Linker Information
General Information of This Linker
| Linker ID |
LIN0EUQTC
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| Linker Name |
AU2023279443A1, Example A15, 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 |
C62H102N11O33P3
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCOCCOCCOCCOCCNC([C@@H](N1C(C=CC1=O)=O)CNC(CCOCCOCCOCCOCCOCCC(NCCCC(P(O)(O)=O)(O)P(O)(O)=O)=O)=O)=O)=O)CC(N[C@H]2CCOC2=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC3=CC=C(C=C3)COP(O)(O)=O)=O)=O)C
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| InChI |
InChI=1S/C62H102N11O33P3/c1-42(2)55(59(83)71-45(5-3-17-66-61(63)85)56(80)68-44-8-6-43(7-9-44)41-106-109(93,94)95)72-57(81)47(39-52(77)69-46-12-23-105-60(46)84)70-51(76)15-22-98-27-31-102-33-36-103-32-28-99-24-19-65-58(82)48(73-53(78)10-11-54(73)79)40-67-50(75)14-21-97-26-30-101-35-38-104-37-34-100-29-25-96-20-13-49(74)64-18-4-16-62(86,107(87,88)89)108(90,91)92/h6-11,42,45-48,55,86H,3-5,12-41H2,1-2H3,(H,64,74)(H,65,82)(H,67,75)(H,68,80)(H,69,77)(H,70,76)(H,71,83)(H,72,81)(H3,63,66,85)(H2,87,88,89)(H2,90,91,92)(H2,93,94,95)/t45-,46-,47-,48-,55-/m0/s1
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| InChIKey |
MFJZJSRNQCMUOH-JNPRNYESSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1622.464
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Polar area
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636.72
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Complexity
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3051.731594
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xlogp Value
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-4.6413
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Heavy Count
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109
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Rot Bonds
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61
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Hbond acc
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27
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Hbond Donor
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17
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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
aU2023279443A1Example A15 [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) | > 106% | 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 | ||