Linker Information
General Information of This Linker
| Linker ID |
LIN0LOHLV
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| Linker Name |
RU20241285-9-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 |
C47H71N10O20P
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| Isosmiles |
CC(C)[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](C(NC3=CC=C(CO)C=C3)=O)CCCNC(N)=O)=O
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| InChI |
InChI=1S/C47H71N10O20P/c1-29(2)41(45(67)55-32(4-3-14-50-47(48)69)42(64)52-31-7-5-30(28-58)6-8-31)56-43(65)34(26-38(61)53-33-11-17-77-46(33)68)54-37(60)12-16-73-19-21-75-23-24-76-22-20-74-18-15-49-44(66)35(57-39(62)9-10-40(57)63)27-51-36(59)13-25-78(70,71)72/h5-10,29,32-35,41,58H,3-4,11-28H2,1-2H3,(H,49,66)(H,51,59)(H,52,64)(H,53,61)(H,54,60)(H,55,67)(H,56,65)(H3,48,50,69)(H2,70,71,72)/t32-,33-,34-,35-,41-/m0/s1
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| InChIKey |
MRUKAPSJIFLNQX-KRLSWSLDSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1127.109
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Polar area
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437.18
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Complexity
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2172.772904
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xlogp Value
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-3.9516
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Heavy Count
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78
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Rot Bonds
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38
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Hbond acc
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18
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Hbond Donor
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12
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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 A14 [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) | > 50% | 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 | ||
aU2023279443A1 Example A8 [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) | > 102% | 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.
Click to Show/Hide
|
||||
| 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 | ||