Name: NAMPT inhibitor-linker 1
Rating: 5 (10 reviews)

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HIT ID:HIT212668136
Cas No:2241019-57-6
常用名:NAMPT inhibitor-linker 1
IUPAC:4-(4-{3-[2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethoxy]propanoyl}piperazin-1-yl)-N-({2-fluoro-4-[(1S,2S)-2-(pyridin-3-yl)cyclopropaneamido]phenyl}methyl)benzamide
IUPAC:4-(4-{3-[2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethoxy]propanoyl}piperazin-1-yl)-N-({2-fluoro-4-[(1S,2S)-2-(pyridin-3-yl)cyclopropaneamido]phenyl}methyl)benzamide
InChI key:ZIJGVXBDFVHKQP-IHLOFXLRSA-N

分子式:C36H37FN6O6
分子量:668.726
氢键供体数 (HBD):2
氢键受体数 (HBA):8
LogP:1.7965916
SMILES:Fc1cc(NC(=O)[C@H]2C[C@@H]2c2cccnc2)ccc1CNC(=O)c1ccc(cc1)N1CCN(CC1)C(=O)CCOCCN1C(=O)C=CC1=O |c:50|
SMILES:Fc1cc(NC(=O)[C@H]2C[C@@H]2c2cccnc2)ccc1CNC(=O)c1ccc(cc1)N1CCN(CC1)C(=O)CCOCCN1C(=O)C=CC1=O |c:50|

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

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