Linker Information
General Information of This Linker
| Linker ID |
LIN0KKZRE
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|---|---|---|---|---|---|---|
| Linker Name |
OXDc-VA-PAB (Glu)
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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 |
C78H123N17O35S
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| Isosmiles |
CC(C)[C@H](NC(COCC(NCC1=CC=CC(C2=NN=C(O2)S(C)(=O)=O)=C1)=O)=O)C(N[C@@H](C)C(NC3=CC=C(C=C3)C(O)CC(N=N4)=CN4CC(NCC(NCC(NCC(NCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCC(N[C@@H](CCC(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)=O)C(NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)=O)=O)=O)=O)=O)=O)=O)=O)=O
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| InChI |
InChI=1S/C78H123N17O35S/c1-47(2)69(90-68(111)46-129-45-67(110)80-34-49-6-5-7-51(32-49)77-92-93-78(130-77)131(4,119)120)76(118)87-48(3)74(116)88-52-10-8-50(9-11-52)55(98)33-53-41-95(94-91-53)42-66(109)85-40-65(108)84-39-64(107)83-38-63(106)82-37-62(105)79-15-17-122-19-21-124-23-25-126-27-29-128-31-30-127-28-26-125-24-22-123-20-18-121-16-14-61(104)89-54(75(117)86-36-57(100)71(113)73(115)59(102)44-97)12-13-60(103)81-35-56(99)70(112)72(114)58(101)43-96/h5-11,32,41,47-48,54-59,69-73,96-102,112-115H,12-31,33-40,42-46H2,1-4H3,(H,79,105)(H,80,110)(H,81,103)(H,82,106)(H,83,107)(H,84,108)(H,85,109)(H,86,117)(H,87,118)(H,88,116)(H,89,104)(H,90,111)/t48-,54-,55?,56-,57-,58+,59+,69-,70+,71+,72+,73+/m0/s1
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| InChIKey |
AUZXINWGHYBISI-GPIVHUKNSA-N
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| Pharmaceutical Properties |
Molecule Weight
|
1890.993
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Polar area
|
758.57
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Complexity
|
.
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xlogp Value
|
-11.6022
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Heavy Count
|
131
|
Rot Bonds
|
71
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Hbond acc
|
40
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Hbond Donor
|
23
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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
wO2024222841A1 ADC40 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
90.10%
|
Low HER2 expression (HER2+) | ||
| Method Description |
Investigated the antitumour effect of 5mg/kg ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D13.
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| In Vivo Model | HER2-low JIMT-1 xenograft NUNU mice tumour model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | < 15 pM | High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of ADC to SK-BR-3 cells
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
wO2024222841A1 ADC40-4 [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) |
15-25 pM
|
High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of ADC to SK-BR-3 cells
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||