Linker Information
General Information of This Linker
| Linker ID |
LIN0ERSEI
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| Linker Name |
KR1020250002133A Trastuzumab-C-21 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 |
C66H101N13O17S
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCN1C(C=CC1=O)=O)=O)CC(NCCOCCOCCOCCOCCOCCOCCOCCOCCN(CC2)CCC2CN3C4=C5C(C=C(S5)C)=NC(N)=C4N=C3CCCC)=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/C66H101N13O17S/c1-5-6-9-53-75-59-60(61-51(73-62(59)67)41-46(4)97-61)79(53)43-47-16-21-77(22-17-47)24-26-90-28-30-92-32-34-94-36-38-96-40-39-95-37-35-93-33-31-91-29-27-89-25-20-69-55(82)42-52(72-54(81)18-23-78-56(83)14-15-57(78)84)64(86)76-58(45(2)3)65(87)74-50(8-7-19-70-66(68)88)63(85)71-49-12-10-48(44-80)11-13-49/h10-15,41,45,47,50,52,58,80H,5-9,16-40,42-44H2,1-4H3,(H2,67,73)(H,69,82)(H,71,85)(H,72,81)(H,74,87)(H,76,86)(H3,68,70,88)/t50-,52-,58-/m0/s1
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| InChIKey |
LWRXJCQPJMYPPL-PLOJTPHXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1380.675
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Polar area
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392.04
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Complexity
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2998.979684
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xlogp Value
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2.23532
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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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9
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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-21 [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) |
0.018 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) |
0.12 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) |
3.13 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) |
573.7 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 | ||