Linker Information
General Information of This Linker
| Linker ID |
LIN0CKVGM
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| Linker Name |
AU2023279443A1, Example A19, 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 |
C34H58N6O22P2
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| Isosmiles |
O=C(C[C@H](NC(CCOCCOCCOCCOCCNC(CCN1C(O)C=CC1=O)=O)=O)C(NCCOCCOCC(NCCOP(O)(OP(O)(O)=O)=O)=O)=O)N[C@H]2CCOC2=O
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| InChI |
InChI=1S/C34H58N6O22P2/c41-27(3-9-40-31(45)1-2-32(40)46)35-6-12-55-16-18-58-20-19-57-17-15-54-10-5-28(42)39-26(23-29(43)38-25-4-11-60-34(25)48)33(47)37-7-13-56-21-22-59-24-30(44)36-8-14-61-64(52,53)62-63(49,50)51/h1-2,25-26,31,45H,3-24H2,(H,35,41)(H,36,44)(H,37,47)(H,38,43)(H,39,42)(H,52,53)(H2,49,50,51)/t25-,26-,31?/m0/s1
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| InChIKey |
UGHLPZTVRKPOAY-WKEDTZOBSA-N
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| Pharmaceutical Properties |
Molecule Weight
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964.806
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Polar area
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381.01
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Complexity
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1524.462712
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xlogp Value
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-4.5355
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Heavy Count
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64
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Rot Bonds
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37
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Hbond acc
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19
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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
aU2023279443A1 Example A19 [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) | > 107% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
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| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Cell growth inhibition rate (%) | > 14% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||