Linker Information
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 | ||||||
| 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
| 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
| 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
| 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
| 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 | ||
