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AMG-900

Chemical Structure : AMG-900

CAS No.: 945595-80-2

AMG-900 (AMG 900;AMG900)

Catalog No.: PC-43432Not For Human Use, Lab Use Only.

AMG-900 (AMG900) is a potent, highly selective, orally bioavailable pan-Aurora kinase inhibitor with IC50 of 5, 4 and 1 nM for Aurora A, B and C, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AMG-900 (AMG900) is a potent, highly selective, orally bioavailable pan-Aurora kinase inhibitor with IC50 of 5, 4 and 1 nM for Aurora A, B and C, respectively.
AMG-900 displays excellent specificity in a panel of 26 kinases with exception of p38α and TYK2 (IC50=53 and 220 nM), also exhibits high affinity (Kd< 50 nM) with DDR1, DDR2, and LTK receptor tyrosine kinases.
AMG-900 blocks the proliferation of multiple human tumor cell lines including cell lines resistant to paclitaxel, AZD1152, MK-0457, and PHA-739358 with IC50 of 0.7-5.3 nM.
AMG-900 blocks the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibits the growth of HCT116 tumor xenografts.

Physicochemical Properties

M.Wt 503.58
Formula C28H21N7OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Phthalazinamine, N-[4-[[3-(2-amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-

References

1. Geuns-Meyer S, et al. J Med Chem. 2015 Jul 9;58(13):5189-207.

2. Juan G, et al. J Transl Med. 2014 Nov 4;12:307.

3. Paller CJ, et al. Cancer Med. 2014 Oct;3(5):1322-35.

4. Payton M, et al. Cancer Res. 2010 Dec 1;70(23):9846-54.

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