-
生物活性
PD184352 (also known as CI-1040), a benzhydroxamate derivative, is a potent and highly selective MEK1/2, two members of the family of MAPKKs, inhibitor that inhibits purified MEK1 with IC50 of 17 nM in a non-ATP and non-ERK1/2 competitive manner.
-
体外研究
-
体内研究
30% PEG400+0.5% Tween80+5% Propylene glycol, pH 9
-
激酶实验
-
细胞实验
0.1-10 μM
-
动物实验
150 mg/kg 口服，一天两次
-
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
|
例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
-
参考文献
[1] Sebolt-Leopold JS, et al. Nat Med, 1999, 5(7), 810-816.
[2] Steensma, D.P., et al. 2003. Haematologica. 88: 1072-1074.
[3] Klein, P.J., et al. 2006. Neoplasia. 8: 1-8.
[4] VanBrocklin, M.W., et al. 2009. Cancer Res. 69: 1985-1994.
[5] Allen et al (2003) CI-1040 (PD184252), a targeted signal transduction inhibitor of MEK (MAPKK). Semin.Oncol. 30 105.
[6] McDaid et al (2005) Enhancement of the therapeutic efficacy of taxol by the mitogen-activated protein kinase kinase inhibitor CI-1040 in nude mice bearing human heterotransplants. Cancer Res. 65 2854.
[7] Solit et al (2006) BRAF mutation predicts sensitivity to MEK inhibition. Nature 439 358.
分子式
C17H14ClF2IN2O2 |
分子量
478.67 |
CAS号
212631-79-3 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
95 mg/mL |
Water
<1 mg/mL |
Ethanol
15 mg/mL |
体内溶解度
-
Clinical Trial Information ( data from http://clinicaltrials.gov )
| NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
| NCT00033384 | Breast Cancer|Colorectal Cancer|Lung Cancer|Pancreatic Cancer | Drug: CI-1040 | University of Alabama at Birmingham|National Cancer Institute (NCI) | Phase 2 | 2002-02-01 | 2013-04-10 |
| NCT00034827 | Colorectal Neoplasms|Breast Neoplasms|Carcinoma, Non-Small-Cell Lung|Pancreatic Neoplasms | Drug: CI-1040 | Pfizer | Phase 2 | 2002-01-01 | 2007-05-03 |
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
-
相关化合物库
-
使用AMQUAR产品发表文献后请联系我们
