General Information of This Linker
Linker ID
LIN0KRUKR
Linker Name
Mal-amido-PEG8-acid
Linker Type
Unclear
Antibody-Linker Relation
Unclear
Structure
Formula
C26H44N2O13
Isosmiles
O=C(O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCN1C(C=CC1=O)=O)=O
PubChem CID
51340955
InChI
InChI=1S/C26H44N2O13/c29-23(3-6-28-24(30)1-2-25(28)31)27-5-8-35-10-12-37-14-16-39-18-20-41-22-21-40-19-17-38-15-13-36-11-9-34-7-4-26(32)33/h1-2H,3-22H2,(H,27,29)(H,32,33)
InChIKey
ARKUDJPBDMAVBL-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
592.639
Polar area
177.62
Complexity
685.5499552
xlogp Value
-0.9748
Heavy Count
41
Rot Bonds
30
Hbond acc
12
Hbond Donor
2
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
aU2023308528A1 ADC4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 20%
Method Description
ADC4 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model at 10 mg/kg single doses and was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50%
Method Description
ADC4 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 6 mg/kg on day 1, dayv8 and day 15. time lasted 57 days.
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 80%
Method Description
ADC4 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 10 mg/kg on day 1, dayv8 and day 15. time lasted 57 days.
In Vivo Model MDA-MB-231 Xenograft Model
aU2023308528A1 ADC3 [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 lnhibition value (TGl) > 30%
Method Description
ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model at 6 mg/kg single doses and was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 60%
Method Description
ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model at 10 mg/kg single doses and was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 60%
Method Description
ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 10 mg/kg was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 80%
Method Description
ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 6 mg/kg was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model MDA-MB-231 Xenograft Model
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 90%
Method Description
ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 3 mg/kg was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model MDA-MB-231 Xenograft Model
aU2023308528A1 ADC3 (DAR of 8) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50% Positive CALU-6 expression (CALU-6+++/++)
Method Description
ADC3 (DAR of 8) was examined in a NSCLC CALU-6 (lung cancer) model after dosing at Q7dx3 at 3 mg/kg.
In Vivo Model NSCLC CALU-6 (lung cancer) model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50% Positive CALU-6 expression (CALU-6+++/++)
Method Description
ADC3 (DAR of 8) was examined in a NSCLC CALU-6 (lung cancer) model after dosing at Q7dx3 at 6 mg/kg.
In Vivo Model NSCLC CALU-6 (lung cancer) model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50% Positive CALU-6 expression (CALU-6+++/++)
Method Description
ADC3 (DAR of 8) was examined in a NSCLC CALU-6 (lung cancer) model after dosing at Q7dx3 at 10 mg/kg.
In Vivo Model NSCLC CALU-6 (lung cancer) model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50%
Method Description
ADC3 (DAR of 8) was examined in a NSCLC CALU-6 (lung cancer) model after dosing at Q7dx3 at 3 mg/kg.
In Vivo Model MDA-MB-231 (TNBC) model
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50%
Method Description
ADC3 (DAR of 8) was examined in a NSCLC CALU-6 (lung cancer) model after dosing at Q7dx3 at 6 mg/kg.
In Vivo Model MDA-MB-231 (TNBC) model
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) > 50%
Method Description
ADC3 (DAR of 8) was examined in a NSCLC CALU-6 (lung cancer) model after dosing at Q7dx3 at 10 mg/kg.
In Vivo Model MDA-MB-231 (TNBC) model
trastuzumab-Compound 30 [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 Effective Concentration (EC50)
3.07 nM
Positive HER2 expression (HER2+++/++)
Method Description
NCI-N87 (HER2+++)
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Antibody-drug conjugates