| Identification | Back Directory | [Name]
AST-1306 | [CAS]
897383-62-9 | [Synonyms]
CS-590
AST-1306
ALS 1306
Allitinib
Allitinib (AST1306)
N-(4-(4-(3-fluorobenzyloxy)-3-chlorophenylamino)quinazolin-6-yl)acrylamide
N-[4-[[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino]quinazolin-6-yl]acrylamide
N-[4-[[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-2-propenamide
2-Propenamide, N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]- | [Molecular Formula]
C24H18ClFN4O2 | [MDL Number]
MFCD17169993 | [MOL File]
897383-62-9.mol | [Molecular Weight]
448.88 |
| Chemical Properties | Back Directory | [Boiling point ]
655℃ | [density ]
1.395 | [Fp ]
350℃ | [storage temp. ]
Store at -20°C | [solubility ]
≥22.45 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid | [pka]
12.16±0.43(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
AST-1306 is a novel irreversible inhibitor of EGFR and ErbB4 with IC50 of 0.5 nM and 0.8 nM, respectively. | [Uses]
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. | [Definition]
ChEBI: N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-6-quinazolinyl]-2-propenamide is a member of quinazolines. | [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. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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