1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. UNC2025

UNC2025 

Cat. No.: HY-12344 Purity: 99.97%
Handling Instructions

UNC2025 is a potent and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.

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

UNC2025 Chemical Structure

UNC2025 Chemical Structure

CAS No. : 1429881-91-3

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10 mM * 1 mL in DMSO USD 63 In-stock
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100 mg USD 450 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of UNC2025:

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Description

UNC2025 is a potent and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia[1].

IC50 & Target

IC50: 0.74 nM (Mer); 0.8 nM (Flt3)[1]

In Vitro

UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively[1].
UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50 of 2.7 nM in 697 B-ALL cells[1].
UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50 of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells[1].
UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells[1].
UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells[2].
UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2[2].

Western Blot Analysis[1]

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[2]

Cell Line: Mononuclear cells 
Concentration: 14 nM–10μM
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[2]

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.
In Vivo

UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively[2].
UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively[2].

Animal Model: NSG mice injected with 697 B-ALL cells[2]
Dosage: 50 or 75 mg/kg
Administration: Orally adminstration
Result: Delayed the disease progression.
Molecular Weight

476.66

Formula

C₂₈H₄₀N₆O

CAS No.

1429881-91-3

SMILES

CN1CCN(CC2=CC=C(C3=CN([[email protected]@H]4CC[[email protected]@H](O)CC4)C5=NC(NCCCC)=NC=C53)C=C2)CC1

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 : 33.33 mg/mL (69.92 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0979 mL 10.4897 mL 20.9793 mL
5 mM 0.4196 mL 2.0979 mL 4.1959 mL
10 mM 0.2098 mL 1.0490 mL 2.0979 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

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

Purity: 99.97%

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Keywords:

UNC2025UNC 2025UNC-2025FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3acuteleukemiaMERTKcancerInhibitorinhibitorinhibit

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UNC2025
Cat. No.:
HY-12344
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