371806

GTP-14564

A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases.

• Sinonimo/i: GTP-14564, 1-Phenyl-3-H-8-oxa-2,3-diaza-cyclopenta[a]inden, 3-Phenyl-1H-benzofuro[3,2-c]pyrazole
• Formula empirica (notazione di Hill): C₁₅H₁₀N₂O
• Numero CAS: 34823-86-4
• Peso molecolare: 234.25
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: pale yellow
• Solubilità: DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C15H10N2O/c1-2-6-10(7-3-1)13-15-14(17-16-13)11-8-4-5-9-12(11)18-15/h1-9H,(H,16,17); DZQLVVLATXPWBK-UHFFFAOYSA-N

Descrizione

Descrizione generale

A cell-permeable, reversible, ATP-competitive, and tricyclic, benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC₅₀ = 300 nM for c-fms, c-kit, wt-FLT3, and internal tandem duplication (ITD)-FLT3; 1 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, Akt, PKC, MEK, or ERK1/2 (IC₅₀ >10 µM). Inhibits FLT-3 ligand-dependent growth of Ba/F3 cells expressing wild type FLT-3. Reported to be useful in differentiating signal transduction pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.

A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC₅₀ = 0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, AKT, PKC, MEK, or ERK1/2 (IC₅₀ ≥ 10 µM). Has been used successfully to differentiate between the signalling pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Class III receptor tyrosine kinases

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Carcinogenic / Teratogenic (D)

Altre note

Murata, K., et al. 2003. J. Biol. Chem.278, 32892.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1