Linker Information
General Information of This Linker
| Linker ID |
LIN0EFVTP
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| Linker Name |
KR1020250002133A Trastuzumab-C-15 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 |
C71H111N13O19S
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCN1C(C=CC1=O)=O)=O)CCCCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCN2CCC(CC2)C3=CC4=NC(N)=C(N=C5CCCC)C(N5)=C4S3)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC6=CC=C(CO)C=C6)=O)=O)C
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| InChI |
InChI=1S/C71H111N13O19S/c1-4-5-11-58-80-64-65(81-58)67(72)78-56-48-57(104-66(56)64)52-18-24-83(25-19-52)27-29-95-31-33-97-35-37-99-39-41-101-43-45-103-47-46-102-44-42-100-40-38-98-36-34-96-32-30-94-28-21-59(86)74-22-7-6-9-54(77-60(87)20-26-84-61(88)16-17-62(84)89)69(91)82-63(50(2)3)70(92)79-55(10-8-23-75-71(73)93)68(90)76-53-14-12-51(49-85)13-15-53/h12-17,48,50,52,54-55,63,85H,4-11,18-47,49H2,1-3H3,(H2,72,78)(H,74,86)(H,76,90)(H,77,87)(H,79,92)(H,80,81)(H,82,91)(H3,73,75,93)/t54-,55-,63-/m0/s1
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| InChIKey |
XJLAFIQASAWCMR-NXELZZONSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1482.808
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Polar area
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421.36
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Complexity
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3092.130849
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xlogp Value
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3.1244
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Heavy Count
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104
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Rot Bonds
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58
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Hbond acc
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24
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Hbond Donor
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10
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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
Trastuzumab-C-15 [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) |
0.017 nM
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-15 was tested in HCC1954,80ul,18ᆬh
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.17 nM
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-15 was tested in NCI-N87,80ul,18ᆬh
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
74.62 nM
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-15 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Emax (TNF-a) |
817.79 pg/mL
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-15 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||