| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408637-1ml |
1ml |
现货  |
|
| 英文别名 | (R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | TAK-733 |
| 生化机理 | TAK-733 是一种强效、选择性 MEK 异位点抑制剂，对 MEK1 的 IC50 值为 3.2 nM，对 Abl1、AKT3、c-RAF、CamK1、CDK2、c-Met 等均无活性。第 1 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 变构调节剂 |
| 作用机制 | 丝裂原活化蛋白激酶激酶 1 的异构调节剂 |
| 产品介绍 |
Information TAK-733 is a potent and selectiveMEKallosteric site inhibitor for MEK1 withIC50of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1. TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. In vivo TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. cell lines： Concentrations： Incubation Time： Powder Purity:≥96% |
| IC50 | MEK1, IC50: 3.2 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CN1C(=O)C(=C(NC2=CC=C(I)C=C2F)C3=C1N=CN(CC(O)CO)C3=O)F |
| 分子量 | 504.23 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 49 mg/mL (200.58 mM); Ethanol: 49 mg/mL (200.58 mM); Water: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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