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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.
M. Wt | 503.58 |
Formula | C28H21N7OS |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 5.04 | 10 with gentle warming |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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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This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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