AST-1306

Modify Date: 2024-01-05 17:47:52

AST-1306 Structure
AST-1306 structure
Common Name AST-1306
CAS Number 897383-62-9 Molecular Weight 448.877
Density 1.4±0.1 g/cm3 Boiling Point 655.0±55.0 °C at 760 mmHg
Molecular Formula C24H18ClFN4O2 Melting Point N/A
MSDS N/A Flash Point 349.9±31.5 °C

 Use of AST-1306


AST1306 is a selective, irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively.

 Names

Name N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide
Synonym More Synonyms

 AST-1306 Biological Activity

Description AST1306 is a selective, irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively.
Related Catalog
Target

EGFR:0.5 nM (IC50)

ErbB2:3 nM (IC50)

EGFRL858R/T790M:12 nM (IC50)

In Vitro AST1306 induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells. In addition, AST1306 effectively inhibits EGFR phosphorylation in HIH3T3-EGFR T790M/L858R cells. AST1306 inhibits the growth of NCI-H1975 cells that harbor the EGFR T790M/L858R mutation in a concentration-dependent manner, and blocks phosphorylation of EGFR and downstream pathways as well. AST1306 inhibits the phosphorylation of EGFR and ErbB2, and downstream signaling in human cancer cells. AST1306 inhibits the proliferation of human cancer cells, with ErbB2-overexpressing cells exhibiting more sensitivity[1].
In Vivo AST1306 potently suppresses tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/Nneu transgenic breast cancer mouse models, but weakly inhibits the growth of EGFR-overexpressing tumor xenografts. Tumor growth inhibition induced by a single dose of AST1306 in the SK-OV-3 xenograft model is accompanied by a rapid (within 2 h) and sustained (≥24 h) inhibition of both EGFR and ErbB2, consistent with an irreversible inhibition mechanism[1].
Cell Assay Cells are seeded into 96-well plates and grown for 24 h. The cells are then treated with increasing concentrations of AST1306 and grown for a further 72 h. Cell proliferation is evaluated using the SRB (Sulforhodamine B) assay[1].
Animal Admin Mice: Mice are administered AST1306 at dosage of 100, 50 and 25 mg/kg twice daily and treated with lapatinib (50 mg/kg) as comparison. Tumors are measured twice a week in two dimensions, using a caliper, and the tumor volume is calculated according to the formula L×W×W/2[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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 655.0±55.0 °C at 760 mmHg
Molecular Formula C24H18ClFN4O2
Molecular Weight 448.877
Flash Point 349.9±31.5 °C
Exact Mass 448.110229
PSA 79.63000
LogP 5.02
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.700
Storage condition 2-8℃

 Synthetic Route

~64%

AST-1306 Structure

AST-1306

CAS#:897383-62-9

Literature: EP1990337 A1, ; Page/Page column 9 ;

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AST-1306 Structure

AST-1306

CAS#:897383-62-9

Literature: EP2292234 A1, ;

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AST-1306 Structure

AST-1306

CAS#:897383-62-9

Literature: EP2292234 A1, ;

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AST-1306 Structure

AST-1306

CAS#:897383-62-9

Literature: EP2292234 A1, ;

 Synonyms

2-Propenamide, N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-
cc-669
AST 1306
N-[4-({3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}amino)-6-quinazolinyl]acrylamide
QCR-149
AST-1306
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