Linker Information
General Information of This Linker
| Linker ID |
LIN0AMHHG
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| Linker Name |
AU2023279443A1, Example A7, 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 |
C49H70N10O19
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| Isosmiles |
CC(C)[C@H](NC([C@@H](NC(CCOCCOCCOCCOCCNC([C@@H](N1C(C=CC1=O)=O)CNC([C@@H]2CCC(O2)=O)=O)=O)=O)CC(N[C@@H](CCO3)C3=O)=O)=O)C(N[C@H](C(NC4=CC=C(CO)C=C4)=O)CCCNC(N)=O)=O
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| InChI |
InChI=1S/C49H70N10O19/c1-29(2)42(47(70)57-32(4-3-15-52-49(50)72)43(66)54-31-7-5-30(28-60)6-8-31)58-44(67)34(26-38(62)55-33-13-18-77-48(33)71)56-37(61)14-17-73-20-22-75-24-25-76-23-21-74-19-16-51-45(68)35(59-39(63)10-11-40(59)64)27-53-46(69)36-9-12-41(65)78-36/h5-8,10-11,29,32-36,42,60H,3-4,9,12-28H2,1-2H3,(H,51,68)(H,53,69)(H,54,66)(H,55,62)(H,56,61)(H,57,70)(H,58,67)(H3,50,52,72)/t32-,33-,34-,35-,36-,42-/m0/s1
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| InChIKey |
WHBVUZSUGIRXRU-JTXZLGNISA-N
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| Pharmaceutical Properties |
Molecule Weight
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1103.15
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Polar area
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405.95
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Complexity
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2180.772904
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xlogp Value
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-3.8138
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Heavy Count
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78
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Rot Bonds
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36
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Hbond acc
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19
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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
aU2023279443A1 Example A7 [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) | > 101% | 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 3 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 | ||