For research use only. Not for therapeutic Use.
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
ADC-3 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <3 pM and 9 pM, respectively[1].
ADC-3 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells[1].
| Catalog Number | I019473 |
| CAS Number | 2241019-57-6 |
| Synonyms | 4-[4-[3-[2-(2,5-dioxopyrrol-1-yl)ethoxy]propanoyl]piperazin-1-yl]-N-[[2-fluoro-4-[[(1S,2S)-2-pyridin-3-ylcyclopropanecarbonyl]amino]phenyl]methyl]benzamide |
| Molecular Formula | C36H37FN6O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C36H37FN6O6/c37-31-20-27(40-36(48)30-21-29(30)25-2-1-12-38-22-25)6-3-26(31)23-39-35(47)24-4-7-28(8-5-24)41-13-15-42(16-14-41)32(44)11-18-49-19-17-43-33(45)9-10-34(43)46/h1-10,12,20,22,29-30H,11,13-19,21,23H2,(H,39,47)(H,40,48)/t29-,30+/m1/s1 |
| InChIKey | ZIJGVXBDFVHKQP-IHLOFXLRSA-N |
| SMILES | C1CN(CCN1C2=CC=C(C=C2)C(=O)NCC3=C(C=C(C=C3)NC(=O)C4CC4C5=CN=CC=C5)F)C(=O)CCOCCN6C(=O)C=CC6=O |
| Reference | [1]. Karpov AS, et al. Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842. |
