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UNC2025

Catalog No.
B8016
orally bioavailable dual MER/FLT3 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$105.00
In stock
5mg
$105.00
In stock
25mg
$315.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with the IC50 value of 0.8/0.74 nM for Mer/Flt3[1].

In vitro: In duplicate versus 305 kinases at Carna Biosciences using a microcapillary electrophoresis assay, UNC2025 inhibited Mer and Flt3 with the greatest potency. In B-ALL 697 cell lysates using the ATP ActivX probe assay, UNC2025 inhhibited the activity of Mer with an IC50 of 0.05 nM. In 697 B-ALL cells, UNC2025 potently inhibited Mer phosphorylation with an IC50 of 2.7 nM. Similarly, in Flt3-ITD positive Molm-14 acute myeloid leukemia cells, treatment with UNC2025 decreased phosphorylation of Flt3 with an IC50 of 14 nM. In soft agar cultures of the A549 NSCLC and Molm-14 AML cell lines, incubation withUNC2025 significantly inhibited colony formation, which was known to depend on Merand Flt3,respectively, for optimal expression of oncogenic phenotypes. Much higher concentrations of UNC2025 were required to effectively inhibit phosphorylation of Axl (IC50 = 122 nM) and Tyro3 (IC50 = 301 nM)[1].

In vivo: In mice with human leukemia xenografts, a single dose of UNC2025 (3 mg/kg) administered orally was sufficient to decrease Merphospho-protein levels in bone marrow leukemia cells by greater than 90% [1].

Reference:
[1]. Zhang W1,DeRyckere D,Hunter D,Liu J,Stashko MA,Minson KA, et,al. UNC2025, a potent and orally bioavailableMER/FLT3dual inhibitor.J Med Chem.2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.

Product Citation

Chemical Properties

StorageDesiccate at -20°C
M.Wt476.66
Cas No.1429881-91-3
FormulaC28H40N6O
Solubility≥23.85 mg/mL in DMSO; insoluble in EtOH; ≥6.09 mg/mL in H2O with ultrasonic
Chemical Name(1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol
SDFDownload SDF
Canonical SMILESCN1CCN(CC2=CC=C(C3=CN([[email protected]@H]4CC[[email protected]@H](O)CC4)C5=NC(NCCCC)=NC=C35)C=C2)CC1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

697 B-ALL cells; Flt3-ITD positive Molm-14 acute myeloid leukemia cells; A549 NSCLC cells

Preparation method

The solubility of this compound in DMSO is >23.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-300 nM; 1 h

Applications

In 697 B-ALL cells, UNC2025 inhibited Mer phosphorylation with IC50 value of 2.7 nM. In Flt3-ITD positive Molm-14 acute myeloid leukemia cells, UNC2025 inhibited phosphorylation of Flt3 with an IC50 of 14 nM. In A549 NSCLC cells and Molm-14 AML cells, UNC2025 inhibited colony formation in Mer-dependent and Flt3-dependent way.

Animal experiment [1]:

Animal models

mice with human leukemia xenografts

Dosage form

3 mg/kg; orally

Application

In mice with human leukemia xenografts, UNC2025 inhibited Mer phosphor-protein levels in bone marrow leukemia cells by greater than 90%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Zhang W1,DeRyckere D,Hunter D,Liu J,Stashko MA,Minson KA, et,al. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. J Med Chem.2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.

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