UNC2025

SKU: orb1300148

Description

UNC-2025 (MRX-6343) is a potent, orally bioavailable small molecule inhibitor targeting MER and FLT3 kinases with IC50 values of 0.74 nM and 0.8 nM, respectively. It demonstrates approximately 20-fold selectivity over Axl and Tyro3. This inhibitor is a valuable research tool for studying oncology, particularly in leukemia and solid tumor models, both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1429881-91-3
• MW: 476.66
• Purity: 97.48% (May vary between batches)
• Formula: C₂₈H₄₀N₆O
• SMILES: CCCCNc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccc(CN2CCN(C)CC2)cc1
• Target: FLT,TAM Receptor
• Solubility: H2O:Insoluble;Ethanol:8 mg/mL (16.78 mM);DMSO:35.71 mg/mL (74.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.39 mM)

Bioactivity

• Target IC50:
  Mer:0.74 nM|FLT3:0.8 nM
• In Vivo:
  In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth.
• In Vitro:
  In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation.

Storage & Handling

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

Alternative Names

Cluster of differentiation antigen 135, CD135, acute, cancer, AXL, inhibit, mrx-6313, Inhibitor, Mer, MERTK, leukemia, Fms like tyrosine kinase 3, FLT3, TAM Receptor, TAMReceptor, Tyro3, UNC2025, UNC-2025, UNC 2025

Compound Identifiers

PubChem CID

73425588