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).

• 別名: 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
• 実験式（ヒル表記法）: C₂₂H₂₉FN₆
• 分子量: 396.50
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: beige
• 溶解性: DMSO: 100 mg/mL; water: 2.5 mg/mL (with gentle warming)
• 保管温度: 2-8°C

詳細

詳細

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.

警告

Toxicity: Standard Handling (A)

物理的形状

Supplied as a trifluoroacetate salt.

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable