Linker Information
General Information of This Linker
| Linker ID |
LIN0SQHTU
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| Linker Name |
KR1020250002133A Trastuzumab-C-11 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 |
C68H102N14O15S
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| Isosmiles |
CC(C)[C@H](NC(CC[C@H](NC(CCCC#CC1=CN=CN=C1)=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/C68H102N14O15S/c1-4-5-12-57-79-61-62(80-57)64(69)77-55-43-56(98-63(55)61)51-20-24-82(25-21-51)26-28-91-30-32-93-34-36-95-38-40-97-42-41-96-39-37-94-35-33-92-31-29-90-27-23-73-65(86)54(76-58(84)13-8-6-7-10-50-44-71-47-72-45-50)18-19-59(85)81-60(48(2)3)67(88)78-53(11-9-22-74-68(70)89)66(87)75-52-16-14-49(46-83)15-17-52/h14-17,43-45,47-48,51,53-54,60,83H,4-6,8-9,11-13,18-42,46H2,1-3H3,(H2,69,77)(H,73,86)(H,75,87)(H,76,84)(H,78,88)(H,79,80)(H,81,85)(H3,70,74,89)/t53-,54-,60-/m0/s1
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| InChIKey |
CRMLOHLQKLXGPD-QCIKBCMQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1387.714
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Polar area
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391.3
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Complexity
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3092.990416
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xlogp Value
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4.0079
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Heavy Count
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98
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Rot Bonds
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50
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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-11 [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 (HER15 +++) | ||
| Method Description |
Trastuzumab-C-11 was tested in NCI-H358,80ul,18ᆬh
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| In Vitro Model | Minimally invasive lung adenocarcinoma | NCI-H358 cells | CVCL_1559 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.026 nM
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High HER2 expression (HER16 +++) | ||
| Method Description |
Trastuzumab-C-11 was tested in NCI-H358,80ul,18ᆬh
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| In Vitro Model | Minimally invasive lung adenocarcinoma | NCI-H358 cells | CVCL_1559 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
331.62 nM
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High HER2 expression (HER17 +++) | ||
| Method Description |
Trastuzumab-C-11 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) |
32.59 nM
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High HER2 expression (HER18 +++) | ||
| Method Description |
Trastuzumab-C-11 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) |
427.95 pg/mL
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High HER2 expression (HER19 +++) | ||
| Method Description |
Trastuzumab-C-11 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||