UNC2250

Alias: UNC-2250; UNC 2250; UNC2250
Cat No.:V0636 Purity: ≥98%
UNC2250 (UNC-2250) is a novel, potent and selective Mer inhibitor with potential antitumor activity.
UNC2250 Chemical Structure CAS No.: 1493694-70-4
Product category: TAM Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

UNC2250 (UNC-2250) is a novel, potent and selective Mer inhibitor with potential antitumor activity. It exhibits selectivity for inhibiting Mer that is between 160 and 60 times higher than that of other closely related kinases like Axl/Tyro3. It inhibits Mer with an IC50 of 1.7 notM. In vitro, UNC2250 exhibits strong anti-proliferative activity, and it also has antitumor efficacy in vivo.

Biological Activity I Assay Protocols (From Reference)
Targets
Mer (IC50 = 1.7 nM); Tyro3 (IC50 = 100 nM)
ln Vitro

UNC2250 (5-500 nM; 1 hour) inhibits 697 B-ALL cells' Mer phosphorylation, with an IC50 value of 9.8 nM[1].
UNC2250 effectively prevents ligand-dependent phosphorylation of a chimeric protein made up of the intracellular tyrosine kinase domain of Mer and the extracellular and transmembrane domains of the epidermal growth factor (EGF) receptor[1].
UNC2250 embryogenesis prevents colony formation in soft agar cultures of the BT-12 rhabdoid tumor and the Colo699 NSCLC cell lines[1].

ln Vivo
UNC2250 has a reasonable oral bioavailability, good solubility, and a moderate half-life, clearance, and volume of distribution, according to an in vivo PK experiment.
Enzyme Assay
In a 384-well polypropylene microplate, activity assays are conducted using a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, and 0.1% bovine serum albumin (BSA). Additionally, 1.0 μM fluorescent substrate and ATP at the Km for each enzyme are presented. The addition of 20 μL of 70 mM EDTA ends all reactions. Phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader fitted with a 12-sipper chip following an incubation period of 180 minutes. Software called EZ Reader is used to analyze data.
Cell Assay
The culture medium for BT-12 rhabdoid tumor cells (10 000 cells) is 2.0 mL of 0.35% soft agar with 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only.This medium is then covered with 0.5 mL of 1× RPMI medium that contains 15% FBS and 10 or DMSO vehicle only. The vehicle is refreshed twice a week for medium and 10 tires. Tetrazolium bromide stained the colonies, and after three weeks, they were counted. In 1.5 mL of 0.35% soft agar with 1× RPMI medium and 10% FBS, Colo699 NSCLC cells (15 000 cells) are cultured. This medium is then covered with 2.0 mL of 1× RPMI medium with 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. The vehicle is refreshed three times a week for both medium and 10 tires. Two weeks after colony formation, they are counted and stained with nitrotetrazolium blue chloride.
Animal Protocol
N/A
Mice or rat
References

[1]. Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem, 2013. 56(23): p. 9683-92.

[2]. Pyrimidine compounds for the treatment of cancer.WO2013177168A1.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H36N6O2
Molecular Weight
440.58
Exact Mass
440.29
Elemental Analysis
C, 65.43; H, 8.24; N, 19.07; O, 7.26
CAS #
1493694-70-4
Appearance
Solid powder
SMILES
CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C3=NC=C(C=C3)CN4CCOCC4
InChi Key
HSYSSKFCQHXOBP-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29)
Chemical Name
4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol
Synonyms
UNC-2250; UNC 2250; UNC2250
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~2 mg/mL (~4.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
5% DMSO+30% PEG 300+ddH2O: 0.5mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2697 mL 11.3487 mL 22.6974 mL
5 mM 0.4539 mL 2.2697 mL 4.5395 mL
10 mM 0.2270 mL 1.1349 mL 2.2697 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • UNC2250

    X-ray structure of 3 in complex with Mer kinase domain (PDB ID Code: 4M3Q). J Med Chem. 2013 Dec 12;56(23):9683-92.

  • UNC2250

    10 inhibits Mer tyrosine kinase activation in acute leukemia cells. J Med Chem. 2013 Dec 12;56(23):9683-92.

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