SML3270
QLT0267
≥98% (HPLC)
别名:
3,5-Diamino-4-(p-methoxyphenyl)hydrazonopyrazole, 4-((4-Methoxyphenyl)diazenyl)-1H-pyrazole-3,5-diamine, ILK-IN-3, KP 15792, KP-15792, KP15792, QLT 0267, QLT-0267
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关于此项目
经验公式（希尔记法）:
C10H12N6O
化学文摘社编号:
分子量:
232.24
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
QLT0267, ≥98% (HPLC)
SMILES string
[nH]1nc(c(c1N)\N=N\c2ccc(cc2)OC)N
InChI
1S/C10H12N6O/c1-17-7-4-2-6(3-5-7)13-14-8-9(11)15-16-10(8)12/h2-5H,1H3,(H5,11,12,15,16)/b14-13+
InChI key
QNRNTYHAOBVOKW-BUHFOSPRSA-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
Orally active, potent and selective integrin-linked kinase (ILK) inhibitor with anti-cancer efficacy in cultures and in vivo.
QLT0267 is an orally active, potent and selective integrin-linked kinase (ILK) inhibitor (IC50 = 26 nM; selectivity: >1000-fold over CK2, CSK, DNA-PK, PIM1, PKB/AKT, PKC, >100-fold over ERK1, GSK3β, LCK, PKA, p70S6K, and RSK1/QLT, >10-fold over CDK1/2/5) that inhibits ILK-dependent cellular signaling (IC50 in 2h = 1 μM against 20 nM EGF-induced pAKT Ser473 phosphorylation in Hth74 cells). QLT0267 treatment causes thyroid cancer cell cycle arrest and apoptosis, leading to anti-proliferation efficacy in cultures (IC50 <6 μM; NPA187, DRO, and K4 cell lines) and in mice in vivo (DRO xenografts-derived tumor growth; 50-100 mg/kg via daily p.o.).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Sofia Nikou et al.
Journal of molecular histology, 51(4), 385-400 (2020-06-28)
Integrin-linked kinase (ILK) forms a heterotrimeric protein complex with PINCH and PARVIN (IPP) in Focal Adhesions (FAs) that acts as a signaling platform between the cell and its microenvironment regulating important cancer-related functions. We aimed to elucidate the role of
Alexandre Ghazi et al.
Oncoimmunology, 10(1), 1940674-1940674 (2021-07-13)
The CMS4 mesenchymal subtype of colorectal cancer (CRC) is associated with poor prognosis and resistance to treatment. The cellular prion protein PrPC is overexpressed in CMS4 tumors and controls the expression of a panel of CMS4-specific genes in CRC cell
Razan Wafai et al.
Breast cancer research : BCR, 22(1), 136-136 (2020-12-06)
Breast cancers acquire aggressive capabilities via epithelial to mesenchymal transition (EMT), in which various integrins/integrin-linked kinase signalling are upregulated. We investigated this in two patient-derived xenografts (PDXs) developed from breast-to-bone metastases, and its functional significance in a breast cancer cell
Maher N Younes et al.
Molecular cancer therapeutics, 4(8), 1146-1156 (2005-08-12)
We investigated integrin-linked kinase (ILK), a focal adhesion serine-threonine protein kinase, as a new molecular target for treating anaplastic thyroid cancer. ILK mediates cell growth and survival signals and is overexpressed in a number of cancers. Therefore, we hypothesized that
Masahiro Shiihara et al.
European journal of cancer (Oxford, England : 1990), 148, 239-250 (2021-03-23)
Pancreatobiliary cancer is a highly aggressive tumour with a dismal prognosis. Personalised medicine represents a promising and effective therapeutic approach for this intractable disease. In this study, we aimed to establish a system for identifying and testing genotype-oriented targeted drugs
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