CAS NO: | 1050500-29-2 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Cas No. | 1050500-29-2 |
别名 | 艾力替尼; AST-1306 (TsOH) |
化学名 | N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide;4-methylbenzenesulfonic acid |
Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)O.C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl |
分子式 | C31H26ClFN4O5S |
分子量 | 621.08 |
溶解度 | DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | AST-1306 is a selective, irreversible inhibitor of ErbB2 and EGFR with IC50 values of 0.5nM and 3nM, respectively [1]. AST-1306 is designed and synthesized based on the chemical structure of lapatinib. The molecular docking method shows AST-1306 binds to the ATP-binding pocket of the kinases and form covalent bind with certain amino acids. AST-1306 can inhibit EGFR and ErbB2 in a cell-free assay with more than 3000-fold selectivity to other kinases. Besides the wild-type EGFR, AST-1306 also inhibits EGFR mutant T790M/L858R both in a cell-free assay and in HIH3T3 cells. The growth of the cells is suppressed by AST-1306 due to the inhibition of the phosphorylation of EGFR. It also occurs in some human cancer cells. Experiments have proved that AST-1306 notly inhibits the phosphorylation of EGFR and ErbB2 and subsequently decreases the downstream pathways of these kinases in A549 cells, Calu-3 cells and SK-OV-3 cells. Moreover, AST-1306 potently inhibits the tumor growth both in ErbB2-overexpressing xenograft models and FVB-2/Nneu transgenic mouse model [1]. References: |