| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| V407853-1ml |
1ml |
现货  |
|
| 别名 | 伐利替尼 |
|---|---|
| 英文别名 | ARRY334543 | (R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Varlitinib |
| 生化机理 | Varlitinib (ARRY334543) 是一种选择性强效 ErbB1（表皮生长因子受体）和 ErbB2（HER2）抑制剂，IC50 分别为 7 nM 和 2 nM。第二阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 受体蛋白-酪氨酸激酶 erbB-2 抑制剂 |
| 产品介绍 |
Information Varlitinib (ARRY334543) is a selective and potentErbB1(EGFR)andErbB2(HER2)inhibitor withIC50of 7 nM and 2 nM, respectively. Phase 2. ARRY334543 behaves as a reversible ATP-competitive inhibitor with nanomolar potency (Ki=1 nM) both in vitro and in cell-based proliferation assays using A431 and BT-474 cells. ARRY334543 is an AKT pathway inhibitor in cells that contains active ErbB-2 receptors. ARRY334543 suppresses ErbB-2 and ErbB-1 phosphorylation in human cancer cells, such as BT-474 with IC50 of 43 nM) and A431 with IC50 of 36 nM) that overexpress ErbB-2 and ErbB-1, respectively. In vivo When dosed orally, ARRY334543 prevents growth of human tumor xenografts that overexpress ErbB-1 (A431) or ErbB-2 (MDA-MB-453) in a dose-dependent manner. In mouse xenograft models utilizing the EGFR overexpressing tumor line A431, ARRY334543 demonstrates significant dose related tumor growth prevention when administered orally, BID, for 21 days. ARRY334543 has very good in vivo and in vitro PK/ADME properties and has shown excellent activity in numerous mouse tumor xenograft models including epidermoid (A431), breast (BT-474, MDA-MB-453), non-small cell lung (H1650, A549, 292), colorectal (Lovo, HT-29) and gastric (N87) carcinoma models. In the BT-474 model, ARRY334543 demonstrates significant dose-related tumor growth inhibition (69% at 100 mg/kg/d and 98% at 200 mg/kg/d) with significant regressions at both dose levels. Excellent single agent activity for ARRY334543 in the SK-OV-3 ovarian carcinoma xenograft model as well as additive acitivity to trastuzumab in SK-OV-3, BT-474 and NCI-N87 models has been demonstrated. In the BT-474 model, ARRY334543 displays excellent additive activity and tolerability with docetaxel. cell lines： Concentrations： Incubation Time： Powder Purity:≥96% |
| IC50 | ErbB2, IC50: 2 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(OCC5=NC=CS5)C=C4)Cl |
| 分子量 | 466.94 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 51 mg/mL (200.59 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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