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UNC5293

Chemical Structure : UNC5293

CAS No.: 2226789-82-6

UNC5293 (UNC-5293)

Catalog No.: PC-72649Not For Human Use, Lab Use Only.

UNC5293 (UNC-5293) is a potent, highly selective, orally available inhibitor of MER receptor tyrosine kinase (MERTK) with IC50 0.9 nM, Ki 0.19 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

UNC5293 (UNC-5293) is a potent, highly selective, orally available inhibitor of MER receptor tyrosine kinase (MERTK) with IC50 0.9 nM, Ki 0.19 nM.
UNC5293 exhibits an excellent Ambit selectivity score (S50 (100 nM) = 0.041), and displays 50-100 fold selectivity over other two TAM Receptor member kinases (Tyro3 and Axl).
UNC5293 demonstrated potent and selective inhibition of MERTK in cell-based assays. has excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability) and was active in bone marrow leukemia cells in a murine model.

Physicochemical Properties

M.Wt 518.706
Formula C30H42N6O2
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

10 mM in DMSO

Chemical Name/SMILES

(2,6-dimethylpyridin-4-yl)(4-(7-((1r,4S)-4-hydroxycyclohexyl)-2-(((S)-pentan-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)piperidin-1-yl)methanone

References

1. Zheng H, et al. Eur J Med Chem. 2021 Aug 5;220:113534.

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