货号	规格	价格	上海	北京	珠海	重庆	武汉
S81153-1mg买3赠1	99.60%	￥200.00 S81153-1mg ￥200.00 现货（买3赠1）	6 6	-	-	-	-
S81153-2mg买3赠1	99.60%	￥300.00 S81153-2mg ￥300.00 现货（买3赠1）	8 8	-	-	-	-
S81153-5mg买3赠1	99.60%	￥420.00 S81153-5mg ￥420.00 现货（买3赠1）	7 7	-	-	-	-
S81153-10mg买3赠1	99.60%	￥560.00 S81153-10mg ￥560.00 现货（买3赠1）	5 5	-	-	-	-
S81153-25mg买3赠1	99.60%	￥660.00 S81153-25mg ￥660.00 现货（买3赠1）	3 3	-	-	-	-
S81153-100mg买3赠1	≥99%	￥1640.00 S81153-100mg ￥1640.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.

靶点：

Aurora A:5 nM (IC50);Aurora B:4 nM (IC50);Aurora C:1 nM (IC50);p38MAPK; TyrosineKinases; AuroraKinase

体内研究：

AMG 900 exhibits significant antitumor activity in all 9 xenograft models tested (50%-97% TGI compared with the vehicle-treated control group, P<0.005, P<0.0005). Importantly, AMG 900 is active in the MES-SA-Dx5 (84% TGI, P<0.0001) and NCI-H460-PTX (66% TGI, P<0.0001) xenograft models that are resistant to either Docetaxel or Paclitaxel administered at their respective maximum tolerated doses. AMG 900 inhibits the activity of aurora-B in HCT116 tumors and suppresses the growth of multiple xenografts that represent diverse tumor types. Treatment with AMG 900 at 15 mg/kg significantly inhibits p-Histone H3 in the G2M cell population in mouse bone marrow (upper panel) and cytokeratin positive COLO 205 tumor (lower panel) compared with vehicle-treated controls. AMG 900 exhibits a low-to-moderate clearance and a small volume of distribution. Its terminal elimination half-life ranged from 0.6 to 2.4 h. AMG 900 is well-absorbed in fasted animals with an oral bioavailability of 31% to 107%. Food intake had an effect on rate (rats) or extent (dogs) of AMG 900 oral absorption

参考文献：

1. Payton M, et al. Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 2010, 70(23), 9846-9854. 2. Juan G, 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 Nov 4;12:307. 3. Huang L, et al. In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases. Xenobiotica. 2011 May;41(5):400-8.

溶解性：

DMSO : ≥ 50 mg/mL (99.29 mM)

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.986 ml	9.929 ml	19.858 ml
5 mM	0.397 ml	1.986 ml	3.972 ml
10 mM	0.199 ml	0.993 ml	1.986 ml
50 mM	0.04 ml	0.199 ml	0.397 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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