OQM5SD32BQ
Dxd
CAS: 1599440-33-1
Molecular Formula: C26H24FN3O6
OQM5SD32BQ - Names and Identifiers
| Name | Dxd |
| Synonyms | Dxd OQM5SD32BQ UNII-OQM5SD32BQ Exatecan derivative Dxd (Exatecan derivative) Exatecan derivative for ADC |
| CAS | 1599440-33-1 |
OQM5SD32BQ - Physico-chemical Properties
| Molecular Formula | C26H24FN3O6 |
| Molar Mass | 493.48 |
| Density | 1.57±0.1 g/cm3(Predicted) |
| Boling Point | 957.9±65.0 °C(Predicted) |
| pKa | 11.18±0.40(Predicted) |
| Use | Bioactive Dxd (Exatecan derivative for ADC) is an effective DNA topoisomerase I inhibitor with an IC50 value of 0.31 μM, which can be used as the payload of antibody-coupled drug ADC (DS-8201a) targeting HER2. |
| In vitro study | 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). |
| In vivo study | 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. |
OQM5SD32BQ - Uses and synthesis methods
Target
Topoisomerase I
0.31 μM (IC 50 )
Camptothecins
in vitro studies
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).
In vivo studies
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.
Last Update：2024-04-09 20:48:19
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Product Name: Exatecan Impurity 1 Request for quotation
CAS: 1599440-33-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 1599440-33-1
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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