ALK inhibitor 1 - CAS 761436-81-1
Catalog number: 761436-81-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
Publictions citing BOC Sciences Products
  • >> More
Benzenesulfonamide, 2-[[5-bromo-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related ALK Products

(CAS: 868612-83-3)

IN-1130 is a selective ALK5 inhibitor with >100 fold selectivity over p38α and a panel of 26 other serine/threonine and tyrosine kinases. It also inhibit phosph...

(CAS: 1357920-84-3)

Belizatinib is inhibitor of both anaplastic lymphoma kinase (ALK) and tropomyosin-related kinases (TRK). Belizatinib can bind to and inhibit both ALK and TRK ki...

CAS 761436-81-1 ALK inhibitor 1

ALK inhibitor 1
(CAS: 761436-81-1)

ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.

CAS 761438-38-4 ALK inhibitor 2

ALK inhibitor 2
(CAS: 761438-38-4)

ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.

CAS 356559-13-2 SB-505124 hydrochloride

SB-505124 hydrochloride
(CAS: 356559-13-2)

SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptor ALK5 and as well as being a selective inhibitor of ALK4 but with less pote...

CAS 1627503-67-6 LDN-214117

(CAS: 1627503-67-6)

LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. There are currently no effective therapi...

CAS 1256580-46-7 Alectinib

(CAS: 1256580-46-7)

Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing ...


BAY-754 is an ALK-1 inhibitor used as an anti-angiogenesis agent. It inhibited the eye vascular leakage in dose manner in mouse model.

Entrectinib (RXDX-101)
(CAS: 1108743-60-7)

Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.

CAS 1432597-26-6 LDN-212854

(CAS: 1432597-26-6)

LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2. LDN-212854 exhibits some selectivity for ALK2 in preference to other...

CAS 1415560-69-8 Crizotinib hydrochloride

Crizotinib hydrochloride
(CAS: 1415560-69-8)

Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is use...

CAS 1197958-12-5 AP-26113

(CAS: 1197958-12-5)

AP26113 is an orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with pote...

CAS 1032900-25-6 Ceritinib

(CAS: 1032900-25-6)

This active molecular is a selective inhibitor of ALK(anaplastic lymphoma kinase)which is a target found in NSCLC (metastatic non-small cell lung cancer). The I...

CAS 1356962-20-3 AZD-3463

(CAS: 1356962-20-3)

AZD-3463 is a potent ALK/IGF1R inhibitor with potential anticancer activity.

Brigatinib (AP-26113)
(CAS: 1197953-54-0)

Brigatinib, is an orally active, also known as AP-26113, potent and selective Dual ALK/EGFR inhibitor. AP26113 binds to and inhibits ALK kinase(ALK belongs to t...

CAS 1206711-16-1 DMH-1

(CAS: 1206711-16-1)

DMH-1 is a second-generation small molecule BMP inhibitor based on dorsomorphin. DMH-1 effectively inhibits the bone morphogenic protein (BMP) ALK2 receptor (IC...

CAS 1380575-43-8 LDK378 dihydrochloride

LDK378 dihydrochloride
(CAS: 1380575-43-8)

Ceritinib, also known as LDK378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 s...

CAS 761439-42-3 TAE684

(CAS: 761439-42-3)

NVP-TAE684 is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC(50) valu...

CAS 856692-39-2 CEP-14083

(CAS: 856692-39-2)

CEP-14083 is a ALK inhibitor. It has a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). CEP-14083 can also inhibit the insulin receptor at a ...

CAS 1116235-97-2 GSK1838705A

(CAS: 1116235-97-2)

GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively. GSK1838705A blocks ...

Chemical Structure

CAS 761436-81-1 ALK inhibitor 1

Quick Inquiry

Verification code

Featured Items