Deruxtecan
Deruxtecan analog
CAS: 1599440-13-7
Molecular Formula: C52H56FN9O13
Deruxtecan - Names and Identifiers
| Name | Deruxtecan analog |
| Synonyms | Deruxtecan MC-GGFG-Exetecan Deruxtecan analog |
| CAS | 1599440-13-7 |
Deruxtecan - Physico-chemical Properties
| Molecular Formula | C52H56FN9O13 |
| Molar Mass | 1034.05 |
| Density | 1.48±0.1 g/cm3(Predicted) |
| Boling Point | 1491.1±65.0 °C(Predicted) |
| pKa | 11.18±0.40(Predicted) |
| Storage Condition | -20℃ |
| Use | Uses HER3 antibody conjugate drug U3-1402 is an antibody conjugate drug targeting human epidermal growth factor receptor 3(humanepithelialgrowthfactorreceptor3,HER3) developed by Japan's First Sankyo Company. Clinical studies have shown that it is resistant to various EGFR and NSCLC patients with unknown drug resistance mechanism have therapeutic effects, and the disease control rate is 100%. The drug is expected to bring new treatment options for EGFR-TKI drug-resistant NSCLC patients. |
| Target | Camptothecins |
Deruxtecan - Reference
| Reference Show more | 1: Takegawa N, Tsurutani J, Kawakami H, Yonesaka K, Kato R, Haratani K, Hayashi H, Takeda M, Nonagase Y, Maenishi O, Nakagawa K. [fam-] trastuzumab deruxtecan, antitumor activity is dependent on HER2 expression level rather than on HER2 amplification. Int J Cancer. 2019 May 14. doi: 10.1002/ijc.32408. [Epub ahead of print] PubMed PMID: 31087550. 2: Shitara K, Iwata H, Takahashi S, Tamura K, Park H, Modi S, Tsurutani J, Kadowaki S, Yamaguchi K, Iwasa S, Saito K, Fujisaki Y, Sugihara M, Shahidi J, Doi T. Trastuzumab deruxtecan (DS-8201a) in patients with advanced HER2-positive gastric cancer: a dose-expansion, phase 1 study. Lancet Oncol. 2019 Jun;20(6):827-836. doi: 10.1016/S1470-2045(19)30088-9. Epub 2019 Apr 29. Erratum in: Lancet Oncol. 2019 May 10;:. PubMed PMID: 31047804. 3: Tamura K, Tsurutani J, Takahashi S, Iwata H, Krop IE, Redfern C, Sagara Y, Doi T, Park H, Murthy RK, Redman RA, Jikoh T, Lee C, Sugihara M, Shahidi J, Yver A, Modi S. Trastuzumab deruxtecan (DS-8201a) in patients with advanced HER2-positive breast cancer previously treated with trastuzumab emtansine: a dose-expansion, phase 1 study. Lancet Oncol. 2019 Jun;20(6):816-826. doi: 10.1016/S1470-2045(19)30097-X. Epub 2019 Apr 29. Erratum in: Lancet Oncol. 2019 May 10;:. PubMed PMID: 31047803. 4: Rinnerthaler G, Gampenrieder SP, Greil R. HER2 Directed Antibody-Drug-Conjugates beyond T-DM1 in Breast Cancer. Int J Mol Sci. 2019 Mar 5;20(5). pii: E1115. doi: 10.3390/ijms20051115. Review. PubMed PMID: 30841523; PubMed Central P |
Deruxtecan - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.967 ml | 4.835 ml | 9.671 ml |
| 5 mM | 0.193 ml | 0.967 ml | 1.934 ml |
| 10 mM | 0.097 ml | 0.484 ml | 0.967 ml |
| 5 mM | 0.019 ml | 0.097 ml | 0.193 ml |
Last Update：2024-01-02 23:10:35
Deruxtecan - Mechanism of action
U3-1402 depends on the patritumab end to target tumor tissues efficiently, reduce systemic exposure of drugs, and finally achieve the purpose of synergistic and toxic reduction. In tumor tissue, the U3-1402 combines with the abnormal expression of HER3 on the surface of tumor cells to form HER3 U3-1402 complex, which is endocytosed into the connotation body, which is swallowed by lysosomes. The U3-1402 is cleaved by cathepsin within the lysosome and releases the free topoisomerase I inhibitor DXd, thereby inducing DNA damage and apoptosis.
Last Update：2024-04-09 21:31:49
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