| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Avitinib maleate dihydrate (AC0010; 0.13 nM-2 μM; 2 h) selectively inhibits mutant EGFR phosphorylation in NCI-H1975 and NIH/3T3_TC32T8 cells with IC50 values of 7.3 and 2.8 nM, respectively, which are approximately 115-fold and 298-fold more sensitive than the inhibition of wild-type EGFR in A431. Avitinib maleate dihydrate potently inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells with a 65-fold selectivity for NCI-H1975 cells over A431 cells. In addition to inhibiting EGFR-Tyr1068 phosphorylation, Avitinib maleate dihydrate also inhibits phosphorylation of downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells [1].
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|---|---|
| ln Vivo |
Avitinib maleate dihydrate (AC0010; 12.5-500 mg/kg; oral; once daily; for 14 days) has long-term inhibition of EGFR mutant tumor growth in xenograft models, but not wild-type EGFR tumor growth [1].
|
| References |
|
| Molecular Formula |
C30H34FN7O8
|
|---|---|
| Molecular Weight |
639.63
|
| CAS # |
1822357-78-7
|
| Related CAS # |
Avitinib;1557267-42-1;Avitinib maleate;1557268-88-8
|
| SMILES |
FC1C=C(C=CC=1N1CCN(C)CC1)NC1N=C(C2C=CNC=2N=1)OC1C=CC=C(C=1)NC(C=C)=O.OC(/C=C\C(=O)O)=O.O.O
|
| Synonyms |
Abivertinib maleate dihydrate; AC0010 maleate dihydrate
|
| 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)
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5634 mL | 7.8170 mL | 15.6340 mL | |
| 5 mM | 0.3127 mL | 1.5634 mL | 3.1268 mL | |
| 10 mM | 0.1563 mL | 0.7817 mL | 1.5634 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.
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