SML3270

QLT0267

≥98% (HPLC)

• Synonym(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
• Empirical Formula (Hill Notation): C₁₀H₁₂N₆O
• CAS Number: 6975-75-3
• Molecular Weight: 232.24
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD01239326
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• 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

Description

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.).

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable