Linker Information
General Information of This Linker
| Linker ID |
LIN0BXPIX
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| Linker Name |
KR1020250002133A Trastuzumab-C-22 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 |
C68H103N13O14S2
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| Isosmiles |
CC([C@@H](NC([C@@H](NC(CCCC#CC1=CN=CN=C1)=O)CSCCOCCOCCOCCOCCOCCOCCOCCOCCN2CCC(CC2)CN3C(CCCC)=NC(C3=C(S4)C(C=C4C)=N5)=C5N)=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/C68H103N13O14S2/c1-5-6-13-58-78-61-62(63-56(76-64(61)69)42-50(4)97-63)81(58)45-51-19-22-80(23-20-51)24-25-88-26-27-89-28-29-90-30-31-91-32-33-92-34-35-93-36-37-94-38-39-95-40-41-96-47-57(75-59(83)14-9-7-8-11-53-43-71-48-72-44-53)66(85)79-60(49(2)3)67(86)77-55(12-10-21-73-68(70)87)65(84)74-54-17-15-52(46-82)16-18-54/h15-18,42-44,48-49,51,55,57,60,82H,5-7,9-10,12-14,19-41,45-47H2,1-4H3,(H2,69,76)(H,74,84)(H,75,83)(H,77,86)(H,79,85)(H3,70,73,87)/t55-,57-,60+/m0/s1
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| InChIKey |
MGFVQGGDHZGEKI-JFYDIBECSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1390.783
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Polar area
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351.34
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Complexity
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3040.32493
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xlogp Value
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5.15912
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Heavy Count
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97
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Rot Bonds
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50
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Hbond acc
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23
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Hbond Donor
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8
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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-22 [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) |
0.053 nM
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-21 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) |
0.103 nM
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-21 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) |
14.05 nM
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-21 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) |
1562.5 pg/mL
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-21 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||