DX-8951衍生物
| 中文名称 | DX-8951衍生物 |
|---|---|
| 中文同义词 | DX-8951衍生物;毒素;依喜替康代谢物;依喜替康衍生物;化合物DXD;N-((1S,9S)-9-乙基-5-氟-9-羟基-4-甲基-10,13-二氧代-2,3,9,10,13,15-六氢-1H,12H-苯并[DE]吡喃并[3',4':6,7]吲哚嗪并[1,2-B]喹啉-1-基)-2-羟基乙酰胺;DXD抗体;DXD,DNA TOPOISOMERASE I 抑制剂 |
| 英文名称 | Dxd |
| 英文同义词 | Dxd;Exatecan derivative;N-[(1S,9S)-9-Ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl]-2-hydroxyacetamide;Exatecan derivative for ADC;Acetamide, N-[(1S,9S)-9-ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl]-2-hydroxy-;OQM5SD32BQ;UNII-OQM5SD32BQ;Dxd (Exatecan derivative) |
| CAS号 | 1599440-33-1 |
| 分子式 | C26H24FN3O6 |
| 分子量 | 493.48 |
| EINECS号 | |
| 相关类别 | 细胞毒素;标准品;生物试剂;化学试剂 |
| Mol文件 | 1599440-33-1.mol |
| 结构式 |  |
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) |
|
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-13631D | Dxd | 1 mg | 1142元 | |
| 2024/04/30 | HY-13631D | DX-8951衍生物 Dxd | 1599440-33-1 | 5mg | 1400元 |