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AMG 900

目录号: PL13940 纯度: ≥99%

AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂，作用于 Aurora A，B 和 C，IC50 分别为 5 nM，4 nM 和 1 nM。

CAS No. :945595-80-2

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中文名称	AMG 900
中文别名	AMG900 抑制剂;N-[4-[[3-(2-氨基-4-嘧啶基)-2-吡啶基]氧基]苯基]-4-(4-甲基-2-噻吩基)-1-酞嗪胺;莪术醇.姜黄醇
英文名称	AMG 900
英文别名	AMG900;AMG-900;N-(4-((3-(2-aminopyrimidin-4-yl)pyridin-2-yl)oxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine;N-[4-[3-(2-aminopyrimidin-4-yl)pyridin-2-yl]oxyphenyl]-4-(4-methylthiophen-2-yl)phthalazin-1-amine;CS-0485;N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine;N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine;AMG 900;N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine (ACI)
Cas No.	945595-80-2
分子式	C₂₈H₂₁N₇Os
分子量	503.58
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂，作用于 Aurora A，B 和 C，IC50 分别为 5 nM，4 nM 和 1 nM。

产品详情	AMG 900 是一种有效的选择性的 pan-Aurora 激酶抑制剂，作用于 Aurora A，B 和 C，IC₅₀ 分别为 5 nM，4 nM 和 1 nM。
生物活性	AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC 50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
性状	Solid
IC50 & Target[1][2]	Aurora A 5 nM (IC50) Aurora B 4 nM (IC
体外研究(In Vitro)	AMG 900 inhibits the enzyme activity of all 3 aurora kinase family members with IC50 values of 5 nM or less. In HeLa cells, AMG 900 inhibits autophosphorylation of aurora-A and -B in a concentration-dependent manner. Treatment of HCT116 cells with 50 nM of AMG 900 for 48 hours resulted in polyploidy and suppresses the formation of colonies after cell replating. AMG 900 inhibits cell proliferation, with EC50 values ranging from 0.7 to 5.3 nM. Importantly, 4 of these AMG 900-sensitive cell lines (HCT-15, MES-SA-Dx5, 769P, and SNU449) are resistant to paclitaxel and other anticancer agents. AMG 900 inhibits p-histone H3 or induced polyploidy across all the cell lines tested irrespective of P-gp or BCRP status with uniform potency (IC50 or EC50 values ranging from 2 to 3 nM). has
体内研究(In Vivo)	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 G 2 M 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 elim
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (99.29 mM)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

AMG 900

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