SML3721
PHA-680632
≥98% (HPLC)
别名:
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′-{3-[4-(4-methylpiperazino)benzamide)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea, PHA 680632, PHA680632
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关于此项目
经验公式（希尔记法）:
C28H35N7O2
化学文摘社编号:
分子量:
501.62
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
N1(CCN(CC1)c2ccc(cc2)C(=O)Nc3n[nH]c4c3CN(C4)C(=O)Nc5c(cccc5CC)CC)C
InChI key
OBWNXGOQPLDDPS-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Potent and selective Aurora kinase inhibitor with anti-cancer efficacy in cultures and in animals in vivo.
PHA-680632 is a potent and selective Aurora kinase inhibitor (Aurora A/B/C IC50 = 27/135/120 nM; FGFR1 IC50 = 390 nM, 30- to 200-fold selectivity for Aurora A over 6 other kinases and IC50 >10 μM against 22 kinases) with antiproliferation activity in cancer cultures (IC50 ranges from 60 nM to 7.15 μM) and anti-tumor efficacy in mice and rats in vivo (15-60 mg/kg i.v. b.i.d. or 15-45 mg/kg i.p. t.i.d.)
PHA-680632 is a potent and selective Aurora kinase inhibitor (Aurora A/B/C IC50 = 27/135/120 nM; FGFR1 IC50 = 390 nM, 30- to 200-fold selectivity for Aurora A over 6 other kinases and IC50 >10 μM against 22 kinases) with antiproliferation activity in cancer cultures (IC50 ranges from 60 nM to 7.15 μM) and anti-tumor efficacy in mice and rats in vivo (15-60 mg/kg i.v. b.i.d. or 15-45 mg/kg i.p. t.i.d.)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity
Clinical Cancer Research, 12(13), 4080-4089 (2006)
Y Tao et al.
British journal of cancer, 97(12), 1664-1672 (2007-11-21)
Overexpression of Aurora-A kinase has been correlated with cancer susceptibility and poor prognosis in several human cancers. In this study, we evaluated the effect of inhibition of Aurora-A kinase on cell cycle progression and tumour cell survival after exposure to
Laura Mazzera et al.
Haematologica, 104(12), 2465-2481 (2019-04-06)
Considering that Aurora kinase inhibitors are currently under clinical investigation in hematologic cancers, the identification of molecular events that limit the response to such agents is essential for enhancing clinical outcomes. Here, we discover a NF-κB-inducing kinase (NIK)-c-Abl-STAT3 signaling-centered feedback
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