UNC2025 hydrochloride is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.
UNC2025 also potently inhibits Axl and Tyro3 (IC50=14 and 17 nM) in vitro.
UNC2025 inhibits Mer phosphorylation (IC50=2.7 nM) in 697 B-ALL cells, decreases phosphorylation of Flt3 (IC50=14 nM) in Flt3-ITD positive Molm-14 AML cells, effectively inhibits phosphorylation of Axl (IC50=122 nM) and Tyro3 (IC50=301 nM), 40- to 100-fold selectivity for Mer over Axl and Tyro3.
UNC2025 inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.
Physicochemical Properties
M.Wt
513.1177
Formula
C28H41ClN6O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
DMSO: 6.66 mg/mL (Need ultrasonic); in vivo: dissolved in DMSO and then diluted with water (DMSO:water=1:6)
