| Identification | Back Directory | [Name]
4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine | [CAS]
6975-75-3 | [Synonyms]
ILK-IN-3
1H-Pyrazole-3,5-diamine, 4-[2-(4-methoxyphenyl)diazenyl]-
4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazole-3,5-diamine
3-amino-4-[(E)-2-(4-methoxyphenyl)diazenyl]-1H-pyrazol-5-ylamine | [Molecular Formula]
C10H12N6O | [MDL Number]
MFCD01239326 | [MOL File]
6975-75-3.mol | [Molecular Weight]
232.24 |
| Chemical Properties | Back Directory | [storage temp. ]
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | [solubility ]
DMSO: 83.33 mg/mL (358.81 mM) | [form ]
Solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel.html" class="link-product" target="_blank">Docetaxel (HY-B0011) in orthotopic LCC6 model[1][2]. | [Biological Activity]
QLT0267 is an orally activepotent and selective integrin-linked kinase (ILK) inhibitor (IC50 = 26 nM; selectivity: >1000-fold over CK2CSKDNA-PKPIM1PKB/AKTPKC>100-fold over ERK1GSK3βLCKPKAp70S6Kand RSK1/QLT>10-fold over CDK1/2/5) th at 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 apoptosisleading to anti-proliferation efficacy in cultures (IC50 <6 μM; NPA187DROand K4 cell lines) and in mice in vivo (DRO xenografts-derived tumor growth; 50-100 mg/kg via daily p.o.). | [in vivo]
ILK-IN-3 (QLT0267) (200 mg/kg; po; 28 days) Inhibits tumor growth in the in situ LCC6 model[1].
| [IC 50]
DYRK1 | [storage]
Store at -20°C | [References]
[1] Jessica Kalra, et al. Validating the Use of a Luciferase Labeled Breast Cancer Cell Line, MDA435LCC6, as a Means to Monitor Tumor Progression and to Assess the Therapeutic Activity of an Established Anticancer Drug, Docetaxel (Dt) Alone or in Combination With the ILK Inhibitor, QLT0267. Cancer Biol Ther. 2011 May 1;11(9):826-38. DOI:10.4161/cbt.11.9.15183
[2] Mavrogeni ME, et al. A facile consensus ranking approach enhances virtual screening robustness and identifies a cell-active DYRK1α inhibitor. Future Med Chem. 2018 Oct;10(20):2411-2430. DOI:10.4155/fmc-2018-0198 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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