Lestaurtinib (CEP-701) 是一种具有口服活性和选择性的 RPTKs（受体蛋白酪氨酸激酶）抑制剂，竞争性抑制 ATP 与 TrkA/B/C 结构域的结合。 Lestaurtinib 抑制 RPTKs 磷酸化，对 FLT3、TrkA 和 JAK2 的 IC50 分别为 2、25 和 0.9 nM。 Lestaurtinib 诱导细胞凋亡和周期阻滞，也可以抑制肿瘤的生长。
| Cas No. | 111358-88-4 |
| 别名 | 来他替尼; CEP-701; KT-5555 |
| 化学名 | (5S,6S,8R)-6-hydroxy-6-(hydroxymethyl)-5-methyl-7,8,14,15-tetrahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacen-13(6H)-one |
| Canonical SMILES | O=C(NC1)C2=C1C(C(C=CC=C3)=C3N45)=C4C(N6[C@@H]7O[C@@]5(C)[C@](CO)(O)C7)=C2C8=C6C=CC=C8 |
| 分子式 | C25H21N3O4 |
| 分子量 | 439.46 |
| 溶解度 | DMF: 5 mg/ml,DMF:PBS (pH 7.2) (1:20): 0.05 mg/ml,DMSO: 3 mg/ml |
| 储存条件 | -20°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Potent JAK2, FLT3 and TrkA inhibitor (IC50values are 0.9, 3 and < 25 nM respectively) that prevents STAT5 phosphorylation (IC50= 20 - 30 nM). Exhibits antiproliferative activityin vitro(IC50= 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disordersin vivo. |
m.cnreagent.com