| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Allitinib tosylate
(formerly AST-1306; AST1306; AST 1306), the tosylate of Allitinib, is a selective and covalent/irreversible inhibitor of EGFR and ErbB2 with
potential anticancer activity.
| ln Vitro |
On the development of HIH3T3-EGFR T790M/L858R cells, AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) can have notable, concentration-dependent inhibitory effects [1]. In A549 cells, Calu-3 cells, and SK-OV-3 cells, AST1306 tosylate suppresses the activation of tyrosine kinases and downstream signaling pathways. In A549 cells, AST1306 tosylates in a dose-dependent manner and notably prevents EGF-induced EGFR phosphorylation [1]. Two tumor cells grown on soft agar can be significantly inhibited by AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM), with SK-OV-3 cells exhibiting far higher sensitivity than A549 cells [1]. Compared to other kinase families, AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000 times more selective for ErbB family kinases [1]. With an IC50 value of 12±2 nmol/L, AST1306 tosylate efficiently suppresses the EGFR T790M/L858R double mutant[1].
|
|---|---|
| ln Vivo |
Tumor growth in SK-OV-3 and Calu-3 xenograft models is significantly inhibited by AST1306 tosylate (AST-1306 (TsOH); oral; 25–100 mg/kg; twice daily; for 28 days [1].
|
| Cell Assay |
Cell Proliferation Assay [1]
Cell Types: NIH3T3 Parental and NIH3T3 Cell Tested Concentrations: 0.19, 0.39, 0.78, 1.56, 3.13, 6.25 μM Incubation Duration: 72 hrs (hours) Experimental Results: Significant concentration-dependent inhibition of EGFR on the growth of HIH3T3- T790M/L858R cells. Western Blot Analysis[1] Cell Types: A549 cells, Calu-3 cells and SK-OV-3 cells Tested Concentrations: 0.001, 0.01, 0.1, 1.0 μM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibition of tyrosine kinases and downstream signaling pathways activation. |
| Animal Protocol |
Animal/Disease Models: SK-OV-3 and Calu-3 tumor nude mice [1]
Doses: 25, 50, 100 mg/kg Route of Administration: po (po (oral gavage)) twice a day; lasted for 28 days. Experimental Results: Dramatically inhibited tumor growth. |
| 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.
|
| Molecular Formula |
C₃₁H₂₆CLFN₄O₅S
|
|---|---|
| Molecular Weight |
621.08
|
| CAS # |
1050500-29-2
|
| Related CAS # |
Allitinib;897383-62-9
|
| SMILES |
FC1=CC=CC(COC2=C(Cl)C=C(NC3=NC=NC4=C3C=C(NC(C=C)=O)C=C4)C=C2)=C1.O=S(C5=CC=C(C)C=C5)(O)=O
|
| Synonyms |
AST-1306 AST 1306AST1306
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~80.50 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6101 mL | 8.0505 mL | 16.1010 mL | |
| 5 mM | 0.3220 mL | 1.6101 mL | 3.2202 mL | |
| 10 mM | 0.1610 mL | 0.8050 mL | 1.6101 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
