Linker Information
General Information of This Linker
| Linker ID |
LIN0VLAZJ
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| Linker Name |
Solubilizing group-PEG2-Hypoxia sensitive linker-Azobenzene
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| Linker Type |
Hypoxia sensitive linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C30H36N6O8
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| Isosmiles |
OCC1=CC=C(/N=N/C(C=C2)=CC=C2C(NCCNC(CCOCCOCCNC(CCN3C(C=CC3=O)=O)=O)=O)=O)C=C1
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| InChI |
InChI=1S/C30H36N6O8/c37-21-22-1-5-24(6-2-22)34-35-25-7-3-23(4-8-25)30(42)33-14-13-31-27(39)12-17-43-19-20-44-18-15-32-26(38)11-16-36-28(40)9-10-29(36)41/h1-10,37H,11-21H2,(H,31,39)(H,32,38)(H,33,42)/b35-34+
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| InChIKey |
RWABVIRRVVLMPZ-XAHDOWKMSA-N
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| Pharmaceutical Properties |
Molecule Weight
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608.652
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Polar area
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188.09
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Complexity
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1256.553564
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xlogp Value
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1.2949
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Heavy Count
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44
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Rot Bonds
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19
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Hbond acc
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10
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Hbond Donor
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4
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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
aZO-ADC-2 [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) |
62.36%
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Low HER2 expression (HER2+) | ||
| Method Description |
Investigated the antitumour effect of 12 MG/KG AZO-ADC-2 in a Herceptin-resistant, HER2low JIMT-1 xenograft tumour model.
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| In Vivo Model | Herceptin-resistant, HER2-low JIMT-1 xenograft tumour model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
90.97%
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High HER2 expression (HER2+++) | ||
| Method Description |
In the HER2high NCI-N87 xenograft model, Herceptin, AZO-ADC-2 and VC-ADC were administered once a week at a dose of 5 or 10 mg/kg for four consecutive weeks. Compared with the control group, AZO-ADC-2 (5 mg/kg) treatment group displayed significant and sustained suppression of tumour growth with an inhibition rate of 90.97 %
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| In Vivo Model | HER2high NCI-N87 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.016 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to HER2+ SK-BR-3 cells
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.027 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to HER2+ BK474 cells
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.053 nM
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| Method Description |
Cytotoxicity of AZO-ADC-2 to SKOV3/MCF-7 co-culture under 0.1% O2
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| In Vitro Model | Ovarian serous cystadenocarcinoma; Invasive breast carcinoma of no special type | SKOV3/MCF-7 co-culture cells | CVCL_0532; CVCL_0031 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.063 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 0.1 % O2
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.069 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to HER2+ NCI-N87 cells
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.079 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 1 % O2
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.088 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.19 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 0.1% O2
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| In Vitro Model | Invasive breast carcinoma of no special type | BT474-HDR cells | CVCL_0179 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.28 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
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| In Vitro Model | Invasive breast carcinoma of no special type | BT474-HDR cells | CVCL_0179 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.57 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 1 % O2
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| In Vitro Model | Invasive breast carcinoma of no special type | BT474-HDR cells | CVCL_0179 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
3.74 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 5 % O2
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
9.12 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 5 % O2
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| In Vitro Model | Invasive breast carcinoma of no special type | BT474-HDR cells | CVCL_0179 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
11.05 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
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| In Vitro Model | Invasive breast carcinoma of no special type | BT474-HDR cells | CVCL_0179 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
27.67 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
66.8 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 20 % O2
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
109.1 nM
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High HER2 expression (HER2+++) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 20 % O2
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| In Vitro Model | Invasive breast carcinoma of no special type | BT474-HDR cells | CVCL_0179 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
115.4 nM
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Low HER2 expression (HER2+) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to HER2- MCF-7 cells
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 18 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
134.7 nM
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| Method Description |
Cytotoxicity of AZO-ADC-2 to SKOV3/MCF-7 co-culture under 20% O2
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| In Vitro Model | Ovarian serous cystadenocarcinoma; Invasive breast carcinoma of no special type | SKOV3/MCF-7 co-culture cells | CVCL_0532; CVCL_0031 | ||
| Experiment 19 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
266.93 nM
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| Method Description |
Cytotoxicity of AZO-ADC-2 to normal cells, LO2 cells
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| In Vitro Model | Human papillomavirus-related endocervical adenocarcinoma | LO2 cells | CVCL_6926 | ||
| Experiment 20 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 666 nM | Low HER2 expression (HER2+) | ||
| Method Description |
Cytotoxicity of AZO-ADC-2 to HER2- MDA-MB-231 cells
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 21 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 666 nM | |||
| Method Description |
Cytotoxicity of AZO-ADC-2 to normal cells, NIH3T3 cells
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| In Vitro Model | Normal | NIH3T3 cells | CVCL_0594 | ||
| Experiment 22 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 666 nM | |||
| Method Description |
Cytotoxicity of AZO-ADC-2 to normal cells, 293T cells
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| In Vitro Model | Normal | 293T cells | CVCL_0063 | ||
References