AST-1306 (Synonyms: AST1306; AST 1306) |
| カタログ番号GC11691 |
AST-1306 (AST-1306) は、経口活性で不可逆的な EGFR および ErbB2 阻害剤であり、IC50 はそれぞれ 0.5 および 3 nM です。 AST-1306 は、0.8 nM の IC50 で ErbB4 も阻害します。 AST-1306はアニリノキナゾリン化合物で、抗がん作用があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 897383-62-9
Sample solution is provided at 25 µL, 10mM.
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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]
Reference:
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.
Cell experiment: | Cells are seeded into 96-well plates and grown for 24 h. The cells are then treated with increasing concentrations of Allitinib (AST1306) and grown for a further 72 h. Cell proliferation is evaluated using the SRB (Sulforhodamine B) assay[1]. |
Animal experiment: | Mice: Mice are administered Allitinib (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. | |
| Cas No. | 897383-62-9 | SDF | |
| 同義語 | AST1306; AST 1306 | ||
| Chemical Name | N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide | ||
| Canonical SMILES | C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl | ||
| Formula | C24H18ClFN4O2 | M.Wt | 448.88 |
| 溶解度 | ≥ 22.45mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2278 mL | 11.1388 mL | 22.2777 mL |
| 5 mM | 0.4456 mL | 2.2278 mL | 4.4555 mL |
| 10 mM | 0.2228 mL | 1.1139 mL | 2.2278 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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