General Information of This Payload (ID: PAY0IJNBT)
Name
I034
Target IKZF1/3
Structure
Isosmiles
OC1(CCC1)C(N2CCC(N3C=C(CC4=CC=C5N(C(C6=CC=CC4=C56)=O)C7CCC(NC7=O)=O)C=N3)CC2)=O
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 0.007 nM
NCI-H929 cells
Multiple myeloma
CVCL_1600 
Half Maximal Degradation Concentration (DC50) 0.024 nM
NCI-H929 cells
Multiple myeloma
CVCL_1600 
Half Maximal Degradation Concentration (DC50) <0.05 nM
PBMC cells
Normal
CVCL_0140 
Half Maximal Degradation Concentration (DC50) 0.092 nM
MM.1S cells
Multiple myeloma
CVCL_8792 
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Belan-VA-I034 (8) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
90.41%
In Vivo Model NCI-H929 CDX 3 mpk (Day 25)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
98.82%
In Vivo Model NCI-H929 CDX 6 mpk (Day25)
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01669 nM
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Degradation Concentration (DC50)
0.06 nM
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Degradation Concentration (DC50)
13.06 nM
In Vitro Model Normal PBMC cells CVCL_0140
Dara-VA-I034 (8) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
99.94%
In Vivo Model NCI-H929 CDX 3 mpk (Day 25)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100%
In Vivo Model NCI-H929 CDX 6 mpk (Day25)
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.00269 nM
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.00941 nM
In Vitro Model Plasma cell myeloma, Multiple myeloma MM.1S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50 nM
In Vitro Model Normal PBMC cells CVCL_0140
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Degradation Concentration (DC50)
0.075 nM
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Degradation Concentration (DC50)
13.8 nM
In Vitro Model Normal PBMC cells CVCL_0140
Dara-VA-I034 (4) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.0183 nM
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.0776 nM
In Vitro Model Plasma cell myeloma, Multiple myeloma MM.1S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50 nM
In Vitro Model Normal PBMC cells CVCL_0140
Belan-VA-I034 (4) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.0540 nM
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
References
Ref 1 Rational engineering of degradation tail-driven CELMoD-antibody conjugates for precision malignancy therapy