897016-82-9 Usage
Uses
Used in Pharmaceutical Industry:
KX2-391 is used as a therapeutic agent for the treatment of various diseases and conditions, particularly those involving abnormal cell growth or signaling pathways. Its ability to inhibit Src tyrosine kinase makes it a promising candidate for targeting cancer cells and potentially other pathologies where this enzyme plays a crucial role.
Used in Cancer Research:
KX2-391 is used as a research tool for studying the role of Src tyrosine kinase in cancer development and progression. Its non-ATP competitive nature allows for the investigation of different mechanisms of action and potential synergistic effects with other drugs in the development of novel cancer therapies.
Used in Drug Development:
KX2-391 is used as a lead compound in the development of new drugs targeting Src tyrosine kinase. Its oral bioavailability and non-ATP competitive mechanism make it a valuable starting point for the design and optimization of more potent and selective inhibitors for clinical use.
Biological Activity
kx2-391 is a highly selective inhibitor of src kinase with ic50 value of 20nm [1].kx2-391 is a non-atp competitive inhibitor of src. it is the first inhibitor that targets src kinase within the substrate binding site. kx2-391 inhibits src catalyzed trans-phosphorylation of fak, shc, paxillin as well as src kinase autophosphorylation. kx2-391 has no effects on pdgfr, egfr, jak1, jak2 and lck demonstrating it as a selective inhibitor. it is also found to be an inhibitor of tubulin polymerization through binding to the unique confirmation on heterodimeric tubulin. in cellular assays, kx2-391 shows growth inhibition in nih3t3/c-src527f cells and syf/c-src527f cells with gi50 values of 23nm and 39nm, respectively [1, 2].since src acts as a regulator in cell proliferation survival, motility and invasiveness, kx2-391 is potent against a variety of solid tumors and many leukemia tumors. it is shown to inhibit primary tumor growth and to suppress metastasis [2].
references
[1] fallah-tafti a, foroumadi a, tiwari r, et al. thiazolyl n-benzyl-substituted acetamide derivatives: synthesis, src kinase inhibitory and anticancer activities. european journal of medicinal chemistry, 2011, 46(10): 4853-4858.[2] naing a, cohen r, dy g k, et al. a phase i trial of kx2-391, a novel non-atp competitive substrate-pocket-directed src inhibitor, in patients with advanced malignancies. investigational new drugs, 2013, 31(4): 967-973.
Check Digit Verification of cas no
The CAS Registry Mumber 897016-82-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,9,7,0,1 and 6 respectively; the second part has 2 digits, 8 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 897016-82:
(8*8)+(7*9)+(6*7)+(5*0)+(4*1)+(3*6)+(2*8)+(1*2)=209
209 % 10 = 9
So 897016-82-9 is a valid CAS Registry Number.
897016-82-9Relevant academic research and scientific papers
Synthesis method of tebuterin
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, (2021/09/08)
The invention belongs to the technical field of synthesis of pharmaceutical compounds, and particularly discloses a synthesis method of tebuterin. 2-5 -dibromopyridine is taken as a raw material, and the compound 2 is obtained by reacting with ethyl bromo
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)
Smolinski, Michael P.,Bu, Yahao,Clements, James,Gelman, Irwin H.,Hegab, Taher,Cutler, David L.,Fang, Jane W. S.,Fetterly, Gerald,Kwan, Rudolf,Barnett, Allen,Lau, Johnson Y. N.,Hangauer, David G.
, p. 4704 - 4719 (2018/06/20)
The discovery of potent, peptide site directed, tyrosine kinase inhibitors has remained an elusive goal. Herein we describe the discovery of two such clinical candidates that inhibit the tyrosine kinase Src. Compound 1 is a phase 3 clinical trial candidat
COMPOSITIONS AND METHODS FOR THE PREVENTION AND TREATMENT OF CANCER
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Paragraph 0121, (2017/09/05)
The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.
PHARMACEUTICAL COMPOSITIONS FOR MODULATING A KINASE CASCADE AND METHODS OF USE THEREOF
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Page/Page column 54; 56; 62; 67-68; 72-73, (2009/05/28)
The invention relates to a pharmaceutical composition comprising 2-(5-(4-(2- mopholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
COMPOSITION AND METHODS FOR MODULATING A KINASE CASCADE
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Page/Page column 77-78; 83, (2008/12/07)
The invention relates to compositions of N-benzyl-2-(5-(4-(2- morpholinoethoxy)phenyl)pyridin-2-yl)acetamide (KX2-391) and methods for modulating one or more components of a kinase cascade.
Compositions and methods of treating cell proliferation disorders
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Page/Page column 84, (2008/06/13)
The invention relates to compounds and methods for treating cell proliferation disorders.
