NAMPT inhibitor-linker 1

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NAMPT inhibitor-linker 1 

NAMPT inhibitor-linker 1 为 ADC 的一部分,由一种 NAMPT 的抑制剂作为有效载荷和一个连接物组成。ADC-3 由一个 NAMPT inhibitor-linker 1 和一个 anti-c-Kit 单克隆抗体组成,对表达 c-Kit 的细胞具有抑制作用,比如 GIST-T1 和 NCI-H526 细胞,IC50 值分别为 <3 pM 和 9 pM。

NAMPT inhibitor-linker 1

NAMPT inhibitor-linker 1 Chemical Structure

CAS No. : 2241019-57-6

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生物活性

NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.

IC50 & Target

Traditional Cytotoxic Agents

 

体外研究
(In Vitro)

ADC-3 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <3 pm and 9 pm, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

ADC-3 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

668.71

Formula

C36H37FN6O6

CAS 号

2241019-57-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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