Linker Information
General Information of This Linker
| Linker ID |
LIN0IYRSR
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| Linker Name |
KR1020250002133A Trastuzumab-C-10 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 |
C68H105N13O17S
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| Isosmiles |
CC(C)[C@@H](NC(CC[C@H](NC(CCCCCN1C(C=CC1=O)=O)=O)C(NCCOCCOCCOCCOCCOCCOCCOCCOCCN2CCC(C3=CC4=NC(N)=C5C(NC(CCCC)=N5)=C4S3)CC2)=O)=O)C(N[C@H](C(NC6=CC=C(CO)C=C6)=O)CCCNC(N)=O)=O
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| InChI |
InChI=1S/C68H105N13O17S/c1-4-5-11-55-77-61-62(78-55)64(69)75-53-45-54(99-63(53)61)49-21-26-80(27-22-49)28-30-92-32-34-94-36-38-96-40-42-98-44-43-97-41-39-95-37-35-93-33-31-91-29-24-71-65(87)52(74-56(83)12-7-6-8-25-81-58(85)19-20-59(81)86)17-18-57(84)79-60(47(2)3)67(89)76-51(10-9-23-72-68(70)90)66(88)73-50-15-13-48(46-82)14-16-50/h13-16,19-20,45,47,49,51-52,60,82H,4-12,17-18,21-44,46H2,1-3H3,(H2,69,75)(H,71,87)(H,73,88)(H,74,83)(H,76,89)(H,77,78)(H,79,84)(H3,70,72,90)/t51-,52-,60+/m0/s1
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| InChIKey |
QYSAYVKQFFZPRA-SXWIWPNCSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1408.729
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Polar area
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402.9
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Complexity
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3000.734572
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xlogp Value
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3.4813
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Heavy Count
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99
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Rot Bonds
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53
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Hbond acc
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22
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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-10 [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) |
0.011 nM
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High HER2 expression (HER10 +++) | ||
| Method Description |
Trastuzumab-C-10 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) |
0.023 nM
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High HER2 expression (HER11 +++) | ||
| Method Description |
Trastuzumab-C-10 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 inhibitory Concentration (lC50) |
164.13 nM
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High HER2 expression (HER12 +++) | ||
| Method Description |
Trastuzumab-C-10 was tested in NCI-H358,80ul,18ᆬh
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| In Vitro Model | Minimally invasive lung adenocarcinoma | NCI-H358 cells | CVCL_1559 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
7.54 nM
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High HER2 expression (HER13 +++) | ||
| Method Description |
Trastuzumab-C-10 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Emax (TNF-a) |
522.28 pg/mL
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High HER2 expression (HER14 +++) | ||
| Method Description |
Trastuzumab-C-10 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||