| Identification | Back Directory | [Name]
PHA-680632 | [CAS]
398493-79-3 | [Synonyms]
CS-411
PHA-680632 USP/EP/BP
PHA-680632(PHA680632)
PHA-680632;PHA680632;PHA 680632
Pyrrolo[3,4-c]pyrazole-5(1H)-carboxaMide, N-(2,6-diethylphenyl)-
N-(2,6-Diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)-benzoyl]amino]pyrrolo[3,4-c]p
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
N-(2,6-diethylphenyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)-4,6-dihydropyrrolo[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)-3-[[4-(4-methylpiperazin-1-yl)benzoyl]amino]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazole-5-carboxamide
Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]-
N-(2,6-diethylphenyl)-3-(4-(4-Methylpiperazin-1-yl)benzaMido)-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazole-5(3H)-carboxaMide | [Molecular Formula]
C28H35N7O2 | [MDL Number]
MFCD16038900 | [MOL File]
398493-79-3.mol | [Molecular Weight]
501.62 |
| Chemical Properties | Back Directory | [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 | [pka]
12.26±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PHA-680632 is a potent and selective inhibitor of Aurora kinase. | [Biological Activity]
pha-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. | [in vivo]
PHA-680632 suppresses tumor growth in animal models. PHA-680632 treatment at 45 mg/kg dose results in 85% of TGI without signs of toxicity in the HL60 human acute myelogenous leukemia xenograft model. PHA-680632 treatment at 60 mg/kg i.v. b.i.d. for 5 days results in 78% of TGI without signs of toxicity in the A2780 human ovarian carcinoma model[1]. PHA680632 in association with radiation leads to an additive effect in cancer cells, especially in the p53-deficient cells, but does not act as a radiosensitiser[2]. | [target]
Aurora A | [IC 50]
Aurora A: 27 nM (IC50); Aurora B: 135 nM (IC50); Aurora C: 120 nM (IC50) | [storage]
Store at -20°C |
|
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|