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Deruxtecan

SKU: orb1308394

Description

Deruxtecan is a drug-linker conjugate featuring a DXd payload connected via a maleimide-GGFG peptide linker. It is a key component in the synthesis of ADCs like DS-8201 and U3-1402, enabling targeted cytotoxicity research in both in vitro and in vivo cancer models.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Deruxtecan

Key Properties

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CAS Number1599440-13-7
MW1034.05
Purity98.20%
FormulaC52H56FN9O13
SMILESCC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cc(F)c(C)c5CC[C@H](NC(=O)COCNC(=O)CNC(=O)[C@H](Cc6ccccc6)NC(=O)CNC(=O)CNC(=O)CCCCCN6C(=O)C=CC6=O)c(c3Cn1c2=O)c45
TargetDrug-Linker Conjugates for ADC,PROTAC Linker
Solubility10% DMSO+90% Corn Oil:2 mg/mL (1.93 mM);DMSO:262 mg/mL (253.37 mM)

Bioactivity

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In Vivo
METHODS: Mouse models of HER2-positive tumors were treated with Trastuzumab Deruxtecan (DS-8201a) (10 mg/kg, i.v), and anti-PD-1 antibodies were also used in combination to evaluate synergistic effects, monitor tumor growth, and perform flow cytometric analysis. To analyze the composition and function of immune cells in tumors. RESULTS Trastuzumab Deruxtecan (DS-8201a) significantly inhibited tumor growth and in some cases resulted in complete remission (CR); mice that achieved CR after treatment were able to reject revaccinated CT26.WT-hHER2 cells as well as non-transgenic CT26.WT-mock cells, showing the formation of immune memory; Trastuzumab Deruxtecan (DS-8201a) increased the number of CD8+ T cells infiltrating within the tumor, upregulated the expression of CD86, an activation marker of dendritic cells (DCs), and enhanced Expression of PD-L1 and MHC class I molecules on tumor cells; the combination of Trastuzumab Deruxtecan (DS-8201a) and an anti-PD-1 antibody is more effective in inhibiting tumor growth than monotherapy, suggesting that Trastuzumab Deruxtecan (DS-8201a) may Promote anti-tumor immunity by activating the immune system and upregulating PD-L1 expression.
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In Vitro
METHODS: Trastuzumab Deruxtecan (DS-8201a) was administered at scalar concentrations of 0.005 μg/mL, 0.05 μg/mL, 0.2 μg/mL, 0.5 μg/mL, and 2.0 μg/mL. Three days after drug treatment, whole cells were harvested, centrifuged, and stained with propidium iodide (2 μl of 500 μg/mL stock solution in phosphate-buffered saline (PBS)). RESULTS DS-8201 induced cell death with a mean IC50 value of 0.03 μM (p<0.0001); statistically significant differences were observed in 3+ HER2/neu ovarian CS cell lines, where the mean IC50 of DS-8201a was 0.03 μM; and in representative HER2/neu non-expressing cell lines, where the mean IC50 of DS-8201a was 20.02 μM.
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Storage & Handling

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Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Inhibitor, inhibit, Camptothecins, DrugLinkerConjugatesforADC, DrugLinker Conjugates for ADC, Deruxtecan, Drug-Linker Conjugates for ADC

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Compound Identifiers

PubChem CID
118305111 ↗

Key Properties

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No computed properties available.

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Deruxtecan (orb1308394)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 90.00
5 mg
$ 140.00
10 mg
$ 190.00
25 mg
$ 310.00
50 mg
$ 460.00
100 mg
$ 680.00
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