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

UNC2025 hydrochloride 

Cat. No.: HY-12344A Purity: 99.41%
Handling Instructions

UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride 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 hydrochloride Chemical Structure

UNC2025 hydrochloride Chemical Structure

CAS No. : 2070015-17-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 68 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 68 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
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25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

Other Forms of UNC2025 hydrochloride:

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Description

UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride 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].

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

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 Proliferation Assay[1]

Cell Line: Mononuclear cells 
Concentration: 14 nM–10 μM
Incubation Time: 48 hours
Result: Showed IC50 values ranged from 9.0 nM to >10 μM with a median IC50 of 2.38 μM.

Western Blot Analysis[2]

Cell Line: Kasumi-1 AML and 697 B-ALL cells
Concentration: 25-300 nM
Incubation Time: 48 hours
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].

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

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

513.12

Formula

C₂₈H₄₁ClN₆O

CAS No.
SMILES

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

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: 

H2O : 55 mg/mL (107.19 mM; Need ultrasonic)

DMSO : 10 mg/mL (19.49 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9489 mL 9.7443 mL 19.4886 mL
5 mM 0.3898 mL 1.9489 mL 3.8977 mL
10 mM 0.1949 mL 0.9744 mL 1.9489 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (194.89 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 1 mg/mL (1.95 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1 mg/mL (1.95 mM); Clear solution

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

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

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Product Name:
UNC2025 hydrochloride
Cat. No.:
HY-12344A
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