Linker Information
General Information of This Linker
| Linker ID |
LIN0JWXZZ
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| Linker Name |
Mal-Met-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 |
C20H34N6O5S
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| Isosmiles |
CSCCC(NC(=O)C(N)CCCCN)C(=O)NCCNC(=O)CCN1C(=O)C=CC1=O
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| InChI |
InChI=1S/C20H34N6O5S/c1-32-13-8-15(25-19(30)14(22)4-2-3-9-21)20(31)24-11-10-23-16(27)7-12-26-17(28)5-6-18(26)29/h5-6,14-15H,2-4,7-13,21-22H2,1H3,(H,23,27)(H,24,31)(H,25,30)
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| InChIKey |
OHFJZRLLNNFUJZ-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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470.596
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Polar area
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176.72
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Complexity
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32
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xlogp Value
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-1.7719
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Heavy Count
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32
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Rot Bonds
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16
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Hbond acc
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8
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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-Met- (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) |
86.68% (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) |
92.40% (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) |
9.00 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) |
12.00 ng/mL
|
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) |
168.00 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 | ||
1F6-Met- (D)Lys-AW [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) |
93.88% (Day 30)
|
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 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
15.00 ng/mL
|
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) |
16.00 ng/mL
|
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) |
19.00 ng/mL
|
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 | ||
1F6-Met- (D)Lys-MMAF [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.00 ng/mL
|
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) |
10.00 ng/mL
|
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) |
123.00 ng/mL
|
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 | ||
1F6-Met- (D)Lys-AM [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
39.00 ng/mL
|
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) |
56.00 ng/mL
|
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) |
1000.00 ng/mL
|
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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