897383-62-9 Usage
Uses
Different sources of media describe the Uses of 897383-62-9 differently. You can refer to the following data:
1. AST-1306 is a novel irreversible inhibitor of EGFR and ErbB4 with IC50 of 0.5 nM and 0.8 nM, respectively.
2. AST-1306 is a selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) 1 and 2. Studies show that AST-1306 inhibited the enzymatic activities of wild-type EGF) and ErbB2 as well
as EGFR resistant mutant in both cell-free and cell-based systems. AST-1306 was more effective in inhibiting tumors with ErbB2-overexpressing cells than EGFR-overexpressing tumor.
Biological Activity
ast1306 is a novel inhibitor of egfr and her2 (ic50 = 0.5 nm and 3 nm respectively)egfr (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. the receptor activation leads to dimerization and tyrosine autophosphorylation. it induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc. her2 is a member of the epidermal growth factor and is associated with breast and ovarian cancers.ast1306 selectively blocked egfr and her2 kinase activities in a cell-free assay. the tyrosine kinase activity of egfr mutant t790m/l858r was also inhibited by ast1306 in intact cell and cell-free assays. in addition, ast1306 attenuated the egfr and her2 phosphorylation and downstream substrates. [1]in erbb2-overexpressing xenograft and fvb-2/nneu transgenic mouse model, ast1306 potently inhibited tumor growth. in sk-ov-3 xenograft model, ast1306 caused a quick and long-lasting (≥24h) inhibition of egfr and her2. [1]
references
1. xie h, lin l, tong l et al. ast1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. plos one. 2011;6(7):e21487.
Check Digit Verification of cas no
The CAS Registry Mumber 897383-62-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,9,7,3,8 and 3 respectively; the second part has 2 digits, 6 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 897383-62:
(8*8)+(7*9)+(6*7)+(5*3)+(4*8)+(3*3)+(2*6)+(1*2)=239
239 % 10 = 9
So 897383-62-9 is a valid CAS Registry Number.
InChI:InChI=1S/C24H18ClFN4O2/c1-2-23(31)29-17-6-8-21-19(11-17)24(28-14-27-21)30-18-7-9-22(20(25)12-18)32-13-15-4-3-5-16(26)10-15/h2-12,14H,1,13H2,(H,29,31)(H,27,28,30)
897383-62-9Relevant articles and documents
The polymorph forms of 4-anilinoquinazoline derivatives, the preparation methods and uses thereof
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, (2012/01/14)
The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods
Compositions Comprising Quinazoline Derivatives, Preparation Methods and Uses Thereof
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, (2011/05/16)
The present invention provides a pharmaceutical composition, useful for the treatment of diseases characterized by abnormal PTKs activity of erbB family in a mammal, comprising pharmaceutically acceptable salts of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phen
SALTS OF 4-ANILINE QUINAZOLINE DERIVATIVE
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Page/Page column 4-5, (2010/07/08)
The present invention relates to salt forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide, methods for preparation thereof, pharmaceutical compositions comprising the same and their use thereof. The salt forms of the pre
