ChemicalBook > CAS DataBase List > AST-1306

AST-1306

Product Name
AST-1306
CAS No.
897383-62-9
Chemical Name
AST-1306
Synonyms
CS-590;ALS 1306;AST-1306;Allitinib;AST-1306 ，E0822;Allitinib (AST1306);Allitinib, 10 mM in DMSO;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
CBNumber
CB82620006
Molecular Formula
C24H18ClFN4O2
Formula Weight
448.88
MOL File
897383-62-9.mol
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AST-1306 Property

Boiling point:
655℃
Density 
1.395
Flash point:
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
InChIKey
MVZGYPSXNDCANY-UHFFFAOYSA-N
SMILES
C(NC1C=CC2C(C=1)=C(NC1=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C1)N=CN=2)(=O)C=C
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
A790045
Product name
AST-1306
Packaging
200mg
Price
$2470
Updated
2021/12/16
ApexBio Technology
Product number
A8367
Product name
AST-1306
Packaging
5mg
Price
$176
Updated
2021/12/16
ApexBio Technology
Product number
A8367
Product name
AST-1306
Packaging
10mM(in 1mL DMSO)
Price
$250
Updated
2021/12/16
ApexBio Technology
Product number
A8367
Product name
AST-1306
Packaging
10mg
Price
$308
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
KIN0001438
Product name
N-[4-[[3-CHLORO-4-[(3-FLUORO PHENYL)-METHOXY]-PHENYL]-AMINO]-6-QUINAZOLINYL]-2-PROPENAMIDE
Purity
95.00%
Packaging
5MG
Price
$534.6
Updated
2021/12/16
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AST-1306 Chemical Properties,Usage,Production

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]

in vivo

AST1306 (AST-1306; p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models[1].

Animal Model:Nude mice with SK-OV-3 and Calu-3 tumors[1]
Dosage:25, 50, 100 mg/kg
Administration:p.o; twice daily; for 28 days
Result:Caused a dramatic suppression of tumor growth.

IC 50

EGFR: 0.5 nM (IC50); EGFRL858R/T790M: 12 nM (IC50); ErbB2: 3 nM (IC50); ErbB4: 0.8 nM (IC50)

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.

AST-1306 Preparation Products And Raw materials

Raw materials

Preparation Products

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AST-1306 Suppliers

Canada 1 China 88 India 1 United States 18 Global 108
Chuzhou KeMail Chemical Technology Co., Ltd
Tel
0550-5196001 15000891977
Fax
0550-5196001
Email
wj520wjxby@126.com
Country
China
ProdList
1944
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
China Kouting Group Limited
Tel
+86 (21) 5811-6473 5811-6475
Fax
+86 (21) 6129-4103
Email
sales@koutingchina.com
Country
China
ProdList
496
Advantage
60
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
25002
Advantage
65
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4720
Advantage
55
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View Lastest Price from AST-1306 manufacturers

Career Henan Chemical Co
Product
AST-1306 897383-62-9
Price
US $9.80/KG
Min. Order
1g
Purity
≥99%
Supply Ability
100kg
Release date
2020-01-12

897383-62-9, AST-1306Related Search:


  • AST-1306
  • ALS 1306
  • 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
  • Allitinib (AST1306)
  • Allitinib
  • CS-590
  • N-(4-(4-(3-fluorobenzyloxy)-3-chlorophenylamino)quinazolin-6-yl)acrylamide
  • 2-Propenamide, N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-
  • anilino-quinazoline,Inhibitor,anti-cancer,Epidermal growth factor receptor,ALS1306,Allitinib,Irreversible,HER1,inhibit,AST1306,AST 1306,ALS-1306,ErbB-1,EGFR
  • Allitinib, 10 mM in DMSO
  • AST-1306 ，E0822
  • 897383-62-9