Dxd
- CAS No.
- 1599440-33-1
- Chemical Name:
- Dxd
- Synonyms
- Dxd (Exatecan derivative);Dxd;OQM5SD32BQ;UNII-OQM5SD32BQ;Exatecan derivative;Exatecan derivative for ADC;Trastuzumab Deruxtecan (DS-8201a);Dxd,Inhibitor,ADC,ADC Cytotoxin,inhibit,Topoisomerase,HER2-targeting,ADC Payload;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',);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',)
- CBNumber:
- CB74796647
- Molecular Formula:
- C26H24FN3O6
- Molecular Weight:
- 493.48
- MDL Number:
- MFCD31657444
- MOL File:
- 1599440-33-1.mol
| Boiling point | 957.9±65.0 °C(Predicted) |
|---|---|
| Density | 1.57±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO:40.0(Max Conc. mg/mL);81.06(Max Conc. mM) |
| pka | 11.18±0.40(Predicted) |
| FDA UNII | OQM5SD32BQ |
Dxd Chemical Properties,Uses,Production
Biological Activity
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor with IC50 value of 0.31 μM, which can be used as a payload for an antibody-drug conjugate ADC (DS-8201a) targeting HER2.
in vitro
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
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.
Dxd Preparation Products And Raw materials
Raw materials
Preparation Products
Dxd Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32715 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Fuxin Pharmaceutical | +86-021-021-50872116 +8613122107989 | contact@fuxinpharm.com | China | 10297 | 58 |
| ENBRIDGE PHARMTECH CO., LTD. | +8613812269233 | tinayang@enbridgepharm.com | China | 303 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| Hangzhou Huarong Pharm Co., Ltd. | 571-86758373 +8613588754946 | sales@huarongpharm.com | CHINA | 3149 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| BTC pharm India | +918790379245 | banny.janga@btcpharm.com | India | 1269 | 58 |
