UNC 569 hydrochloride

SKU: orb1306407

Description

UNC 569 hydrochloride is a potent, ATP-competitive inhibitor of Mer (IC50=2.9 nM; Ki=4.3 nM), with additional activity against Axl and Tyro3. It is a valuable research tool for studying the role of TAM kinases in cancers such as acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors in experimental models.

Research Area

Signal Transduction

Key Properties

• MW: 432.96
• Purity: 99.93% (May vary between batches)
• Formula: C₂₂H₃₀ClFN₆
• SMILES: CCCCNC1=NC=C(C2=N1)C(C3=CC=C(F)C=C3)=NN2C[C@@H]4CC[C@@H](N)CC4.Cl
• Target: TAM Receptor,TAM Receptor
• Solubility: 0.1M HCl:6 mg/mL (13.86 mM);DMSO:3.61 mg/mL (8.34 mM)

Bioactivity

• In Vivo:
  In Leukemic zebrafish, UNC 569 hydrochloride (4 µM) induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish. UNC 569 hydrochloride has low systemic clearance (19.5 mL/min/kg), high volume of distribution (Vss of 5.83 L/kg), and good oral bioavailability (57%).
• In Vitro:
  UNC 569 hydrochloride inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL 697 and Jurkat cell lines, respectively. UNC 569 hydrochloride (1 µM) treatment effectively inhibits the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways. In ALL cell lines, UNC 569 hydrochloride (0.4 -2 µM) induces apoptosis and increases the levels of cleaved Caspase 3 and cleaved PARP.

Storage & Handling

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

Alternative Names

1350547-65-7, 1350547-65-7 Free base, AXL, Mer, TAMReceptor, TAM Receptor, Tyro3, UNC 569 hydrochloride, UNC 569 Hydrochloride, UNC 569 hydrochloride (1350547-65-7 Free base), UNC-569 Hydrochloride, UNC569 Hydrochloride

Compound Identifiers

PubChem CID

168012328