VIP会员
N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺
生物活性靶点体外研究体内研究 用途与合成方法 MSDS N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺价格(试剂级) 上下游产品信息
| 中文名称 | N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺 |
|---|---|
| 中文同义词 | N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺;阿贝卡尔杂质3;阿贝卡尔杂质1;N-(2-((1S,4R)-6-((4-(环丁基氨基)-5-(三氟甲基)嘧啶-2-基)氨基)-1,2,3,4-四氢-1,4-EPIMINO萘-9-基)-2-氧代乙基)乙酰胺;PF03814735|||INHIBIT|||PF-03814735;PF-03814735,AURORA激酶A和B抑制剂 |
| 英文名称 | PF-03814735 |
| 英文同义词 | PF-03814735;N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]acetamide;Acetamide, N-[2-[(1S,4R)-6-[[4-(cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-;RYYNGWLOYLRZLK-RBUKOAKNSA-N;CS-240;PF-03814735 USP/EP/BP;Abecarnil Impurity 3;PF-03814735 PF03814735 |
| CAS号 | 942487-16-3 |
| 分子式 | C23H25F3N6O2 |
| 分子量 | 474.48 |
| EINECS号 | |
| 相关类别 | 细胞周期;Inhibitor |
| Mol文件 | 942487-16-3.mol |
| 结构式 | ![N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺 结构式](https://yunshiji.oss-cn-shenzhen.aliyuncs.com/202410/29/1000578118800000199.gif) |
N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺 性质
| 熔点 | 181-183°C |
|---|---|
| 密度 | 1.443 |
| 储存条件 | -20°C |
| 溶解度 | 在DMSO中的溶解度为20mg/mL，澄清 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 15.02±0.46(Predicted) |
| 颜色 | 白色至米色 |
N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺 用途与合成方法
生物活性
PF-03814735是有效，有口服性，ATP 竞争性的，可逆的极光激酶A和B (aurora A/B) 的抑制剂，IC50值分别为0.8和5 nM。
靶点
Aurora 1 0.8 nM (IC 50) | Aurora 2 5 nM (IC 50) | Flt-1 10 nM (IC 50) | FAK 22 nM (IC 50) | TrkA 30 nM (IC 50) | Met 100 nM (IC 50) | FGFR1 100 nM (IC 50) |
体外研究
In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells. Small cell lung cancer (SCLC) and, to a lesser extent, colon cancer lines are very sensitive to PF-03814735. The status of the Myc gene family and retinoblastoma pathway members significantly correlates with the efficacy of PF-03814735.
体内研究
Once-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition. PF-03814735 is much more effective in NCI-H82 xenografts when administered on a weekly dosing schedule at 80 mg/kg compared with a daily schedule at 15 mg/kg. PF-03814735 delayed growth by 23.5 days on the weekly schedule, which corresponds to 0.9 logs of net cell kill during the course of treatment.
安全信息
| WGK Germany | 3 |
|---|
MSDS信息
N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-14574 | PF-03814735 | 1 mg | 569元 | |
| 2024/08/19 | HY-14574 | N-[2-[(1S,4R)-6-[[4-(环丁基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1,2,3,4-四氢萘-1,4-亚氨-9-基]-2-氧代乙基]乙酰胺 PF-03814735 | 942487-16-3 | 5 mg | 1252元 |
粤公网安备44196802000105号
400-6226-992