Linker Information
General Information of This Linker
| Linker ID |
LIN0SYRPY
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| Linker Name |
DBCO-PEG3-EGC-PABQ
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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 |
C51H68N9O13+
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| Isosmiles |
C[N+](CCO)(C)CC1=CC=C(NC([C@@H](NC(CNC([C@@H](NC(COCCOCCOCCNC(CCC(N2C3=C(C#CC(C=CC=C4)=C4C2)C=CC=C3)=O)=O)=O)CCC(O)=O)=O)=O)CCCNC(N)=O)=O)C=C1
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| InChI |
InChI=1S/C51H67N9O13/c1-60(2,25-26-61)34-36-13-17-40(18-14-36)56-50(69)41(11-7-23-54-51(52)70)57-45(63)32-55-49(68)42(19-22-48(66)67)58-46(64)35-73-31-30-72-29-28-71-27-24-53-44(62)20-21-47(65)59-33-39-10-4-3-8-37(39)15-16-38-9-5-6-12-43(38)59/h3-6,8-10,12-14,17-18,41-42,61H,7,11,19-35H2,1-2H3,(H8-,52,53,54,55,56,57,58,62,63,64,66,67,68,69,70)/p+1/t41-,42-/m0/s1
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| InChIKey |
XXRJNPYWSNFIRF-COCZKOEFSA-O
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| Pharmaceutical Properties |
Molecule Weight
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1015.155
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Polar area
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306.15
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Complexity
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2319.416939
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xlogp Value
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0.4857
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Heavy Count
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73
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Rot Bonds
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32
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Hbond acc
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12
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Hbond Donor
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9
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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
EGC-PABQ-DuoDM gluc 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) |
0.01۪.004 nM
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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).
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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) |
0.02۪.009 nM
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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).
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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) |
0.14۪.16 nM
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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).
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| 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
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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).
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| 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 |
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).
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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 |
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
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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 | 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).
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| In Vitro Model | Colon carcinoma | RKO cells | CVCL_0504 | ||
References