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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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0044752
Product name
Dxd
Packaging
1mg
Price
$520
Updated
2021/12/16
ChemScene
Product number
CS-0044752
Product name
Dxd
Packaging
5mg
Price
$1050
Updated
2021/12/16
ChemScene
Product number
CS-0044752
Product name
Dxd
Packaging
10mg
Price
$1360
Updated
2021/12/16
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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

Dxd Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Dxd manufacturers

ZHENGZHOU JIUYI TIME NEW MATERIALS CO,.LTD
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
Henan Aochuang Chemical Co.,Ltd.
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

1599440-33-1, DxdRelated Search:


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  • Exatecan derivative
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  • Dxd (Exatecan derivative)
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  • UNII-OQM5SD32BQ
  • N-((1S,9S)-9-Ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl)-2-hydroxyacetamide
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  • Dxd, 10 mM in DMSO
  • D5-Exatecan derivative for ADC
  • 1599440-33-1
  • 599440-33-1