UNC-2025

SKU: orb1223306

Description

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.

Key Properties

• CAS Number: 1429881-91-3
• MW: 513.12
• Purity: >98% (HPLC)
• Formula: C₂₈H₄₁ClN₆O
• SMILES: CCCCNc1ncc2c(cn(c2n1)[C@H]1CC[C@@H](CC1)O)c1ccc(cc1)CN1CCN(CC1)C.Cl.Cl
• Target: TRP/TRPV Channel
• Solubility: DMSO : 33.33 mg/mL. 69.92 mM

Bioactivity

• In Vitro:
  Western blot analysis. Cell line: 32D Cells. Concentration: 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-10 μM. Incubation time: 48 hour. Result: 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

UNC2025, UNC2025, UNC 2025

Quick Database Links

Gene Symbol

TRP/TRPV Channel