NAMPT inhibitor-linker 2

Modify Date: 2024-01-09 23:42:10

NAMPT inhibitor-linker 2 Structure
NAMPT inhibitor-linker 2 structure
Common Name NAMPT inhibitor-linker 2
CAS Number 2241014-82-2 Molecular Weight 624.66
Density N/A Boiling Point N/A
Molecular Formula C34H33FN6O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of NAMPT inhibitor-linker 2


NAMPT inhibitor-linker 2 is a drug-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.

 Names

Name NAMPT inhibitor-linker 2

 NAMPT inhibitor-linker 2 Biological Activity

Description NAMPT inhibitor-linker 2 is a drug-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.
Related Catalog
In Vitro ADC-4 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[1]. ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle[1]. Cell Proliferation Assay[1] Cell Line: GIST-T1 cells Concentration: 0.1 pM-10 nM Incubation Time: 144 hours Result: Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.
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.
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 C34H33FN6O5
Molecular Weight 624.66
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