-
生物活性
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.
-
体外研究
-
体内研究
-
激酶实验
-
细胞实验
0.5，5.0，50 nM
-
动物实验
3.75，7.5，或15 mg/kg 口服给药
-
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] Payton M, et al, Cancer Res, 2010, 70(23), 9846-9854.
[2] Channing J Paller,et al. Combining the pan-aurora kinase inhibitor AMG 900 with histone deacetylase inhibitors enhances antitumor activity in prostate cancer. Cancer Med. 2014 Oct; 3(5): 1322–1335. Published online 2014 Jul 3. doi: 10.1002/cam4.289.
[3] Gloria Juan,et al. AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues. J Transl Med. 2014; 12: 307. Published online 2014 Nov 4. doi: 10.1186/s12967-014-0307-x.
分子式
C28H21N7OS |
分子量
503.58 |
CAS号
945595-80-2 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
100 mg/mL |
Water
<1 mg/mL |
Ethanol
<1 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 |
| NCT00858377 | Advanced Malignancy|Advanced Solid Tumors|Cancer|Solid Tumors|Tumors | Drug: Arm 1- Dose Escalation|Drug: Arm 1- Dose Expansion | Amgen | Phase 1 | 2009-08-01 | 2017-02-01 |
| NCT01380756 | Cancer|Hematologic Malignancies|Leukemia|Myeloid Leukemia | Drug: Arm 1- Dose Escalation|Drug: Arm 2- Dose Expansion | Amgen | Phase 1 | 2011-07-01 | 2015-02-18 |
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
