Linker Information
General Information of This Linker
| Linker ID |
LIN0BIJEQ
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| Linker Name |
Linker of ADC2-58
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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 |
C29H45N7O14
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCNC(CNC(/C=C\C(O)=O)=O)=O)=O)CCC(NC[C@@H](O1)[C@@H](O)[C@@H](O)[C@@H]1CC(N)=O)=O)=O)C(N[C@@H](C)C(O)=O)=O)C
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| InChI |
InChI=1S/C29H45N7O14/c1-13(2)24(28(47)34-14(3)29(48)49)36-27(46)15(35-21(40)8-9-31-22(41)12-33-20(39)6-7-23(42)43)4-5-19(38)32-11-17-26(45)25(44)16(50-17)10-18(30)37/h6-7,13-17,24-26,44-45H,4-5,8-12H2,1-3H3,(H2,30,37)(H,31,41)(H,32,38)(H,33,39)(H,34,47)(H,35,40)(H,36,46)(H,42,43)(H,48,49)/b7-6-/t14-,15-,16-,17+,24-,25-,26+/m0/s1
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| InChIKey |
BJKYCMGTAVYUTH-SBPQMXFVSA-N
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| Pharmaceutical Properties |
Molecule Weight
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715.714
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Polar area
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341.98
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Complexity
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1238.383091
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xlogp Value
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-5.2744
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Heavy Count
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50
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Rot Bonds
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21
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Hbond acc
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12
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Hbond Donor
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11
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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
BGA9962 [Investigative]
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
106%
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously
administered vehicle, BGA9962 (2 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly.
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| In Vivo Model | Human patient-derived gastric xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
107%
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously
administered vehicle, BGA9962 (6 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly.
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| In Vivo Model | Human patient-derived gastric xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.17 nM
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Lung adenocarcinoma | NCI-H2122 cells | CVCL_1531 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.39 nM
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Gastric adenocarcinoma | MKN45 cells | CVCL_0434 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.83 nM
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Colon adenocarcinoma | Ls147T cells | CVCL_1384 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
27 nM
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Negative CEA expression (CEA-) | ||
| Method Description |
MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||