UNC2541 is a potent and MerTK-specific inhibitor and exhibits sub-micro molar inhibitory activity in the cell-based ELISA assay through SAR studies. In addition, an X-ray structure of MerTK protein in complex with UNC2541 was resolved to show that these macro-cycles bind in the MerTK ATP pocket.
Graphical abstract
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Name | UNC2541 |
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Iupac Chemical Name | (S)-7-amino-N-(4-fluorobenzyl)-8-oxo-2,9,16-triaza-1(2,4)-pyrimidinacyclohexadecaphane-15-carboxamide |
Synonyms | UNC2541; UNC-2541; UNC 2541; |
Molecular Formula | C24H34FN7O2 |
Molecular Weight | 471.57 |
Smile | O=C([C@H](CCCCN1)N)NCCCCCCNC2=NC=C(C(NCC3=CC=C(C=C3)F)=O)C1=N2 |
InChiKey | ONIHBIZGUJZDHG-FQEVSTJZSA-N |
InChi | InChI=1S/C24H34FN7O2/c25-18-10-8-17(9-11-18)15-30-22(33)19-16-31-24-29-14-5-2-1-4-13-28-23(34)20(26)7-3-6-12-27-21(19)32-24/h8-11,16,20H,1-7,12-15,26H2,(H,28,34)(H,30,33)(H2,27,29,31,32)/t20-/m0/s1 |
CAS Number | 1612782-86-1 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO, not in water |
Handling | |
Shipping Condition | Shipped under ambient temperature |
HS Code |
Targets | MerTK-specific inhibitor |
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Mechanism | UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM). |
Cell study | |
Animal study | |
Clinical study |