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- 规格参数
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Biochem/physiol Actions
Orally available, cell penetrant, potent and highly selective PROTAC that induces NAMPT degradation in several cancer cells lines
SIAIS630121 is an orally available, cell penetrant, potent and highly selective proteolysis-targeting chimera (PROTAC) that induces NAMPT (nicotinamide phosphoribosyltransferase) degradation in several cancer cells lines (SW620, HT29, and HCT116). It contains NAMPT inhibitor FK866 linked to cereblon (CRBN) ligand lenalidomide. SIAIS630121 exhibits rapid and potent degradation of iNAMPT and eNAMPT.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | -10 to -25°C |
| SMILES string | O=C(/C=C/C1=CN=CC=C1)NCCCCC2CCN(CC2)C(C3=CC=C(C=C3)N4CCN(CC4)CCCCCCC#CC5=CC=CC6=C5CN(C6=O)C7C(NC(CC7)=O)=O)=O |
| InChI | 1S/C49H59N7O5/c57-45(22-16-38-12-10-26-50-35-38)51-27-7-6-11-37-24-29-55(30-25-37)48(60)40-17-19-41(20-18-40)54-33-31-53(32-34-54)28-8-4-2-1-3-5-13-39-14-9-15-42-43(39)36-56(49(42)61)44-21-23-46(58)52-47(44)59/h9-10,12,14-20,22,26,35,37,44H,1-4,6-8,11,21, |
| InChI key | JTTGVFCANBFLCE-CJLVFECKSA-N |
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