2. Cell Cycle/DNA Damage Antibody-drug Conjugate/ADC Related
  3. Topoisomerase ADC Cytotoxin
  4. Dxd

Dxd  (Synonyms: Exatecan derivative for ADC)

Cat. No.: HY-13631D Purity: ≥99.0%
COA Handling Instructions

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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).

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 85 In-stock
10 mg USD 120 In-stock
50 mg USD 290 In-stock
100 mg USD 400 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Dxd:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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).

IC50 & Target[1]

Topoisomerase I

0.31 μM (IC50)

Camptothecins

 

In Vitro

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). 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].

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

Dxd Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

493.48

Formula

C26H24FN3O6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (81.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

COA (261 KB) HNMR (266 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0264 mL 10.1321 mL 20.2642 mL 50.6606 mL
5 mM 0.4053 mL 2.0264 mL 4.0528 mL 10.1321 mL
10 mM 0.2026 mL 1.0132 mL 2.0264 mL 5.0661 mL
15 mM 0.1351 mL 0.6755 mL 1.3509 mL 3.3774 mL
20 mM 0.1013 mL 0.5066 mL 1.0132 mL 2.5330 mL
25 mM 0.0811 mL 0.4053 mL 0.8106 mL 2.0264 mL
30 mM 0.0675 mL 0.3377 mL 0.6755 mL 1.6887 mL
40 mM 0.0507 mL 0.2533 mL 0.5066 mL 1.2665 mL
50 mM 0.0405 mL 0.2026 mL 0.4053 mL 1.0132 mL
60 mM 0.0338 mL 0.1689 mL 0.3377 mL 0.8443 mL
80 mM 0.0253 mL 0.1267 mL 0.2533 mL 0.6333 mL
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Dxd Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dxd1599440-33-1Exatecan derivative for ADCTopoisomeraseADC CytotoxinADC PayloadHER2-targetingADCInhibitorinhibitorinhibit

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