Linker Information
General Information of This Linker
| Linker ID |
LIN0SMAZQ
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| Linker Name |
KR1020250002133A Trastuzumab-C-9 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 |
C65H99N13O17S
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| Isosmiles |
CC(C)[C@H](NC(CC[C@H](NC(CCN1C(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/C65H99N13O17S/c1-4-5-8-52-74-58-59(75-52)61(66)72-50-42-51(96-60(50)58)46-17-22-77(23-18-46)25-27-89-29-31-91-33-35-93-37-39-95-41-40-94-38-36-92-34-32-90-30-28-88-26-21-68-62(84)49(71-54(81)19-24-78-55(82)15-16-56(78)83)13-14-53(80)76-57(44(2)3)64(86)73-48(7-6-20-69-65(67)87)63(85)70-47-11-9-45(43-79)10-12-47/h9-12,15-16,42,44,46,48-49,57,79H,4-8,13-14,17-41,43H2,1-3H3,(H2,66,72)(H,68,84)(H,70,85)(H,71,81)(H,73,86)(H,74,75)(H,76,80)(H3,67,69,87)/t48-,49-,57-/m0/s1
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| InChIKey |
BFXKBYSMYZBERG-YJHPNKSSSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1366.648
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Polar area
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402.9
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Complexity
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2946.06517
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xlogp Value
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2.311
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Heavy Count
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96
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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-9 [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) |
0.021 nM
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High HER2 expression (HER5 +++) | ||
| Method Description |
Trastuzumab-C-9 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) |
0.058 nM
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High HER2 expression (HER6 +++) | ||
| Method Description |
Trastuzumab-C-9 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) |
136.77 nM
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High HER2 expression (HER7 +++) | ||
| Method Description |
Trastuzumab-C-9 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) |
24.41 nM
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High HER2 expression (HER8 +++) | ||
| Method Description |
Trastuzumab-C-9 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) |
470.23 pg/mL
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High HER2 expression (HER9 +++) | ||
| Method Description |
Trastuzumab-C-9 was tested in HCC1954 and PBMC,50ul,24h
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| In Vitro Model | Breast ductal carcinoma | HCC1954 cells | CVCL_1259 | ||