Linker Information
General Information of This Linker
| Linker ID |
LIN0XLBDG
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| Linker Name |
KR1020250002133A Trastuzumab-C-8 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 |
C114H195N15O39S
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| Isosmiles |
CCCCC1=NC2=C(N)N=C(C3=C2N1)C=C(S3)C4CCN(CC4)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NCCCC[C@H](NC(CCN5C(C=CC5=O)=O)=O)C(N[C@H](C(N(CCOCCOCCOCCOCCOCCOCCOCCOCCOC)CCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)CCC(N[C@H](C(N[C@@H](CCCNC(N)=O)C(NC6=CC=C(CO)C=C6)=O)=O)C(C)C)=O)=O)=O
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| InChI |
InChI=1S/C114H195N15O39S/c1-6-7-13-99-124-106-107(125-99)109(115)121-97-88-98(169-108(97)106)92-22-28-127(29-23-92)31-35-144-43-47-150-55-59-156-67-71-162-79-85-168-87-86-167-82-78-161-70-66-155-58-54-149-46-42-143-34-25-100(131)117-26-9-8-11-94(120-102(133)24-30-129-103(134)20-21-104(129)135)111(137)123-96(18-19-101(132)126-105(90(2)3)112(138)122-95(12-10-27-118-114(116)140)110(136)119-93-16-14-91(89-130)15-17-93)113(139)128(32-36-145-44-48-151-56-60-157-68-72-163-80-83-165-76-74-159-64-62-153-52-50-147-40-38-141-4)33-37-146-45-49-152-57-61-158-69-73-164-81-84-166-77-75-160-65-63-154-53-51-148-41-39-142-5/h14-17,20-21,88,90,92,94-96,105,130H,6-13,18-19,22-87,89H2,1-5H3,(H2,115,121)(H,117,131)(H,119,136)(H,120,133)(H,122,138)(H,123,137)(H,124,125)(H,126,132)(H3,116,118,140)/t94-,95-,96-,105-/m0/s1
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| InChIKey |
DKRAEASXENEOKZ-ODHLBUQVSA-N
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| Pharmaceutical Properties |
Molecule Weight
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2431.947
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Polar area
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636.91
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Complexity
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.
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xlogp Value
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2.7764
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Heavy Count
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169
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Rot Bonds
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117
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Hbond acc
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44
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Hbond Donor
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11
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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-8 [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) |
0.112 nM
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High HER2 expression (HER2 +++) | ||
| Method Description |
Trastuzumab-C-8 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) |
0.25 nM
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High HER2 expression (HER2 +++) | ||
| Method Description |
Trastuzumab-C-8 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) |
374.766 nM
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High HER2 expression (HER2 +++) | ||
| Method Description |
Trastuzumab-C-8 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) |
17.72 nM
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High HER2 expression (HER3 +++) | ||
| Method Description |
Trastuzumab-C-8 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) |
1836.92 pg/mL
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High HER2 expression (HER4 +++) | ||
| Method Description |
Trastuzumab-C-8 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||