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Merck
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Key Documents

SML3270

Sigma-Aldrich

QLT0267

≥98% (HPLC)

Sinónimos:

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

Fórmula empírica (notación de Hill):
C10H12N6O
Número de CAS:
6975-75-3
Peso molecular:
232.24
MDL number:
MFCD01239326
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

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+

InChI key

QNRNTYHAOBVOKW-BUHFOSPRSA-N

Biochem/physiol Actions

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.).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Jacqueline Tan et al.
Heliyon, 5(8), e02294-e02294 (2019-08-30)
Insulin promotes neuronal survival by activating a phosphatidylinositol 3-kinase (PI 3-kinase)/AKT-dependent signaling pathway and reducing caspase activation. We investigated a role for integrin-linked kinase (ILK) in insulin-mediated cell survival in cultured neurons and differentiated R28 cells. We used a serum
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
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
Rouhollah Mousavizadeh et al.
Scientific reports, 10(1), 12644-12644 (2020-07-30)
Tendons are specialized tissues composed primarily of load-responsive fibroblasts (tenocytes) embedded in a collagen-rich extracellular matrix. Habitual mechanical loading or targeted exercise causes tendon cells to increase the stiffness of the extracellular matrix; this adaptation may occur in part through
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