Linker Information
General Information of This Linker
| Linker ID |
LIN0HAZZL
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| Linker Name |
Quaternary ammonium linker Gluc
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| Linker Type |
Glycosidases-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C24H28N4O14
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| Isosmiles |
NCC(C(=O)NCCC(=O)Nc1cc(COC(=O)O)ccc1OC1OC(C(=O)O)C(O)C(O)C1O)N1C(=O)C=CC1=O
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| InChI |
InChI=1S/C24H28N4O14/c25-8-12(28-15(30)3-4-16(28)31)21(35)26-6-5-14(29)27-11-7-10(9-40-24(38)39)1-2-13(11)41-23-19(34)17(32)18(33)20(42-23)22(36)37/h1-4,7,12,17-20,23,32-34H,5-6,8-9,25H2,(H,26,35)(H,27,29)(H,36,37)(H,38,39)
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| InChIKey |
QFBPBHGJGQKJRR-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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596.502
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Polar area
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284.58
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Complexity
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42
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xlogp Value
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-3.1507
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Heavy Count
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42
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Rot Bonds
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12
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Hbond acc
|
13
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Hbond Donor
|
8
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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
CC2B-h15H3-gluc-MMAE [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 86.40% (Day 25) | Positive ITGA5 expression (ITGA5 +++/++) | ||
| Method Description |
Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
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| In Vivo Model | HPAF-II CDX model | ||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | HPAF-II cells | CVCL_0313 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 96.10% (Day 29) | Positive ITGA5 expression (ITGA5 +++/++) | ||
| Method Description |
Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
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| In Vivo Model | Detroit 562 CDX model | ||||
| In Vitro Model | Pharyngeal squamous cell carcinoma | Detroit 562 cells | CVCL_1171 | ||
h15H3-gluc-MMAE [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.93% (Day 29) | Positive ITGA5 expression (ITGA5 +++/++) | ||
| Method Description |
Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
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| In Vivo Model | Detroit 562 CDX model | ||||
| In Vitro Model | Pharyngeal squamous cell carcinoma | Detroit 562 cells | CVCL_1171 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.94% (Day 25) | Positive ITGA5 expression (ITGA5 +++/++) | ||
| Method Description |
Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
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| In Vivo Model | HPAF-II CDX model | ||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | HPAF-II cells | CVCL_0313 | ||
References
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