2241014-82-2

Name	NAMPT inhibitor-linker 2
CAS	2241014-82-2
Molecular Formula	C34H33FN6O5
MDL Number	MFCD31813687
Molecular Weight	624.66
MOL File	2241014-82-2.mol

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]-

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Chemical Properties

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

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

Supplier

Fan De(Beijing) Biotechnology Co., Ltd.

Telephone 15911056312

Websitehttp://www.bio-fount.com/

Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.

Telephone025-025-66113011 15955137747

Websitehttp://www.aikonchem.com

SuZhou GoodChemTech Co., Ltd

Telephone18136139868; 18136139868

Website

Shandong Dayou Pharmaceutical Research and Development Co., Ltd.

Telephonehanfangpharma@126.com 15165037910

Websitehttps://hanfangpharma@126.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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