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UNC2025 hydrochloride

Chemical Structure : UNC2025 hydrochloride

CAS No.:

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 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; also potently inhibits Axl and Tyro3 (IC50=14 and 17 nM) in vitro; 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; 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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