Name: NAMPT inhibitor-linker 2
Rating: 5 (10 reviews)

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HIT ID:HIT212668137
Cas No:2241014-82-2
常用名:NAMPT inhibitor-linker 2
IUPAC: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
IUPAC: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
InChI key:BCYXMGSOTBLGDN-IZLXSDGUSA-N

分子式:C34H33FN6O5
分子量:624.673
氢键供体数 (HBD):2
氢键受体数 (HBA):7
LogP:1.8435671
SMILES:Fc1cc(NC(=O)[C@H]2C[C@@H]2c2cccnc2)ccc1CNC(=O)c1ccc(cc1)N1CCN(CC1)C(=O)CCN1C(=O)C=CC1=O |c:47|
SMILES:Fc1cc(NC(=O)[C@H]2C[C@@H]2c2cccnc2)ccc1CNC(=O)c1ccc(cc1)N1CCN(CC1)C(=O)CCN1C(=O)C=CC1=O |c:47|

NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

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