Drug Information
Drug (ID: DG01764) and It's Reported Resistant Information
Name |
Futuximab
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Synonyms |
Futuximab
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Target | . | NOUNIPROTAC | [1] |
Type(s) of Resistant Mechanism of This Drug
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Epidermal growth factor receptor (EGFR) | [1] | |||
Molecule Alteration | Missense mutation | p.R451C (c.1351C>T) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | EGFR signaling pathway | Regulation | hsa01521 | |
In Vitro Model | LIM1215 cells | Colon | Homo sapiens (Human) | CVCL_2574 |
NIH3T3 cells | Embryo | Homo sapiens (Human) | N.A. | |
EGFR cells | N.A. | . | N.A. | |
In Vivo Model | Male BALB/c nude mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay; FACS assay; Crystal violet staining assay | |||
Mechanism Description | Contrary to cetuximab and panitumumab, Sym004 effectively binds to and prevents activation of all the EGFR mutants. Sym004 effectively inhibits proliferation and EGFR downstream signaling in cetuximab-resistant derivatives harboring the S492R and G465R EGFR mutations. Sym004 causes profound and sustained regression in S492R-mutant EGFR and delays tumor growth in G465R-mutant EGFR in vivo. | |||
Key Molecule: Epidermal growth factor receptor (EGFR) | [1] | |||
Molecule Alteration | Missense mutation | p.K467T (c.1400A>C) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | EGFR signaling pathway | Regulation | hsa01521 | |
In Vitro Model | LIM1215 cells | Colon | Homo sapiens (Human) | CVCL_2574 |
NIH3T3 cells | Embryo | Homo sapiens (Human) | N.A. | |
EGFR cells | N.A. | . | N.A. | |
In Vivo Model | Male BALB/c nude mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay; FACS assay; Crystal violet staining assay | |||
Mechanism Description | Contrary to cetuximab and panitumumab, Sym004 effectively binds to and prevents activation of all the EGFR mutants. Sym004 effectively inhibits proliferation and EGFR downstream signaling in cetuximab-resistant derivatives harboring the S492R and G465R EGFR mutations. Sym004 causes profound and sustained regression in S492R-mutant EGFR and delays tumor growth in G465R-mutant EGFR in vivo. |
Colorectal cancer [ICD-11: 2B91]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Epidermal growth factor receptor (EGFR) | [1] | |||
Molecule Alteration | Missense mutation | p.R451C (c.1351C>T) |
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Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | EGFR signaling pathway | Regulation | hsa01521 | |
In Vitro Model | LIM1215 cells | Colon | Homo sapiens (Human) | CVCL_2574 |
NIH3T3 cells | Embryo | Homo sapiens (Human) | N.A. | |
EGFR cells | N.A. | . | N.A. | |
In Vivo Model | Male BALB/c nude mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay; FACS assay; Crystal violet staining assay | |||
Mechanism Description | Contrary to cetuximab and panitumumab, Sym004 effectively binds to and prevents activation of all the EGFR mutants. Sym004 effectively inhibits proliferation and EGFR downstream signaling in cetuximab-resistant derivatives harboring the S492R and G465R EGFR mutations. Sym004 causes profound and sustained regression in S492R-mutant EGFR and delays tumor growth in G465R-mutant EGFR in vivo. | |||
Key Molecule: Epidermal growth factor receptor (EGFR) | [1] | |||
Molecule Alteration | Missense mutation | p.G465R (c.1393G>A) |
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Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | EGFR signaling pathway | Regulation | hsa01521 | |
In Vitro Model | LIM1215 cells | Colon | Homo sapiens (Human) | CVCL_2574 |
NIH3T3 cells | Embryo | Homo sapiens (Human) | N.A. | |
EGFR cells | N.A. | . | N.A. | |
In Vivo Model | Male BALB/c nude mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay; FACS assay; Crystal violet staining assay | |||
Mechanism Description | Contrary to cetuximab and panitumumab, Sym004 effectively binds to and prevents activation of all the EGFR mutants. Sym004 effectively inhibits proliferation and EGFR downstream signaling in cetuximab-resistant derivatives harboring the S492R and G465R EGFR mutations. Sym004 causes profound and sustained regression in S492R-mutant EGFR and delays tumor growth in G465R-mutant EGFR in vivo. | |||
Key Molecule: Epidermal growth factor receptor (EGFR) | [1] | |||
Molecule Alteration | Missense mutation | p.K467T (c.1400A>C) |
||
Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | EGFR signaling pathway | Regulation | hsa01521 | |
In Vitro Model | LIM1215 cells | Colon | Homo sapiens (Human) | CVCL_2574 |
NIH3T3 cells | Embryo | Homo sapiens (Human) | N.A. | |
EGFR cells | N.A. | . | N.A. | |
In Vivo Model | Male BALB/c nude mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay; FACS assay; Crystal violet staining assay | |||
Mechanism Description | Contrary to cetuximab and panitumumab, Sym004 effectively binds to and prevents activation of all the EGFR mutants. Sym004 effectively inhibits proliferation and EGFR downstream signaling in cetuximab-resistant derivatives harboring the S492R and G465R EGFR mutations. Sym004 causes profound and sustained regression in S492R-mutant EGFR and delays tumor growth in G465R-mutant EGFR in vivo. | |||
Key Molecule: Epidermal growth factor receptor (EGFR) | [1] | |||
Molecule Alteration | Missense mutation | p.S492R (c.1476C>A) |
||
Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | EGFR signaling pathway | Regulation | hsa01521 | |
In Vitro Model | LIM1215 cells | Colon | Homo sapiens (Human) | CVCL_2574 |
NIH3T3 cells | Embryo | Homo sapiens (Human) | N.A. | |
EGFR cells | N.A. | . | N.A. | |
In Vivo Model | Male BALB/c nude mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay; FACS assay; Crystal violet staining assay | |||
Mechanism Description | Contrary to cetuximab and panitumumab, Sym004 effectively binds to and prevents activation of all the EGFR mutants. Sym004 effectively inhibits proliferation and EGFR downstream signaling in cetuximab-resistant derivatives harboring the S492R and G465R EGFR mutations. Sym004 causes profound and sustained regression in S492R-mutant EGFR and delays tumor growth in G465R-mutant EGFR in vivo. | |||
Key Molecule: Epidermal growth factor receptor (EGFR) | [2] | |||
Molecule Alteration | Missense mutation | p.S492R (c.1476C>G) |
||
Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | HT29 Cells | Colon | Homo sapiens (Human) | CVCL_A8EZ |
DLD1 cells | Colon | Homo sapiens (Human) | CVCL_0248 | |
SW620 cells | Colon | Homo sapiens (Human) | CVCL_0547 | |
LS1034 cells | Colon | Homo sapiens (Human) | CVCL_1382 | |
COLO205 cells | Colon | Homo sapiens (Human) | CVCL_F402 | |
GEO cells | Colon | Homo sapiens (Human) | CVCL_0271 | |
HCT15 cells | Colon | Homo sapiens (Human) | CVCL_0292 | |
SW480 cells | Colon | Homo sapiens (Human) | CVCL_0546 | |
CaCo2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
HCT116 cells | Colon | Homo sapiens (Human) | CVCL_0291 | |
LOVO cells | Colon | Homo sapiens (Human) | CVCL_0399 | |
LS174T cells | Colon | Homo sapiens (Human) | CVCL_1384 | |
SW948 cells | Colon | Homo sapiens (Human) | CVCL_0632 | |
SW403 cells | Colon | Homo sapiens (Human) | CVCL_0545 | |
SW837 cells | Colon | Homo sapiens (Human) | CVCL_1729 | |
T84 cells | Colon | Homo sapiens (Human) | CVCL_0555 | |
SW1463 cells | Rectum | Homo sapiens (Human) | CVCL_1718 | |
H716 cells | Ascites | Homo sapiens (Human) | CVCL_1581 | |
H508 cells | Abdominal wall | Homo sapiens (Human) | CVCL_1564 | |
SNUC2A cells | Cecum | Homo sapiens (Human) | CVCL_1709 | |
COLO678 cells | Colon | Homo sapiens (Human) | CVCL_1129 | |
GP5D cells | Colon | Homo sapiens (Human) | CVCL_1235 | |
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
WST-1 assay |
References
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