Linker Information
General Information of This Linker
| Linker ID |
LIN0OACJX
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
DBCO-PEG4-VC-PABC- (PEG2)
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C57H79N9O16
|
|||||
| Isosmiles |
CN(CCN(CCOCCO)C(O)=O)C(OCC1=CC=C(NC([C@@H](NC([C@@H](NC(CCOCCOCCOCCOCCNC(CCC(N2C3=C(C#CC(C=CC=C4)=C4C2)C=CC=C3)=O)=O)=O)C(C)C)=O)CCCNC(N)=O)=O)C=C1)=O
|
|||||
| InChI |
InChI=1S/C57H79N9O16/c1-41(2)52(54(72)62-47(12-8-23-60-55(58)73)53(71)61-46-18-14-42(15-19-46)40-82-57(76)64(3)25-26-65(56(74)75)27-31-79-32-28-67)63-50(69)22-29-77-33-35-80-37-38-81-36-34-78-30-24-59-49(68)20-21-51(70)66-39-45-11-5-4-9-43(45)16-17-44-10-6-7-13-48(44)66/h4-7,9-11,13-15,18-19,41,47,52,67H,8,12,20-40H2,1-3H3,(H,59,68)(H,61,71)(H,62,72)(H,63,69)(H,74,75)(H3,58,60,73)/t47-,52-/m0/s1
|
|||||
| InChIKey |
GYPKAJHPWYVRJQ-HWPOXGSQSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
1146.306
|
Polar area
|
328.29
|
||
|
Complexity
|
2480.713227
|
xlogp Value
|
2.556
|
|||
|
Heavy Count
|
82
|
Rot Bonds
|
38
|
|||
|
Hbond acc
|
15
|
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
VC-PABC-DuoDM ADC [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) |
0.12۪.02 nM
|
High EREG expression (EREG +++) | ||
| Method Description |
Colorectal 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) |
0.15۪.06 nM
|
High EREG expression (EREG +++) | ||
| Method Description |
Colorectal 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) |
0.33۪.093 nM
|
Moderate EREG expression (EREG++) | ||
| Method Description |
Colorectal 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 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.52۪.39 nM
|
High EREG expression (EREG +++) | ||
| Method Description |
Colorectal 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 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 10000 nM | Negative EREG expression (EREG-) | ||
| Method Description |
Colorectal 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 |
Colorectal 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 | Low EREG expression (EREG+) | ||
| Method Description |
Colorectal 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