Linker Information
General Information of This Linker
| Linker ID |
LIN0WKPJE
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| Linker Name |
Sulfosuccinimidyl-N-succinimidyl-4-(5-nitro-2-pyridyldithio) pentanoate (SSNPP)
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| Linker Type |
Thiol-sensitive linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C5H11NOS
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| Isosmiles |
CC(S)CCC(N)=O
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| InChI |
InChI=1S/C5H11NOS/c1-4(8)2-3-5(6)7/h4,8H,2-3H2,1H3,(H2,6,7)
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| InChIKey |
SOGYAORYDQNPPQ-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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133.216
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Polar area
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43.09
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Complexity
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8
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xlogp Value
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0.5702
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Heavy Count
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8
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Rot Bonds
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3
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Hbond acc
|
2
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Hbond Donor
|
2
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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
F105-SSNPP-DM4 [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) | ≈ 0.00% (Day 37) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
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| In Vivo Model | HT-29 CDX model | ||||
| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
CNTO95-SSNPP-DM4 [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) | ≈ 0.00% (Day 37) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
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| In Vivo Model | HT-29 CDX model | ||||
| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 71.21% (Day 24) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (5 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
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| In Vivo Model | A375.S2 CDX model | ||||
| In Vitro Model | Amelanotic melanoma | A375.S2 cells | CVCL_0136 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.15% (Day 24) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (10 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
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| In Vivo Model | A375.S2 CDX model | ||||
| In Vitro Model | Amelanotic melanoma | A375.S2 cells | CVCL_0136 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.10% (Day 49) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
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| In Vivo Model | A549 CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.00 ug/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.00 ug/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.20 ug/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.50 ug/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.19 mg/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.27 mg/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.27 mg/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | A2780 cells | CVCL_0134 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.29 mg/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.30 mg/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | A2780 cells | CVCL_0134 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.42 mg/mL
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Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
Tmab-SSNPP-DM4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.60% (Day 10) | High HER2 expression (HER2+++) | ||
| Method Description |
Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
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| In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
| In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
Tmab-SSNPP-DM3 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.60% (Day 10) | High HER2 expression (HER2+++) | ||
| Method Description |
Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
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| In Vivo Model | MMTV-HER2 Fo5 CDX model (Trastuzumab resistant) | ||||
| In Vitro Model | Breast cancer | MMTV-HER2 cells | Mus musculus | ||
References
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