PHA-680632

PHA-680632 Basic information
Product Name:PHA-680632
Synonyms:N-(2,6-Diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide;Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]-;Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-(2,6-diethylphenyl)-;N-(2,6-diethylphenyl)-3-(4-(4-Methylpiperazin-1-yl)benzaMido)-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazole-5(3H)-carboxaMide;PHA-680632(PHA680632);N-(2,6-Diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)-benzoyl]amino]pyrrolo[3,4-c]pyra;N-(2,6-diethylphenyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)pyrrolo[3,4-c]pyrazole-5(1H,4H,6H)-carboxamide;PHA-680632;PHA680632;PHA 680632
CAS:398493-79-3
MF:C28H35N7O2
MW:501.62
EINECS:
Product Categories:Inhibitors;Inhibitor
Mol File:398493-79-3.mol
PHA-680632 Structure
PHA-680632 Chemical Properties
Melting point 240-242 °C
Boiling point 709.0±60.0 °C(Predicted)
density 1.294
storage temp. Store at -20°C
solubility ≥50.2 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
form Powder
pka12.26±0.70(Predicted)
Safety Information
MSDS Information
PHA-680632 Usage And Synthesis
UsesPHA-680632 is a potent and selective inhibitor of Aurora kinase.
Biological Activitypha-680632 is a novel and potent inhibitor of aurora kinases, a small family of serine/threonine kinases regulating mitosis in chromosome segregation and cell division, that inhibits the activity of all three aurora kinases with 50% inhibition concentration ic50 values of 27 nm, 135 nm and 120 nm for aurora a, b and c kinases respectively. pha-680632 also cross-reacts with other kinases, including fgfr1, flt3, lck, plk1, stlk2, vegfr2 and vegfr3, to a lesser extent and exhibits much higher ic50 values (390 to 5500 nm) compared to aurora kinases. moreover, pha-680632 potently inhibits proliferation in a wide range of cancer cell types, including hct116, a2780, hl60 and hela cells, with ic50 values ranging from 0.06 to 7.15 μm.soncini c, carpinelli p, gianellini l, fancelli d, vianello p, rusconi l, storici p, zugnoni p, pesenti e, croci v, ceruti r, giorgini ml, cappella p, ballinari d, sola f, varasi m, bravo r, moll j. pha-680632, a novel aurora kinase inhibitor with potent antitumoral activity. clin cancer res. 2006 jul 1;12(13):4080-9.
targetAurora A
PHA-680632 Preparation Products And Raw materials
Doxorubicin hydrochloride PD 0332991 HCl MG-132 (+)-JQ1 AZD-8055 NU7441 (KU-57788)

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