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NAMPT inhibitor-linker 1

Names

[ CAS No. ]:
2241019-57-6

[ Name ]:
NAMPT inhibitor-linker 1

Biological Activity

[Description]:

NAMPT inhibitor-linker 1 is a drug-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.

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Antibody-drug Conjugate >> Drug-Linker Conjugates for ADC
Signaling Pathways >> Metabolic Enzyme/Protease >> Nampt

[In Vitro]

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].

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C36H37FN6O6

[ Molecular Weight ]:
668.71

Related Compounds