Linker Information
General Information of This Linker
| Linker ID |
LIN0PKTBT
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| Linker Name |
BGA0179 Linker
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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 |
C32H52N8O15
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCNC(OCC[C@@H](NC(/C=C\C(O)=O)=O)CN)=O)=O)CCC(NC[C@@H]1[C@@H](O)[C@@H](O)[C@H](CC(N)=O)O1)=O)=O)C(N[C@@H](C)C(O)=O)=O)C
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| InChI |
InChI=1S/C32H52N8O15/c1-15(2)26(30(50)37-16(3)31(51)52)40-29(49)18(4-5-22(42)36-14-20-28(48)27(47)19(55-20)12-21(34)41)39-24(44)8-10-35-32(53)54-11-9-17(13-33)38-23(43)6-7-25(45)46/h6-7,15-20,26-28,47-48H,4-5,8-14,33H2,1-3H3,(H2,34,41)(H,35,53)(H,36,42)(H,37,50)(H,38,43)(H,39,44)(H,40,49)(H,45,46)(H,51,52)/b7-6-/t16-,17+,18-,19-,20+,26-,27-,28+/m0/s1
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| InChIKey |
DQCQFAZHHYDZSX-NFLYOOKFSA-N
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| Pharmaceutical Properties |
Molecule Weight
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788.809
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Polar area
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377.23
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Complexity
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1335.419109
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xlogp Value
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-4.947
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Heavy Count
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55
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Rot Bonds
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24
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Hbond acc
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14
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Hbond Donor
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12
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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
BGA0179 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.16 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) |
0.3 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) |
0.62 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) |
24 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 | ||