treated with targeted therapies. There is limited data on the use of radiofrequency ablation (RFA) in this same setting. We present a case of an anaplastic lymphoma kinase (ALK)-positive lung cancer patient with hepatic oligometastatic progression who was successfully treated with both stereotactic ablative radiation and RFA while continuing with an ALK inhibitor.
2.Optimizing Treatment Risk and Benefit for Elderly Patients With Advanced Non-Small-Cell Lung Cancer: The Right Treatment for the Right Patient.
Presley CJ1, Gross CP1, Lilenbaum RC2. J Clin Oncol. 2016 May 1;34(13):1438-42. doi: 10.1200/JCO.2015.65.9599. Epub 2016 Mar 21.
The Oncology Grand Rounds series is designed to place original reports published in theJournal into clinical context. A case presentation is followed by a description of diagnostic and management challenges, a review of the relevant literature, and a summary of the authors' suggested management approaches. The goal of this series is to help readers better understand how to apply the results of key studies, including those published inJournal of Clinical Oncology, to patients seen in their own clinical practice.A 78-year-old woman with a 40-pack-year smoking history has been referred for treatment of advanced non-small-cell lung cancer. She presented with a persistent cough and worsening dyspnea on exertion. A chest x-ray followed by a chest computed tomography scan revealed a 3-cm right upper lobe mass along with a moderate-size pleural effusion. Pleural fluid cytology was positive for adenocarcinoma. A brain magnetic resonance imaging scan was negative.
3.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.
4.Elucidation of Resistance Mechanisms to Second-Generation ALK Inhibitors Alectinib and Ceritinib in Non-Small Cell Lung Cancer Cells.
Dong X1, Fernandez-Salas E2, Li E3, Wang S4. Neoplasia. 2016 Mar;18(3):162-71. doi: 10.1016/j.neo.2016.02.001.
Crizotinib is the first anaplastic lymphoma kinase (ALK) inhibitor to have been approved for the treatment of non-small cell lung cancer (NSCLC) harboring an ALK fusion gene, but it has been found that, in the clinic, patients develop resistance to it. Alectinib and ceritinib are second-generation ALK inhibitors which show remarkable clinical responses in both crizotinib-naive and crizotinib-resistant NSCLC patients harboring an ALK fusion gene. Despite their impressive activity, clinical resistance to alectinib and ceritinib has also emerged. In the current study, we elucidated the resistance mechanisms to these second-generation ALK inhibitors in the H3122 NSCLC cell line harboring the EML4-ALK variant 1 fusion in vitro. Prolonged treatment of the parental H3122 cells with alectinib and ceritinib led to two cell lines which are 10 times less sensitive to alectinib and ceritinib than the parental H3122 cell line. Although mutations of ALK in its kinase domain are a common resistance mechanism for crizotinib, we did not detect any ALK mutation in these resistant cell lines.
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CAS 761436-81-1 ALK inhibitor 1

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