Linker Information
General Information of This Linker
| Linker ID |
LIN0JHLBB
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| Linker Name |
BCN-PEG3-EGC-PABC-SPACER
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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 |
C44H67N9O14
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| Isosmiles |
CNCCN(C)C(OCC1=CC=C(NC([C@@H](NC(CNC([C@@H](NC(COCCOCCOCCNC(OC[C@H]2[C@@]3([H])CCC#CCC[C@]32[H])=O)=O)CCC(O)=O)=O)=O)CCCNC(N)=O)=O)C=C1)=O
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| InChI |
InChI=1S/C44H67N9O14/c1-46-18-20-53(2)44(62)67-27-30-11-13-31(14-12-30)50-41(59)35(10-7-17-47-42(45)60)51-37(54)26-49-40(58)36(15-16-39(56)57)52-38(55)29-65-25-24-64-23-22-63-21-19-48-43(61)66-28-34-32-8-5-3-4-6-9-33(32)34/h11-14,32-36,46H,5-10,15-29H2,1-2H3,(H,48,61)(H,49,58)(H,50,59)(H,51,54)(H,52,55)(H,56,57)(H3,45,47,60)/t32-,33+,34-,35-,36-/m0/s1
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| InChIKey |
APVILVUKBYPHBH-YNOSRJHOSA-N
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| Pharmaceutical Properties |
Molecule Weight
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946.069
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Polar area
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316.41
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Complexity
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1723.949203
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xlogp Value
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0.0276
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Heavy Count
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67
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Rot Bonds
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32
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Hbond acc
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14
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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
H232 EGC-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) |
0.05۪.14 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 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.06۪.048 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 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.19۪.07 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 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.38۪.19 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) |
4.93۬.79 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 | SW620 cells | CVCL_0547 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
31.66䔼.12 nM
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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 | ||
| 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 adenocarcinoma | DLD-1 cells (EREG KO) | CVCL_0248 | ||
References