Linker Information
General Information of This Linker
| Linker ID |
LIN0UHLTJ
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| Linker Name |
DBCO-PEG4-VC-PABC-PEG2
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C56H79N9O14
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| Isosmiles |
CN(CCNCCOCCO)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
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| InChI |
InChI=1S/C56H79N9O14/c1-41(2)52(54(71)62-47(12-8-23-60-55(57)72)53(70)61-46-18-14-42(15-19-46)40-79-56(73)64(3)27-24-58-25-30-75-32-28-66)63-50(68)22-29-74-33-35-77-37-38-78-36-34-76-31-26-59-49(67)20-21-51(69)65-39-45-11-5-4-9-43(45)16-17-44-10-6-7-13-48(44)65/h4-7,9-11,13-15,18-19,41,47,52,58,66H,8,12,20-40H2,1-3H3,(H,59,67)(H,61,70)(H,62,71)(H,63,68)(H3,57,60,72)/t47-,52+/m0/s1
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| InChIKey |
QRQALMJPCMOOEI-SMTSAFDASA-N
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| Pharmaceutical Properties |
Molecule Weight
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1102.297
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Polar area
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299.78
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Complexity
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2343.048054
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xlogp Value
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2.1656
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Heavy Count
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79
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Rot Bonds
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38
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Hbond acc
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15
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Hbond Donor
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8
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
H231 VC-cDuoDM [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.002 nM
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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).
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| 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
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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).
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| 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
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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).
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| 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
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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).
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| 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 |
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).
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| 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).
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| 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).
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| In Vitro Model | Colon carcinoma | RKO cells | CVCL_0504 | ||
References