General Information of This Payload
Payload ID
PAY0LUOFI
Name
FGX8-46
Synonyms
FGX8-46
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Target(s) Human Deoxyribonucleic acid (hDNA)
Structure
Formula
C36H34ClN3O5
Isosmiles
COc1cc2c(cc1OCc1cccc(CC(=O)N3CC(CCl)c4c3cc(O)c3ccccc43)c1)N=CC1CCCCN1C2=O
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
InChIKey
LWFGSXUGQCLYJN-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
624.137
Polar area
91.67
Complexity
45
xlogp Value
6.7553
Heavy Count
45
Rot Bonds
7
Hbond acc
6
Hbond Donor
1
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 1.1 pM
Reh cells
B acute lymphoblastic leukemia
CVCL_1650 
[1]
Half Maximal Inhibitory Concentration (IC50) 22 pM
JVM-2 cells
Mantle cell lymphoma
CVCL_1319 
[1]
Half Maximal Inhibitory Concentration (IC50) 22 pM
SW48 cells
Colon adenocarcinoma
CVCL_1724 
[1]
Half Maximal Inhibitory Concentration (IC50) 434 pM
U-138MG cells
Astrocytoma
CVCL_0020 
[1]
Half Maximal Inhibitory Concentration (IC50) 47 pM
Jurkat cells
T acute lymphoblastic leukemia
CVCL_0065 
[1]
Half Maximal Inhibitory Concentration (IC50) 489 pM
ZR-75-1 cells
Invasive breast carcinoma
CVCL_0588 
[1]
Half Maximal Inhibitory Concentration (IC50) 55 pM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[1]
Half Maximal Inhibitory Concentration (IC50) 69 pM
SW620 cells
Colon adenocarcinoma
CVCL_0547 
[1]
Half Maximal Inhibitory Concentration (IC50) 73 pM
Raji cells
EBV-related Burkitt lymphoma
CVCL_0511 
[1]
Half Maximal Inhibitory Concentration (IC50) 1.3 nM
LIM1215 cells
Colon adenocarcinoma
CVCL_2574 
[1]
Half Maximal Inhibitory Concentration (IC50) 2.72 nM
MCF-7 cells
Invasive breast carcinoma
CVCL_0031 
[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
Click To Hide/Show 5 Activity Data Related to This Level
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.
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.
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.
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.
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.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
References
Ref 1 DNA sequence-selective G-A cross-linking ADC payloads for use in solid tumour therapies. Commun Biol. 2022 Jul 29;5(1):741.

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