Linker Information
General Information of This Linker
| Linker ID |
LIN0AQEFU
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| Linker Name |
Mal-NorVal-D-Asp
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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 |
C18H27N5O7
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| Isosmiles |
CCCC(NC(=O)C(N)CC(=O)O)C(=O)NCCNC(=O)CCN1C(=O)C=CC1=O
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| InChI |
InChI=1S/C18H27N5O7/c1-2-3-12(22-17(29)11(19)10-16(27)28)18(30)21-8-7-20-13(24)6-9-23-14(25)4-5-15(23)26/h4-5,11-12H,2-3,6-10,19H2,1H3,(H,20,24)(H,21,30)(H,22,29)(H,27,28)
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| InChIKey |
OVQINOCZYFXSIX-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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425.442
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Polar area
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188
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Complexity
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30
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xlogp Value
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-2.3792
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Heavy Count
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30
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Rot Bonds
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13
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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-NorVal- (D)Asp-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) |
92.33% (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) |
95.90% (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) |
12.00 ng/mL
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Positive CD70 expression (CD70+++/++) | ||
| 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) |
24.00 ng/mL
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Positive CD70 expression (CD70+++/++) | ||
| 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) |
28.00 ng/mL
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Positive CD70 expression (CD70+++/++) | ||
| 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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