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UNC2025 hydrochloride

Chemical Structure : UNC2025 hydrochloride

CAS No.: 2070015-17-5

UNC2025 hydrochloride (UNC-2025 hydrochloride)

Catalog No.: PC-42994Not For Human Use, Lab Use Only.

UNC2025 is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

UNC2025 hydrochloride is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.
UNC2025 also potently inhibits Axl and Tyro3 (IC50=14 and 17 nM) in vitro.
UNC2025 inhibits Mer phosphorylation (IC50=2.7 nM) in 697 B-ALL cells, decreases phosphorylation of Flt3 (IC50=14 nM) in Flt3-ITD positive Molm-14 AML cells, effectively inhibits phosphorylation of Axl (IC50=122 nM) and Tyro3 (IC50=301 nM), 40- to 100-fold selectivity for Mer over Axl and Tyro3.
UNC2025 inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.

Physicochemical Properties

M.Wt 513.1177
Formula C28H41ClN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 6.66 mg/mL (Need ultrasonic); in vivo: dissolved in DMSO and then diluted with water (DMSO:water=1:6)

Chemical Name/SMILES

Cyclohexanol, 4-[2-(butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans-, hydrochloride

References

1. Zhang W, et al. J Med Chem. 2014 Aug 28;57(16):7031-41.

2. Cummings CT, et al. Mol Cancer Ther. 2015 Sep;14(9):2014-22.

3. DeRyckere D, et al. Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

4. Branchford BR, et al. J Thromb Haemost. 2018 Feb;16(2):352-363.

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