| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408612-1ml |
1ml |
现货  |
|
| 英文别名 | AST-6 | 2-Propenamide, N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-, 4-methylbenzenesulfonate (1:1) |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Allitinib (AST-1306) |
| 生化机理 | 阿利替尼（AST-1306，AST-6）是一种新型的表皮生长因子受体（EGFR）和表皮生长因子受体（ErbB2）不可逆抑制剂，IC50 为 0.5 nM 和 3 nM，对突变的表皮生长因子受体（EGFR）T790M/L858R 也有效，对表达 ErbB2 的细胞更有效，对 ErbB 家族的选择性是其他激酶的 3000 倍。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
AST-1306 TsOH是一种新型，不可逆的EGFR和ErbB2抑制剂，IC50分别为0.5 nM和3 nM，对突变型EGFR T790M/L858R也有效，作用于过表达ErbB2的细胞更有效，作用于ErbB家族比作用于其他激酶选择性高3000倍。A potent and selective inhibitor of EGFR phosphorylation. Information Allitinib (AST-1306, AST-6) is a novel irreversible inhibitor ofEGFRandErbB2withIC50of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases. AST-1306 also ErB2 and EGFR T790M/L858R double mutant. AST-1306 is approximately 500-fold more potent than lapatinib and more than 3000-fold selective for ErbB family kinases over other kinase families including PDGFR, KDR and c-Met. AST-1306 might covalently bind to specific amino acid residues of EGFR and ErbB2. AST-1306 acts in a concentration dependent manner to significantly inhibit the growth of HIH3T3-EGFR T790M/L858R cells. AST-1306 effectively suppresses EGFR phosphorylation in HIH3T3-EGFR T790M/L858R cells. Moreover, AST-1306 blocks the growth of NCI-H1975 cells that harbor the EGFR T790M/L858R mutation in a concentration-dependent manner. AST-1306 blocks phosphorylation of EGFR and downstream pathways as well. In addition, AST-1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells. AST-1306 inhibits the phosphorylation of EGFR and ErbB2, and downstream signaling in human cancer cells including A549 cells, Calu-3 cells and SK-OV-3 cells. In vivo Twice daily oral administration of AST-1306 gives rise to a dramatic prevention of tumor growth in SK-OV-3 and Calu-3 xenograft models. In SK-OV-3 models, tumors nearly disappears after treatment with AST-1306 for 7 days. In contrast, AST-1306 only slightly inhibits the growth of tumor in HO-8910 and A549 xenograft models. Therefore, the antitumor efficacy of AST-1306 is greater in ErbB2-overexpressing tumor models than in models expressing low levels of ErbB2. AST-1306 is well tolerated. Lapatinib displays antitumor activity in these ErbB2-overexpressing tumor models, but AST-1306 is more efficacious than lapatinib in the SK-OV-3 xenograft tumor model when given at the same dose and schedule. In addition, oral administration of AST-1306 twice daily for 3 weeks dramatically suppresses the growth of tumor in the FVB-2/Nneu models. After treatment for 11 days, tumors almost completely disappears. The body weights of the mice reduces by less than 20% during treatment. cell lines： Concentrations：0.001-1 μM Incubation Time：72 hours Powder Purity:≥99% |
| Isomeric 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 |
|---|---|
| 分子量 | 621.08 |
| Reaxy-Rn | 20392877 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20392877&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 2 mg/mL (7.86 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
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