897016-82-9 Usage
Uses
A synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase inhibitor with an IC50 of average 72 nM.
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 articles and documents
Synthesis method of tebuterin
-
Paragraph 0024-0026; 0030-0031, (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
COMPOSITIONS AND METHODS FOR THE PREVENTION AND TREATMENT OF CANCER
-
, (2017/09/05)
The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.
COMPOSITION AND METHODS FOR MODULATING A KINASE CASCADE
-
Page/Page column 62, (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.
