AMG-900, Inhibitor
AMG-900
Purity
>98% (HPLC)
Synonyms
AMG-900; AMG 900; AMG900; inhibitor
Purity/Purification
>98% (HPLC)
Suitability
10mM in DMSO
Target
Aurora Kinase
Receptor
AuroraA; AuroraB; AuroraC; p38alpha; Tyk2
Chemical Name
1-Phthalazinamine, N-[4-[[3-(2-amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)
SMILES
CC1=CSC(C2=NN=C(NC3=CC=C(OC4=NC=CC=C4C5=NC(N)=NC=C5)C=C3)C6=C2C=CC=C6)=C1
Molecular Formula
C28H21N7OS
CAS Number
945595-80-2
Preparation and Storage
Store at -20 degree C
Stability: >=2 years
Shipping: Ice Pack
Stability: >=2 years
Shipping: Ice Pack
Structure
Related Product Information for AMG-900, inhibitor
AMG-900 (AMG900) is a potent, highly selective, orally bioavailable pan-Aurora kinase inhibitor with IC50 of 5, 4 and 1nM for Aurora A, B and C, respectively; displays excellent specificity in a panel of 26 kinases with exception of p38alpha and TYK2 (IC50=53 and 220nM), also exhibits high affinity (Kd<50nM) with DDR1, DDR2, and LTK receptor tyrosine kinases; blocks the proliferation of multiple human tumor cell lines including cell lines resistant to paclitaxel, AZD1152, MK-0457, and PHA-739358 with IC50 of 0.7-5.3nM; blocks the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibits the growth of HCT116 tumor xenografts. Blood Cancer Phase 1 Clinical
Product Categories/Family for AMG-900, inhibitor
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.
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.
