Linker Information
General Information of This Linker
| Linker ID |
LIN0ZPAQB
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| Linker Name |
Mal-Val-Cit-PABC
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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 |
C23H30N6O7
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| Isosmiles |
CC(C)C(NC(=O)N1C(=O)C=CC1=O)C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1
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| InChI |
InChI=1S/C23H30N6O7/c1-13(2)19(28-23(36)29-17(31)9-10-18(29)32)21(34)27-16(4-3-11-25-22(24)35)20(33)26-15-7-5-14(12-30)6-8-15/h5-10,13,16,19,30H,3-4,11-12H2,1-2H3,(H,26,33)(H,27,34)(H,28,36)(H3,24,25,35)
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| InChIKey |
VUBLQDRBXNCAJX-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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502.528
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Polar area
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200.03
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Complexity
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36
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xlogp Value
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-0.2901
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Heavy Count
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36
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Rot Bonds
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11
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Hbond acc
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7
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Hbond Donor
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6
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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-Val-Cit-PABC-MMAF [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) |
84.59% (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) |
85.01% (Day 30)
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Positive TNF expression (TNF+++/++) | ||
| Method Description |
1 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 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
93.25% (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) |
5.90±2.00 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 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
6.10±2.70 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 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
9.10±3.60 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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