| Identification | Back Directory | [Name]
NAMPT inhibitor-linker 2 | [CAS]
2241014-82-2 | [Synonyms]
NAMPT inhibitor-linker 2
Benzamide, 4-[4-[3-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxopropyl]-1-piperazinyl]-N-[[2-fluoro-4-[[[(1S,2S)-2-(3-pyridinyl)cyclopropyl]carbonyl]amino]phenyl]methyl]- | [Molecular Formula]
C34H33FN6O5 | [MDL Number]
MFCD31813687 | [MOL File]
2241014-82-2.mol | [Molecular Weight]
624.66 |
| Chemical Properties | Back Directory | [Boiling point ]
940.2±65.0 °C(Predicted) | [density ]
1.395±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.91±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively. | [in vivo]
ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells[1]. | Animal Model: | Female scid-beige (SCID bg) mice[1] | | Dosage: | 20 mg/kg | | Administration: | A single intravenous injection (i.v.) for 28 days | | Result: | Significantly inhibited the growth of tumor in mice. |
| [IC 50]
Traditional Cytotoxic Agents | [References]
[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. DOI:10.1021/acsmedchemlett.8b00254 |
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MedChemExpress
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