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PHA-680632 Chemical Structure

PHA-680632

Data Sheet For research use only. Not for human use.
Cat. No. :BCP02311CAS No. :398493-79-3Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 398493-79-3 Cat. No. BCP02311
Name PHA-680632
Synonyms PHA680632;PHA 680632;
SMILES
Chemical Name
Formula C28H35N7O2 M. Wt 501.62
Purity 98% Storage Store at 4-8°C
Description PHA-680632 potently inhibits all three Aurora kinases (A, B, and C) with IC50 values of 27, 135, and 120 nM, respectively. PHA-680632 is selective for Aurora kinases, with 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, VEGFR2, and VEGFR3, and with IC50 higher than 10 μM for another 22 kinases. PHA-680632 shows potent anti-proliferative effects in a wide range of cell types with IC50 values of 0.06–7.15 μM, including HeLa, HCT116, HT29, LOVO, DU145, and NHDF cells. PHA-680632 (0.5 μM) causes polyploidy in tumor cells. The mechanism of action of PHA-680632 is in agreement with inhibition of Aurora kinases. PHA680632 in association with radiation leads to additive effects in cancer cells, especially in the p53-deficient cells. Combined ionising radiation (IR) and treatment of PHA680632 (100–400 nM) prior to IR leads to an enhancement of radiation-induced Annexin V positive cells, micronuclei formation, and Brca1 foci formation only in HCT116 cells with deficient p53, other
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