1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
  3. UNC569

UNC569 

Cat. No.: HY-117596 Purity: 98.64%
Handling Instructions

UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research

For research use only. We do not sell to patients.

UNC569 Chemical Structure

UNC569 Chemical Structure

CAS No. : 1350547-65-7

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Description

UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research[1][2]

IC50 & Target

IC50: 2.9 nM (Mer), 37 nM (Axl), 48 nM (Tyro3)[1] Ki: 4.3 nM (Mer)[1]

In Vitro

UNC569 (24 hours) induces apoptosis in ALL cell lines, and increases the levels of cleaved Caspase 3 and cleaved PARP[2].
UNC569 (1 µM; 1.5 hours) treatment effectively inhibit the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways[2].
UNC569 (1 hour) inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL (acute lymphoblastic leukemia) 697 and Jurkat cell lines, respectively[1][2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: 697 and Jurkat cells
Concentration: 0.4 µM, 0.8 µM, 1 µM, 1.2 µM, 1.4 µM, 1.6 µM, 1.8 µM, 2 µM
Incubation Time: 24 hours
Result: Induced apoptosis in ALL cell lines.

Western Blot Analysis[2]

Cell Line: 697 and Jurkat cells
Concentration: 1 µM
Incubation Time: 1.5 hours
Result: Inhibited Mer activation and downstream signaling through ERK1/2 and AKT.
In Vivo

The in vivo pharmacokinetic properties of UNC569 (3 mg/kg) are also assessed in mice via both intravenous (IV) and oral (PO) administration. UNC569 has low systemic clearance (19.5 mL/min/kg), high volume of distribution (Vss of 5.83 L/kg), and good oral bioavailability (57%)[1].
Leukemic zebrafish are treated continuously for 2 weeks by immersion in 4 µM UNC569. the result shows that UNC569 induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

396.50

Formula

C₂₂H₂₉FN₆

CAS No.
SMILES

FC1=CC=C(C2=NN(C[[email protected]]3CC[[email protected]](N)CC3)C4=NC(NCCCC)=NC=C42)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (78.81 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5221 mL 12.6103 mL 25.2207 mL
5 mM 0.5044 mL 2.5221 mL 5.0441 mL
10 mM 0.2522 mL 1.2610 mL 2.5221 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

UNC569UNC 569UNC-569TAM ReceptorTyro3AxlMerpyrazolopyrimidineATP-competitiveALLanti-oncogenicAKTERKInhibitorinhibitorinhibit

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UNC569
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