Payload Information
General Information of This Payload
Payload ID | PAY0LUOFI |
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Name | FGX8-46 |
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Synonyms |
FGX8-46
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Target(s) | Human Deoxyribonucleic acid (hDNA) | |||||
Structure | ||||||
Formula | C36H34ClN3O5 |
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Isosmiles | COc1cc2c(cc1OCc1cccc(CC(=O)N3CC(CCl)c4c3cc(O)c3ccccc43)c1)N=CC1CCCCN1C2=O |
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InChI |
InChI=1S/C36H34ClN3O5/c1-44-32-15-28-29(38-19-25-9-4-5-12-39(25)36(28)43)16-33(32)45-21-23-8-6-7-22(13-23)14-34(42)40-20-24(18-37)35-27-11-3-2-10-26(27)31(41)17-30(35)40/h2-3,6-8,10-11,13,15-17,19,24-25,41H,4-5,9,12,14,18,20-21H2,1H3
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InChIKey |
LWFGSXUGQCLYJN-UHFFFAOYSA-N
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Pharmaceutical Properties | Molecule Weight |
624.137 |
Polar area |
91.67 |
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Complexity |
45 |
xlogp Value |
6.7553 |
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Heavy Count |
45 |
Rot Bonds |
7 |
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Hbond acc |
6 |
Hbond Donor |
1 |
The activity data of This Payload
Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
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Half Maximal Inhibitory Concentration (IC50) | 1.1 | pM |
Reh cells
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B acute lymphoblastic leukemia
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 22 | pM |
JVM-2 cells
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Mantle cell lymphoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 22 | pM |
SW48 cells
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Colon adenocarcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 434 | pM |
U-138MG cells
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Astrocytoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 47 | pM |
Jurkat cells
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T acute lymphoblastic leukemia
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 489 | pM |
ZR-75-1 cells
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Invasive breast carcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 55 | pM |
SK-BR-3 cells
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Breast adenocarcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 69 | pM |
SW620 cells
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Colon adenocarcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 73 | pM |
Raji cells
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EBV-related Burkitt lymphoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 1.3 | nM |
LIM1215 cells
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Colon adenocarcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 2.72 | nM |
MCF-7 cells
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Invasive breast carcinoma
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[1] |
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Cetuximab- (FGX16-11) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 42.79% (Day 36) | High EGFR expression (EGFR+++) | ||
Method Description |
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg.
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In Vivo Model | Colon cancer CDX model | ||||
In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 63.01% (Day 36) | High EGFR expression (EGFR+++) | ||
Method Description |
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 5 mg/kg.
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In Vivo Model | Colon cancer CDX model | ||||
In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.22% (Day 36) | High EGFR expression (EGFR+++) | ||
Method Description |
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 10 mg/kg.
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In Vivo Model | Colon cancer CDX model | ||||
In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.98% (Day 36) | High EGFR expression (EGFR+++) | ||
Method Description |
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 20 mg/kg.
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In Vivo Model | Colon cancer CDX model | ||||
In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 36) | High EGFR expression (EGFR+++) | ||
Method Description |
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 40 mg/kg.
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In Vivo Model | Colon cancer CDX model | ||||
In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 |
References
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