Linker Information
General Information of This Linker
| Linker ID |
LIN0NQMDK
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| Linker Name |
Mal-PhenylGly-D-Lys
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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 |
C23H32N6O5
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| Isosmiles |
NCCCCC(N)C(=O)NC(C(=O)NCCNC(=O)CCN1C(=O)C=CC1=O)c1ccccc1
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| InChI |
InChI=1S/C23H32N6O5/c24-12-5-4-8-17(25)22(33)28-21(16-6-2-1-3-7-16)23(34)27-14-13-26-18(30)11-15-29-19(31)9-10-20(29)32/h1-3,6-7,9-10,17,21H,4-5,8,11-15,24-25H2,(H,26,30)(H,27,34)(H,28,33)
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| InChIKey |
ALSAHDFKBZWQGR-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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472.546
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Polar area
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176.72
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Complexity
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34
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xlogp Value
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-1.1523
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Heavy Count
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34
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Rot Bonds
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14
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Hbond acc
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7
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Hbond Donor
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5
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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
1F6-PhenylGly- (D)Lys-AF [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) |
93.39% (Day 30)
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Positive TNF expression (TNF+++/++) | ||
| Method Description |
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
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| In Vivo Model | 786-O human RCC cell line xenograft model | ||||
| In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
44.00 ng/mL
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Positive TNF expression (TNF+++/++) | ||
| Method Description |
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
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| In Vitro Model | Clear cell renal cell carcinoma | Caki-1 cells | CVCL_0234 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
275.00 ng/mL
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Positive TNF expression (TNF+++/++) | ||
| Method Description |
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
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| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
339.00 ng/mL
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Positive TNF expression (TNF+++/++) | ||
| Method Description |
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
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| In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 | ||
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