| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T408307-1ml |
1ml |
现货  |
|
| 英文别名 | 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine |
|---|---|
| 规格或纯度 | Moligand™, 2mM in DMSO |
| 英文名称 | TAE684 (NVP-TAE684) |
| 生化机理 | TAE684（NVP-TAE684）是一种强效的选择性 ALK 抑制剂，在无细胞实验中的 IC50 为 3 nM，对 ALK 的敏感性是 InsR 的 100 倍。TAE684 (NVP-TAE684) 可诱导细胞周期停滞和细胞凋亡。 |
| 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 | ALK 受体酪氨酸激酶抑制剂 |
| 产品介绍 |
TAE684 (NVP-TAE684)是一种有效的，选择性的ALK抑制剂，IC50为3 nM，作用于ALK比作用于InsR选择性高100倍。A selective NPM-ALK phosphorylation inhibitor which also inhibits ALK and LRRK2 Kinase Information TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis . TAE684 does not exhibit significant cross-reactivity against other kinases. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for TAE684. TAE684 treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines. TAE684 markedly overcomes Crizotinib-resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis. Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM. In vivo After 4 weeks of treatment with TAE684 at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. TAE684 treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression. TAE684 also shows impressive antitumor activity against H3122 CR xenograft tumors. Furthermore, treatment with TAE684 improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q, whereas Crizotinib has little effect on either phenotype. cell lines： Concentrations：1 nM-10 μM Incubation Time：2–3 days Powder Purity:≥97% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC |
| PubChem CID | 16038120 |
| 分子量 | 614.2 |
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