UNC-2025

Research use only, not for human use.

UNC-2025（ IC50 of 0.74 nM and 0.8 nM） is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.

UNC-2025 is a novel potent and highly orally bioavailable Mer/FLT3 dual inhibitor, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.

Western Blot Analysis Cell Line:32D CellsConcentration:0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM Incubation Time:1 hour Result:Inhibited p-MEK, p-AXL, p-TYRO3 expression Cell Viability Assay Cell Line:Mononuclear cells?Concentration:14 nM–10μM Incubation Time:48 hourResult:Showed IC50 values ranged from 9.0 nM to >10μ M with a median IC50 of 2.38 μM.Western Blot Analysis Cell Line:MERTK-expressing B-cell and T-cell acute lymphoid leukemia (B-ALL and T-ALL) and acute myeloid leukemia (AML) cell lines Concentration:25-300 nM Incubation Time:1 hour Result:Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.

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UNC2025, UNC2025, UNC 2025

Membrane Transporter/Ion Channel

TRP/TRPV Channel

FLT3| AXL| Mer| Tyro3

Cancer

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1429881-91-3

513.12

C28H41ClN6O

>98% (HPLC)

DMSO : 33.33 mg/mL. 69.92 mM;

CCCCNc1ncc2c(cn(c2n1)[C@H]1CC[C@@H](CC1)O)c1ccc(cc1)CN1CCN(CC1)C.Cl.Cl

(1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol

(-20℃)

With Ice Pack

≥ 2 years