Dxd
- Product Name
- Dxd
- CAS No.
- 1599440-33-1
- Chemical Name
- Dxd
- Synonyms
- Dxd (Exatecan derivative);Dxd;OQM5SD32BQ;UNII-OQM5SD32BQ;Dxd, 10 mM in DMSO;Exatecan derivative;Exatecan derivative for ADC;D5-Exatecan derivative for ADC;Trastuzumab Deruxtecan (DS-8201a);Dxd (Exatecan derivative for ADC)
- CBNumber
- CB74796647
- Molecular Formula
- C26H24FN3O6
- Formula Weight
- 493.48
- MOL File
- 1599440-33-1.mol
Dxd Property
- 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)
- form
- Solid
- color
- 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
N-Bromosuccinimide Price
- Product number
- CS-0044752
- Product name
- Dxd
- Packaging
- 1mg
- Price
- $520
- Updated
- 2021/12/16
- Product number
- CS-0044752
- Product name
- Dxd
- Packaging
- 5mg
- Price
- $1050
- Updated
- 2021/12/16
- Product number
- CS-0044752
- Product name
- Dxd
- Packaging
- 10mg
- Price
- $1360
- Updated
- 2021/12/16
Dxd Chemical Properties,Usage,Production
Uses
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).
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.
IC 50
Topoisomerase I: 0.31 μM (IC50); Camptothecins
References
[1] Ogitani Y, et al. DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1. Clin Cancer Res. 2016 Oct 15;22(20):5097-5108. DOI:10.1158/1078-0432.CCR-15-2822
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View Lastest Price from Dxd manufacturers
- Product
- Dxd 1599440-33-1
- Price
- US $3.00-9.00/KG
- Min. Order
- 0.1KG
- Purity
- 99%
- Supply Ability
- g-kg-tons, free sample is available
- Release date
- 2025-06-27
- Product
- Dxd 1599440-33-1
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1Ton
- Release date
- 2022-10-13