Linker Information
General Information of This Linker
| Linker ID |
LIN0MZMPD
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
BCN-PEG3-EGC-PABQ
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C49H63N9O12
|
|||||
| Isosmiles |
O=C(NCC(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(CN(C)C)C=C1)=O)=O)[C@@H](NC(COCCOCCOCCNC(CCC(N2C3=C(C#CC(C=CC=C4)=C4C2)C=CC=C3)=O)=O)=O)CCC(O)=O
|
|||||
| InChI |
InChI=1S/C49H63N9O12/c1-57(2)31-34-13-17-38(18-14-34)54-48(66)39(11-7-23-52-49(50)67)55-43(60)30-53-47(65)40(19-22-46(63)64)56-44(61)33-70-29-28-69-27-26-68-25-24-51-42(59)20-21-45(62)58-32-37-10-4-3-8-35(37)15-16-36-9-5-6-12-41(36)58/h3-6,8-10,12-14,17-18,39-40H,7,11,19-33H2,1-2H3,(H,51,59)(H,53,65)(H,54,66)(H,55,60)(H,56,61)(H,63,64)(H3,50,52,67)/t39-,40-/m0/s1
|
|||||
| InChIKey |
DEWYIQILAVWEHH-ZAQUEYBZSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
970.094
|
Polar area
|
289.16
|
||
|
Complexity
|
2233.525418
|
xlogp Value
|
0.9786
|
|||
|
Heavy Count
|
70
|
Rot Bonds
|
30
|
|||
|
Hbond acc
|
12
|
Hbond Donor
|
8
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
H233 VC-qDuoDM gluc [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.01۪.004 nM
|
Moderate EREG expression (EREG++) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | LoVo cells | CVCL_0399 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.02۪.009 nM
|
High EREG expression (EREG +++) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon carcinoma | HCT116 cells | CVCL_0291 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.14۪.16 nM
|
Moderate EREG expression (EREG++) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | DLD-1 cells | CVCL_0248 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.31۪.05 nM
|
Low EREG expression (EREG+) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | SW48 cells | CVCL_1724 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 10000 nM | Negative EREG expression (EREG-) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | DLD-1 cells (EREG KO) | CVCL_0248 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 10000 nM | Low EREG expression (EREG+) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | SW620 cells | CVCL_0547 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 10000 nM | Negative EREG expression (EREG-) | ||
| Method Description |
Cancer cells were plated at ~1,000 cells/well in 96-half-well plates. Serial dilutions of unconjugated H231, cmAb, H231 ADCs, or cADC were added and incubated at 37°C for 4 or 5 days. Cell viability was measured using CellTiter-Glo 2.0 (Promega, cat. #G9242) according to the manufacturer's protocol. Luminescence was measured using a Tecan Infinite M1000 plate reader (RRID: SCR_025732).
Click to Show/Hide
|
||||
| In Vitro Model | Colon carcinoma | RKO cells | CVCL_0504 | ||
References