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UNC2025

Chemical Structure : UNC2025

CAS No.: 1429881-91-3

UNC2025 (UNC 2025, UNC-2025)

Catalog No.: PC-42993Not 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.
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.
UNC2025 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 476.6568
Formula C28H40N6O
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: 33.33 mg/mL; H2O: < 4.9 mg/mL

Chemical Name/SMILES

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

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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