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 IC 50 s of <3 pM and 9 pM, respectively.
In Vitro
ADC-3 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC 50 s of <3 pM and 9 pM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ADC-3 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female scid-beige (SCID bg) mice Dosage: 20 mg/kg Administration: A single intravenous injection (i.v.) for 28 days Result: Significantly inhibited the growth of tumor in mice.