产品描述

Dxd is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC. 

靶点活性

Topoisomerase I    Camptothecins  

体外活性

Dxd shows obviously suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines with IC50s of 26.8, 25.4, and 6.7 ng/mL respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)[1]. 

体内活性

Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM. In HER2 low-expressing ST565 and ST313 models has HER2 IHC 1+/FISH-negative expression[1].

别名

Exatecan derivative for ADC , 化合物Dxd

纯度

98%

分子量

493.48 

分子式

C26H24FN3O6

CAS No.

1599440-33-1

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 50 mg/mL (101.32 mM)

H2O: insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

参考文献

1. Ogitani Y, et al. DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1. Clin Cancer Res. 2016 Oct 15;22(20):5097-5108.

Note

For research use only .