Deruxtecan Antibody Conjugated Drug

English name：Deruxtecan
CAS number：1599440-13-7
Another name:
Deruxtecan analog;Deruxtecan;Glycinamide,N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]glycylglycyl-L-phenylalanyl-N-[[2-[[(1S,9S)-9-ethyl-5-fluoro-2,3,9,10,13,15-hexahydro-9-hydroxy-4-methyl-10,13-dioxo-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl]amino]-2-oxoethoxy]methyl]-; MC-GGFG-Exetecan; Deruxtecan（DX-8951);N-((S)-10-Benzyl-1-(((1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3',4':6,7]indolizino[1,2-b]quinolin-1-yl)amino)-1,6,9,12,15-pentaoxo-3-oxa-5,8,11,14-tetraazahexadecan-16-yl)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamide;Drug-Linker Conjugates for ADC, Inhibitor, inhibit, Deruxtecan;N-[(S)-10-Benzyl-1-[[(1S,9S)-9-ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-1,2,3,9,10,12,13,15-octahydrobenzo[de]pyrano[3’,4’:6,7]indolizino[1,2-b]quinolin-1-yl]amino]-1,6,9,12,15-pentaoxo-3-oxa-5,8,11,14-tetraazahexadecan-16-yl]-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl) hexanamide

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Products Description

English name：Deruxtecan

CAS number：1599440-13-7

Molecular formula: C52H56FN9O13

Molecular weight: 1,034.05

EINECS No.:

Related categories:

Peptide; HER 3 antibody conjugated drug-U3-1402; drug substance; antibody conjugated drug intermediates; active small molecule library; chemical reagent; biological reagent; biological; Pharmaceutical; API; ADC

The Mol file: 1599440-13-7.mol

Structural formula:

Drutecan properties

Boiling point: 1491.1 ± 65.0 C (Predicted)

Density: 1.48±0.1g/cm3 (Predicted)

Solubility: DMSO: 67.5 (Chemicalbook maximum concentration mg/mL); 65.28 (maximum concentration mM)

Aciity coefficient (pK a): 11.18 ± 0.40 (Predicted)

Form: solid

Color: White to yellow

InChIKey:XSLGWYQNBQGZTG-MCZRLCSDSA-N

Drutecan use and synthesis method

Antibody-conjugated drugs

Trastuzumab-Drutecan (DS-8201) is an antibody-conjugated drug (ADC) composed of humanized anti-HER 2 monoclonal antibody (Trastuzumab), cleavable tetrapeptide-based linker and cytotoxic topoisomerase I inhibitor (DXd), which prevents cancer cells from replicating DNA and causes cancer cell death from Chemicalbook. Trastuzumab-drutecan has been approved for the treatment of patients with HER 2 positive metastatic breast cancer and gastric cancer. Trastuzumab-Drutecan (DS-8201) was developed by Japanese pharmaceutical companies, and AstraZeneca signed a global cooperative development and commercialization agreement of $6.9 billion with Number Three in March 2019.

Use

HER 3 antibody conjugated drug U3-1402 is an antibody conjugated drug targeting human epidermal growth factor receptor 3 (humanepithelialgrowthfactorreceptor3, HER 3) Chemicalbook developed by Japan. Clinical studies show that it has therapeutic effect in NSCLC patients with various EGFR resistance and unknown resistance mechanisms, and the disease control rate reached 100%. The drug is expected to bring new treatment options for EGFR-TKI resistant NSCLC patients.

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Mechanism of action

U3-1402 relies on the patritumab terminus to efficiently target tumor tissues, reduce systemic exposure of the drug, and ultimately achieve synergistic and attenuated purposes. In tumor tissue, U3-1402 binds to abnormally express HER 3 on the tumor cell surface to form the ChemicalbookHER3U3-1402 complex, which is endocytosed into the connotation body, which is engulfed by lysosomes. U3-1402 is cleaved by cathepsins within the lysosomes and releases the free topoisomerase I inhibitor DXd, thereby inducing DNA damage and apoptosis.

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