Linker Information
General Information of This Linker
| Linker ID |
LIN0WIIKN
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| Linker Name |
Mal-Me3Lys-Pro
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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 |
C23H39N6O5+
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| Isosmiles |
C[N+](C)(C)CCCCC(NC(=O)C1CCCN1)C(=O)NCCNC(=O)CCN1C(=O)C=CC1=O
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| InChI |
InChI=1S/C23H38N6O5/c1-29(2,3)16-5-4-7-18(27-23(34)17-8-6-12-24-17)22(33)26-14-13-25-19(30)11-15-28-20(31)9-10-21(28)32/h9-10,17-18,24H,4-8,11-16H2,1-3H3,(H2-,25,26,27,30,33,34)/p+1
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| InChIKey |
JDNIQQPBIDHGDS-UHFFFAOYSA-O
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| Pharmaceutical Properties |
Molecule Weight
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479.602
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Polar area
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136.71
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Complexity
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34
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xlogp Value
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-1.3528
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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
|
6
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Hbond Donor
|
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
1F6-Me3-Lys-Pro-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) |
66.35% (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 | DBTRG-05MG glioblastoma cell line xenograft model | ||||
| In Vitro Model | Anaplastic astrocytoma | DBTRG-05MG cells | CVCL_1169 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
93.15% (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) |
11.00 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) |
20.00 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 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
24.00 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 | ||
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