1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Topoisomerase
    ADC Cytotoxin

Dxd (Synonyms: Exatecan derivative)

Cat. No.: HY-13631D Purity: 98.20%
Handling Instructions

Dxd 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).

For research use only. We do not sell to patients.

Dxd Chemical Structure

Dxd Chemical Structure

CAS No. : 1599440-33-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1628 In-stock
Estimated Time of Arrival: December 31
1 mg USD 750 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Dxd 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).

IC50 & Target[1]

Topoisomerase I

0.31 μM (IC50)

In Vitro

Dxd 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). Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s 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 IC50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)[1].

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[1].

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (101.32 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0264 mL 10.1321 mL 20.2642 mL
5 mM 0.4053 mL 2.0264 mL 4.0528 mL
10 mM 0.2026 mL 1.0132 mL 2.0264 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.07 mM); Suspended solution; Need ultrasonic

References
Cell Assay
[1]

Cells are seeded to a 96-well plate at 1,000 cells per well. After overnight incubation, Dxd is added. Cell viability is evaluated after 6 days using a CellTiter-Glo Luminescent Cell Viability Assay. For the detection of HER2 expression in each cell line, cells are incubated on ice for 30 minutes with FITC Mouse IgG1, κ Isotype Control, or anti-HER2/neu FITC. After washing, the labeled cells are analyzed by FACSCalibur. Relative mean fluorescence intensity (rMFI) is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Briefly, each cell suspension or tumor fragment is inoculated subcutaneously into specific pathogen-free female nude mice. When the tumor has grown to an appropriate volume, the tumor-bearing mice are randomized into treatment and control groups based on the tumor volumes, and dosing is initiated on day 0. Each substance (DS-8201a, 1 or 10 mg/kg, i.v.; Dxd is the payload) is administered intravenously to the mice. Tumor growth inhibition (TGI, %) is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

493.48

Formula

C₂₆H₂₄FN₃O₆

CAS No.

1599440-33-1

SMILES

O=C1[[email protected]](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[[email protected]@H]5NC(CO)=O)C(C)=C(F)C=C6N=C4C3=C2)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.20%

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Product Name:
Dxd
Cat. No.:
HY-13631D
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Dxd

Cat. No.: HY-13631D