UNC2541
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
A structure-based drug design approach led to macrocyclic pyrimidines as potent Mer tyrosine kinase (MerTK)-specific inhibitors. Through SAR studies, analogue 11 (UNC2541) was identified as a key compound and exhibits sub-micro molar inhibitory activity in the cell-based enzyme-linked immunosorbent assay (ELISA). In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket.
UNC2541, Bulk in stock, contact us by email for the quotation.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | UNC2541 |
|---|---|
| Iupac 化学名称 | (S)-7-amino-N-(4-fluorobenzyl)-8-oxo-2,9,16-triaza-1(2,4)-pyrimidinacyclohexadecaphane-15-carboxamide |
| 同义词 | UNC2541; UNC-2541; UNC 2541; |
| 英文同义词 | UNC2541; UNC-2541; UNC 2541; |
| 分子式 | C24H34FN7O2 |
| 分子量 | 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号 | 1612782-86-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色至白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期可在0-4度保存，数天至数月；长期可在-20度保存三年。 |
| 可溶性 | 可溶于DMSO；不溶于水 |
| 处理方式 | |
| 运输条件 | 产品可以在室温下运输 |
| 海关编码 |
| Targets | MerTK-specific inhibitor |
|---|---|
| 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 |
