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.

Product information

CAS Number: 2241014-82-2

Molecular Weight: 624.66

Formula: C34H33FN6O5

Chemical Name: 4-{4-[3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanoyl]piperazin-1-yl}-N-({2-fluoro-4-[(1S,2S)-2-(pyridin-3-yl)cyclopropaneamido]phenyl}methyl)benzamide

Smiles: O=C(CCN1C(=O)C=CC1=O)N1CCN(CC1)C1C=CC(=CC=1)C(=O)NCC1=CC=C(C=C1F)NC(=O)[C@H]1C[C@@H]1C1=CN=CC=C1

InChiKey: BCYXMGSOTBLGDN-IZLXSDGUSA-N

InChi: InChI=1S/C34H33FN6O5/c35-29-18-25(38-34(46)28-19-27(28)23-2-1-12-36-20-23)6-3-24(29)21-37-33(45)22-4-7-26(8-5-22)39-14-16-40(17-15-39)30(42)11-13-41-31(43)9-10-32(41)44/h1-10,12,18,20,27-28H,11,13-17,19,21H2,(H,37,45)(H,38,46)/t27-,28+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle.

In Vivo:

ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells.

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.

Products are for research use only. Not for human use.