| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S408594-1ml |
1ml |
现货  |
|
| 英文别名 | N-(5-chlorobenzo[d][1,3]dioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Saracatinib (AZD0530) |
| 生化机理 | 沙拉卡替尼（AZD0530）是一种强效的 Src 抑制剂，在无细胞实验中的 IC50 为 2.7 nM，对 c-Yes、Fyn、Lyn、Blk、Fgr 和 Lck 均有效；对 Abl 和表皮生长因子受体（L858R 和 L861Q）的活性较低。Saracatinib 可诱导自噬。2/3期 |
| 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 | 酪氨酸蛋白激酶 SRC 抑制剂 |
| 产品介绍 |
Saracatinib (AZD0530)是一种有效的Src抑制剂，IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck等也有活性；但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。 Information Saracatinib (AZD0530) is a potentSrcinhibitor withIC50of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib inducesautophagy. Phase 2/3. Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. Saracatinib sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. Saracatinib significantly impairs the invasion of HT1080 cells through a 3-dimensional collagen matrix and completely inhibits EGF-induced cell scattering in NBT-II bladder cancer cells. Saracatinib potent inhibits Src activation in DU145 and PC3 cells, which through inhibition of Y419 phosphorylation. Saracatinib inhibits the growth of prostate cancer including PC3, DU145, CWR22Rv1 and LNCaP, while Saracatinib shows low activity in LAPC-4, PZ-HPV7 and RWPE-1 cells. Saracatinib induces cell cycle arrest at G1/S but not caspase 3 cleavages. Saracatinib also significantly inhibits DU145 and PC3 migration in the Boyden chamber. Saracatinib gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells. Saracatinib inhibits osteoclast in activity, resorption and formation. Saracatinib also reversibly prevents osteoclast precursor migration. In vivo Saracatinib shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily). cell lines： Concentrations：62.5 nM - 16 mM Incubation Time：1, 3 and 5 days Powder Purity:≥98% |
| IC50 | EGFR, IC50: 66 nM; EGFR (L858R), IC50: 5 nM; EGFR (L861Q), IC50: 4 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CN1CCN(CCOC2=CC(=C3C(=NC=NC3=C2)NC4=C(Cl)C=CC5=C4OCO5)OC6CCOCC6)CC1 |
| 分子量 | 542.03 |
| 溶解性 | Solubility (25°C) In vitro |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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