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Cat. No. Name Size Price Add Cart
KI3375PHA-680632QuoteQuote

Chemical Characteristic

Product NamePHA-680632
CAS No.398493-79-3
Molecular Weight 501.62
FormulaC28H35N7O2
Chemical NameN-(2,6-diethylphenyl)-3-[[4-(4-methylpiperazin-1-yl)benzoyl]amino]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazole-5-carboxamide
Smilesn1[nH]c2c(c1NC(=O)c1ccc(cc1)N1CCN(CC1)C)CN(C2)C(=O)Nc1c(cccc1CC)CC
Chemical Structure

Biological activities

PHA-680632 is a novel, highly selective Aurora kinase inhibitor. PHA-680632 inhibits Aurora A, B, and C kinases with IC50s of 27, 135, and 120 nM, respectively. PHA-680632 also inhibits FLT3, LCK, PLK1, STLK2, VEGFR2, and VEGFR3 kinases with IC50s of 0.82, 1.95, 0.78, 5.5, 1.92 and 1.00 µM, respectively. PHA-680632 is a potent inhibitor of the phosphorylation of histone H3. PHA-680632 has potent anti-proliferative activity in a wide range of cell types (C33A, HeLa, HCT116, HT29, LOVO, A549, MCF7) with IC50s ranging from 0.06 to 7.15 µM.[1] PHA-680632 (24 hours exposure) is an effective inhibitor of colony formation in vitro, with a dose-dependent effect at the range of 50 nM to 2.5 mM in different cell lines (HCT116, HT29, and A549 cells). PHA-680632 (0.2 to 0.4 µM) induces polyploidy in HCT116 cell line. PHA-680632 enhances radiation-induced apoptosis in p53-/- HCT116 cells.[2] PHA-680632 suppresses tumor growth in syngeneic models in mouse and rat.[1] PHA-680632 induces a marked tumour growth inhibition in vivo xenograft in nude mice.[2]

Protocols

In vitro, PHA-680632 is dissolved in DMSO.[1]

References

[1] Soncini C, et al. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006, 12(13): 4080-4089.
[2] Tao Y, et al. Enhancement of radiation response by inhibition of Aurora-A kinase using siRNA or a selective Aurora kinase inhibitor PHA-680632 in p53-deficient cancer cells. Br J Cancer. 2007, 97(12): 1664-1672.

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