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抑制剂/激活剂

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凋亡与自噬

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Dxd

Dxd (Exatecan derivative for ADC) 是一种有效的 DNA topoisomerase I 抑制剂，IC50 值为 0.31 μM，可用作靶作用于 HER2 的抗体偶联药物 ADC (DS-8201a) 的有效载荷。

货号：
TK0246
规格：

1mg

5mg
价格：
￥0.00

产品参数

CAS No.	1599440-33-1
生物活性	Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
分子式	C26H24FN3O6
分子量	493.48
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	-20°C, stored under nitrogen
溶解性数据	DMSO : 7.14 mg/mL (14.47 mM; Need ultrasonic)
体内研究	DS-8201a (Dxd is the payload, 10 mg/kg, i.v.) shows potent antitumor activity in HER2-positive models with KPL4, JIMT-1, and Capan-1 and in HER2 low-expressing ST565 and ST313 models with HER2 IHC 1+/FISH-negative expression.
体外研究	Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). 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, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC50 values 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).
文献	•Pharmaceuticals. 2021, 14(3), 247. •Patent. US20210009719A1.
纯度及产品资料	98%

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