AMG-900

Research use only, not for human use.

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 (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; 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; 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; 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.

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AMG 900 | AMG900

Cell Cycle/DNA Damage

Aurora Kinase

AuroraA|AuroraB|AuroraC|p38α|Tyk2

Cancer

Blood cancer

945595-80-2

503.6

C28H21N7OS

>98% (HPLC)

10 mM in DMSO

CC1=CSC(C2=NN=C(NC3=CC=C(OC4=NC=CC=C4C5=NC(N)=NC=C5)C=C3)C6=C2C=CC=C6)=C1

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

(-20℃)

With Ice Pack

≥ 2 years