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Submit ReviewAMG 900 is a potent pan-Aurora kinase inhibitor (IC50 values are 1 nM, 4 nM, and 5 nM for Aurora C, B, and A, respectively). It is more than 10-fold selective for Aurora kinases over JNK2, Tie2, p38α, Met, and TYK2. AMG 900 inhibits autophosphorylation of Aurora A and B, as well as the phosphorylation of histone H3 on Ser in HeLa cells. AMG 900 inhibits proliferation of 26 tumor cell lines (EC50 ranges from 0.7 nM - 5.3 nM), including Paclitaxel (Cat. No. 1097)-resistant tumor cell lines. In an HCT116 tumor xenograft model, AMG 900 inhibits phosphorylation of histone H3 and tumor growth. It is orally bioavailable.
分子量 | 503.58 |
公式 | C28H21N7OS |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 945595-80-2 |
PubChem ID | 24856041 |
InChI Key | IVUGFMLRJOCGAS-UHFFFAOYSA-N |
Smiles | N1=NC(C=2SC=C(C2)C)=C3C=CC=CC3=C1NC4=CC=C(OC=5N=CC=CC5C6=NC(=NC=C6)N)C=C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 5.04 | 10 温和加热 |
以下数据基于产品分子量 503.58。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 19.86 mL | 99.29 mL | 198.58 mL |
0.5 mM | 3.97 mL | 19.86 mL | 39.72 mL |
1 mM | 1.99 mL | 9.93 mL | 19.86 mL |
5 mM | 0.4 mL | 1.99 mL | 3.97 mL |
参考文献是支持产品生物活性的出版物。
Payton et al (2010) 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. 70 9846 PMID: 20935223
If you know of a relevant reference for AMG 900, please let us know.
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