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Dxd

Cat. No. M13744
Dxd Structure
Synonym:

Exatecan derivative for ADC

Size Price Availability Quantity
5mg USD 612  USD612 In stock
10mg USD 1020  USD1020 In stock
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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 493.48
CAS Number 1599440-33-1
Solubility (25°C) DMSO 7.14 mg/mL
Storage -20°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ibrahim Azar, et al. Lung Cancer (Auckl). Spotlight on Trastuzumab Deruxtecan (DS-8201,T-DXd) for HER2 Mutation Positive Non-Small Cell Lung Cancer

[2] Peter Sidaway. Nat Rev Clin Oncol. T-DXd effective in HER2-mutant NSCLC

[3] Heidi M Haikala, et al. Cancer Res. EGFR Inhibition Enhances the Cellular Uptake and Antitumor-Activity of the HER3 Antibody-Drug Conjugate HER3-DXd

[4] Pasi A Jnne, et al. Cancer Discov. Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor-Resistant, EGFR-Mutated Non-Small Cell Lung Cancer

[5] Hiromi Okamoto, et al. Xenobiotica. Pharmacokinetics of trastuzumab deruxtecan (T-DXd), a novel anti-HER2 antibody-drug conjugate, in HER2-positive tumour-bearing mice

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Keywords: Dxd, Exatecan derivative for ADC supplier, Topoisomerase, inhibitors, activators


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