产品名称 | indusatumab vedotin |
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CAS编号和信息 | Ab175563 |
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IMGT/mAb-DB | 532 |
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Target ID | 1750 | ||||||||||||||||||||||||
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名称 | Guanylyl cyclase-C | ||||||||||||||||||||||||
缩写名 | GC-C | ||||||||||||||||||||||||
家族 | Transmembrane guanylyl cyclases | ||||||||||||||||||||||||
别名 | GHSR-1a | ||||||||||||||||||||||||
基因和蛋白信息 |
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Ensembl Gene | ENSG00000070019 (Hs) , ENSMUSG00000042638 (Mm) , ENSRNOG00000009031 (Rn) | ||||||||||||||||||||||||
Entrez Gene | 14917 (Mm) , 25711 (Rn) , 2984 (Hs) | ||||||||||||||||||||||||
OMIM | 601330 (Hs) | ||||||||||||||||||||||||
Protein GI | 6981000 (Rn) , 222080083 (Hs) , 187960051 (Mm) | ||||||||||||||||||||||||
UniProtKB | P23897 (Rn) , P25092 (Hs) , Q3UWA6 (Mm) | ||||||||||||||||||||||||
RefSeq Nucleotide | NM_001127318 (Mm) , NM_004963 (Hs) , NM_013170 (Rn) | ||||||||||||||||||||||||
RefSeq Protein | NP_001120790 (Mm) , NP_004954 (Hs) , NP_037302 (Rn) , NP_659504 (Mm) | ||||||||||||||||||||||||
Orphanet | 317726 (Hs) | ||||||||||||||||||||||||
DrugBank Target | P25092 (Hs) | ||||||||||||||||||||||||
CATH/Gene3D | 3.30.70.1230 (N/A) | ||||||||||||||||||||||||
ChEMBL Target | CHEMBL1795197 (Hs) |
Ligand ID | 8718 |
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名称 | indusatumab vedotin |
别名 | 5F9vcMMAE |
类别 | Antibody |
学名 | 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide |
生物活性评价 |
The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in |
评价 |
Indusatumab vedotin was a clinical lead antibody-drug conjugate (ADC). It comprises an anti-guanylate cyclase 2C (GUCY2C) antibody linked to the synthetic antineoplastic toxin monomethyl auristatin E (MMAE, aka vedotin; PubChem CID 11542188). Peptide sequence information for this antibody is available from its IMGT/mAb-DB record. A BLAST search of patented peptide sequences reveals that the heavy and light chain variable regions of indusatumab are identical to SEQ ID NO: 18 and SEQ ID NO: 20 respectively, from patent US8785600 B2 |
单字母多肽序列 | |
三字母多肽序列 | |
翻译后修饰 | |
化学修饰 | |
临床描述 |
The purpose of this study is to assess the efficacy, safety and tolerability of MLN0264 in patients with advanced or metastatic guanylyl cyclase C (GCC)-positive adenocarcinoma of the pancreas. This is an Open-Label, Multicenter, Dose Escalation, First-in-Human Study of MLN0264 in Adult Patients With Advanced Gastrointestinal Malignancies Expressing Guanylyl Cyclase C. |
来源公司 |
Takeda Takeda |
1. Lucas KA, Pitari GM, Kazerounian S, Ruiz-Stewart I, Park J, Schulz S, Chepenik KP, Waldman SA. (2000) Guanylyl cyclases and signaling by cyclic GMP.. Pharmacol Rev, 52 (3): (375-414). [PMID:10977868] |
2. Schulz S, Hyslop T, Haaf J, Bonaccorso C, Nielsen K, Witek ME, Birbe R, Palazzo J, Weinberg D, Waldman SA. (2006) A validated quantitative assay to detect occult micrometastases by reverse transcriptase-polymerase chain reaction of guanylyl cyclase C in patients with colorectal cancer.. Clin Cancer Res, 12 (15): (4545-52). [PMID:16899600] |
3. Birbe R, Palazzo JP, Walters R, Weinberg D, Schulz S, Waldman SA. (2005) Guanylyl cyclase C is a marker of intestinal metaplasia, dysplasia, and adenocarcinoma of the gastrointestinal tract.. Hum Pathol, 36 (2): (170-9). [PMID:15754294] |
4. Almhanna K, Miron ML, Wright D, Gracian AC, Hubner RA, Van Laethem JL, López CM, Alsina M, Mu?oz FL, Bendell J et al.. (2017) Phase II study of the antibody-drug conjugate TAK-264 (MLN0264) in patients with metastatic or recurrent adenocarcinoma of the stomach or gastroesophageal junction expressing guanylyl cyclase C.. Invest New Drugs, 35 (2): (235-241). [PMID:28188407] |
5. Almhanna K, Wright D, Mercade TM, Van Laethem JL, Gracian AC, Guillen-Ponce C, Faris J, Lopez CM, Hubner RA, Bendell J et al.. (2017) A phase II study of antibody-drug conjugate, TAK-264 (MLN0264) in previously treated patients with advanced or metastatic pancreatic adenocarcinoma expressing guanylyl cyclase C.. Invest New Drugs, 35 (5): (634-641). [PMID:28527133] |
6. Carrithers SL, Barber MT, Biswas S, Parkinson SJ, Park PK, Goldstein SD, Waldman SA. (1996) Guanylyl cyclase C is a selective marker for metastatic colorectal tumors in human extraintestinal tissues.. Proc Natl Acad Sci USA, 93 (25): (14827-32). [PMID:8962140] |