DX-8951衍生物
DX-8951衍生物 性质
| 沸点 | 957.9±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.57±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO:40.0(最大浓度 mg/mL);81.06(最大浓度 mM) |
| 酸度系数(pKa) | 11.18±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | Off-white to yellow |
| InChIKey | PLXLYXLUCNZSAA-QLXKLKPCSA-N |
| SMILES | C(N[C@@H]1C2C3C(N=C4C5N(C(=O)C6COC(=O)[C@@](CC)(O)C=6C=5)CC4=2)=CC(F)=C(C)C=3CC1)(=O)CO |
DX-8951衍生物 用途与合成方法
|
Topoisomerase I 0.31 μM (IC 50 ) |
Camptothecins
|
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC 50 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 IC 50 s 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 IC 50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC 50 , >10,000 ng/mL).
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.
DX-8951衍生物 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-09-15 | HY-13631D | DX-8951衍生物 | 1599440-33-1 | 5mg | 640 |
| 2026-09-15 | HY-13631D | DX-8951衍生物 | 1599440-33-1 | 10 mM * 1 mLin DMSO | 695 |
