Linker Information
General Information of This Linker
| Linker ID |
LIN0XIGAL
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| Linker Name |
AU2023279443A1, Example A3, 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 |
C47H72N10O23P2
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCOCCOCCOCCOCCNC([C@@H](N1C(C=CC1=O)=O)CNC(CCP(O)(O)=O)=O)=O)=O)CC(N[C@@H](CCO2)C2=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/C47H72N10O23P2/c1-29(2)41(45(66)55-32(4-3-14-50-47(48)68)42(63)52-31-7-5-30(6-8-31)28-80-82(72,73)74)56-43(64)34(26-38(60)53-33-11-17-79-46(33)67)54-37(59)12-16-75-19-21-77-23-24-78-22-20-76-18-15-49-44(65)35(57-39(61)9-10-40(57)62)27-51-36(58)13-25-81(69,70)71/h5-10,29,32-35,41H,3-4,11-28H2,1-2H3,(H,49,65)(H,51,58)(H,52,63)(H,53,60)(H,54,59)(H,55,66)(H,56,64)(H3,48,50,68)(H2,69,70,71)(H2,72,73,74)/t32-,33-,34-,35-,41-/m0/s1
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| InChIKey |
PKXCJBPGTKHCGE-KRLSWSLDSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1207.088
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Polar area
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483.71
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Complexity
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2354.031757
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xlogp Value
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-3.8346
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Heavy Count
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82
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Rot Bonds
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40
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Hbond acc
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19
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Hbond Donor
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13
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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 A3 [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) | > 100% | 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 | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) | > 105% | 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 | ||