445835-M

Mer RTK Inhibitor, UNC569

Mer RTK Inhibitor, UNC569, 1350547-65-7 is a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM).

• Synonyme(s) : Mer RTK Inhibitor, UNC569, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-(( trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
• Formule empirique (notation de Hill): C₂₂H₂₉FN₆
• Poids moléculaire : 396.50
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: beige
• Solubilité: DMSO: 100 mg/mL; water: 2.5 mg/mL (with gentle warming)
• Température de stockage: 2-8°C

Description

Description générale

An orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC₅₀ = 2.9 nM; K_i = 4.3 nM) with ~10-fold greater selectivity over other TAM family kinases (IC₅₀ = 37 and 48 nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30 nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC₅₀ of 141 nM. Exhibits desirable pharmacokinetic profile and efficacy in mice.

Avertissement

Toxicity: Standard Handling (A)

Forme physique

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable fo rup to 6 months at -20°C.

Autres remarques

Liu, J., et al. 2012. ACS Med. Chem. Lett.3, 129.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable