| Chemical Properties | Back Directory | [Boiling point ]
960.3±65.0 °C(Predicted) | [density ]
1.372±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.91±0.70(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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. | [in vivo]
ADC-3 (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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