PHA-680632 is the first representative of a new class of Aurora inhibitors (Aurora A/B/C IC50 at 27, 135 and 120 nM, respectively). This agent has a high potential for further development as an anticancer therapeutic. PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor growth inhibition in different animal tumor models at well-tolerated doses. The IC50 of PHA-680632 for cell anti-proliferation ranged from 0.11 uM to 5.6 uM.
|Cell lines||HeLa, HCT116, HT29, LOVO, DU145, and NHDF cells|
|Preparation method||Seeding cells (5 ×103 to 1.5 ×104 per cm2) in 24-well plate. 24 hours later, treating plates with PHA-680632 and incubating for 72 hours. At the end of incubation time, detaching cells from each plate and using a cell counter to count . Calculating IC50s using percentage of growth versus untreated cont|
|Concentrations||0.001-1 μM, dissolved in DMSO as 10 mM stock solution|
|Incubation time||72 hours|
|Animal models||Mice (female athymic nude) xenografts models of p53−/− HCT116 cells|
|Formulation||Dissolved in 20% Tween-80 in 5% glucose solution|
|Administration||Intraperitoneal (i.p.) injection twice a day|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 90 mg/mL|
|Related Aurora Kinase Products|
LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with Ki values of 0.8 nM and 1038 nM for AurA and AurB, respectively.
SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
|Aurora Kinase Inhibitor III
Aurora Kinase Inhibitor III is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM.
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex.
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