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Key Documents

SML3270

Sigma-Aldrich

QLT0267

≥98% (HPLC)

Synonyme(s) :

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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About This Item

Formule empirique (notation de Hill):
C10H12N6O
Numéro CAS:
6975-75-3
Poids moléculaire :
232.24
Numéro MDL:
MFCD01239326
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

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+

Clé InChI

QNRNTYHAOBVOKW-BUHFOSPRSA-N

Actions biochimiques/physiologiques

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.).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

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
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
Katharina Rothe et al.
Cell stem cell, 27(1), 110-124 (2020-05-16)
Patients with chronic myeloid leukemia (CML) often require lifelong therapy with ABL1 tyrosine kinase inhibitors (TKIs) due to a persisting TKI-resistant population of leukemic stem cells (LSCs). From transcriptome profiling, we show integrin-linked kinase (ILK), a key constituent of focal
Panagiota Chadla et al.
Digestive diseases and sciences, 66(5), 1510-1523 (2020-06-05)
Genomic instability is a hallmark of cancer cells contributing to tumor development and progression. Integrin-linked kinase (ILK) is a focal adhesion protein with well-established role in carcinogenesis. We have previously shown that ILK overexpression is critically implicated in human colorectal
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