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Trastuzumab deruxtecan

Catalog No. T36646 CAS 1826843-81-5

Synonyms: DS-8201a, VRN-101099, DS 8201, T-DXd

Trastuzumab deruxtecan (T-DXd) is an antibody-activated molecule coupling (ADC) with anticancer and antitumour activity.Trastuzumab deruxtecan has been shown to have an ameliorative effect in HER2-positive breast and gastric cancers.

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Trastuzumab deruxtecan Chemical Structure

Trastuzumab deruxtecan, CAS 1826843-81-5

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Description	Trastuzumab deruxtecan (T-DXd) is an antibody-activated molecule coupling (ADC) with anticancer and antitumour activity.Trastuzumab deruxtecan has been shown to have an ameliorative effect in HER2-positive breast and gastric cancers.
Targets&IC50	Axl(KPL-4 cells):109.7 pM
In vitro	Trastuzumab deruxtecan, at concentrations ranging from 1 pM to 10 nM for 5 days (solution), inhibits the growth of HER2-positive KPL-4 cells, with an IC50 of 109.7 pM[4].Trastuzumab deruxtecan, at 10 nM for 5 days (solution), shows bystander killing effects in HER2-negative MDA-MB-468 cells[4].
In vivo	Trastuzumab deruxtecan (solution) at a single intravenous dose of 3 mg/kg exhibits antitumor activity against not only HER2-positive tumors but also HER2-negative tumors under the co-inoculated condition[4].Trastuzumab deruxtecan (solution) administered intravenously on days 0 and 7 at a dose of 10 mg/kg inhibits tumor growth in the EMT6-hHER2 syngeneic mouse model[3].Female BALB/c nude mice injected with NCI‐N87 and MDA‐MB‐468‐Luc cells[4]

Synonyms	DS-8201a, VRN-101099, DS 8201, T-DXd
Molecular Weight	N/A
Formula	N/A
CAS No.	1826843-81-5

Storage

store at low temperature

store at -20°C

References and Literature

1. Kumagai K, et al. Interstitial pneumonitis related to trastuzumab deruxtecan, a human epidermal growth factor receptor 2-targeting Ab-drug conjugate, in monkeys. Cancer Sci. 2020 Dec;111(12):4636-4645. 2. Iwata TN, et, al. [Fam-] trastuzumab deruxtecan (DS-8201a)-induced antitumor immunity is facilitated by the anti-CTLA-4 antibody in a mouse model. PLoS One. 2019 Oct 1;14(10):e0222280. 3. Ogitani Y, et, al. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46. 4. Kotani D, et, al. Trastuzumab deruxtecan for the treatment of patients with HER2-positive gastric cancer. Ther Adv Med Oncol. 2021 Jan 7;13:1758835920986518.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Trastuzumab deruxtecan 1826843-81-5 Others DS-8201a VRN-101099 DS 8201 T-DXd inhibitor inhibit

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