Linker Information
General Information of This Linker
| Linker ID |
LIN0QYKBB
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| Linker Name |
Mc-PEG8-Val-Lys-Gly
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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 |
C39H68N6O16
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| Isosmiles |
CC(C)C(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCN1C(=O)C=CC1=O)C(=O)NC(CCCCN)C(=O)NCC(=O)O
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| InChI |
InChI=1S/C39H68N6O16/c1-30(2)37(39(53)43-31(5-3-4-10-40)38(52)42-29-36(50)51)44-33(47)9-13-54-15-17-56-19-21-58-23-25-60-27-28-61-26-24-59-22-20-57-18-16-55-14-11-41-32(46)8-12-45-34(48)6-7-35(45)49/h6-7,30-31,37H,3-5,8-29,40H2,1-2H3,(H,41,46)(H,42,52)(H,43,53)(H,44,47)(H,50,51)
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| InChIKey |
VBOTUUSCLIBMAR-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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876.999
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Polar area
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290.94
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Complexity
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61
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xlogp Value
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-2.104
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Heavy Count
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61
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Rot Bonds
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41
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Hbond acc
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16
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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
H00-CPT-LC [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) | ≈ 50.46% (Day 11) | Positive CD30 expression (CD30+++/++) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of h00-CPT-Lc=10 mg/kg.
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| In Vivo Model | ALCL CDX model | ||||
| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells/Karpas BVR cells | CVCL_1324 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
930.00 ng/mL
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High CD30 expression (CD30+++; 285,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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| In Vitro Model | Precursor T-cell acute lymphoblastic leukemia | ALCL cells | CVCL_A036 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 400,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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| In Vitro Model | Hodgkin's disease | L540cy cells | Homo sapiens | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 320,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
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| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells | CVCL_1324 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | Low CD30 expression (CD30+; 70,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
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| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | High CD30 expression (CD30+++; 180,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
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| In Vitro Model | Anaplastic large cell lymphoma | DEL/BVR cells | CVCL_1170 | ||
CAC10-CPT-LC [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) | ≈ 54.80% (Day 51) | Low CD30 expression (CD30+) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-CPT-Lc=1 mg/kg.
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| In Vivo Model | HD CDX model | ||||
| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 72.65% (Day 51) | Low CD30 expression (CD30+) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-CPT-Lc=3 mg/kg.
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| In Vivo Model | HD CDX model | ||||
| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 76.00% (Day 28) | Positive CD30 expression (CD30+++/++) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-CPT-Lc=0.3 mg/kg.
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| In Vivo Model | HD CDX model | ||||
| In Vitro Model | Hodgkin's disease | L540cy cells | Homo sapiens | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.00% (Day 11) | Positive CD30 expression (CD30+++/++) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-CPT-Lc=3 mg/kg.
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| In Vivo Model | ALCL CDX model | ||||
| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells/Karpas BVR cells | CVCL_1324 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 90.00% (Day 11) | Positive CD30 expression (CD30+++/++) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-CPT-Lc=10 mg/kg.
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| In Vivo Model | ALCL CDX model | ||||
| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells/Karpas BVR cells | CVCL_1324 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 28) | Positive CD30 expression (CD30+++/++) | ||
| Method Description |
Tumor cells, as suspensions, were implanted subcutaneously in SCID or nude mice. Upon tumor engraftment, mice were randomized to study groups (5 mice per group) when the average tumor volume reached about 100 mm3. The ADC or vehicle controls were dosed once via intraperitoneal injection. The dose of cAC10-CPT-Lc=1 mg/kg.
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| In Vivo Model | HD CDX model | ||||
| In Vitro Model | Hodgkin's disease | L540cy cells | Homo sapiens | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.00 ng/mL
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High CD30 expression (CD30+++; 400,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
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|
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| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.00 ng/mL
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High CD30 expression (CD30+++; 285,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
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| In Vitro Model | Precursor T-cell acute lymphoblastic leukemia | ALCL cells | CVCL_A036 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.00 ng/mL
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High CD30 expression (CD30+++; 320,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
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| In Vitro Model | ALK-positive anaplastic large cell lymphoma | Karpas-299 cells | CVCL_1324 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.00 ng/mL
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High CD30 expression (CD30+++; 180,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
|
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| In Vitro Model | Anaplastic large cell lymphoma | DEL/BVR cells | CVCL_1170 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000.00 ng/mL | Low CD30 expression (CD30+; 70,000 CD30 molecules/cell) | ||
| Method Description |
Serial dilutions of ADCs in cell culture media were prepared at 4x working concentrations, and 50 uL of each dilution was added to the 96-well plates. Following addition of test articles, cells were incubated for 4 days at 37°C, after which growth inhibition was assessed by the addition of CellTiter-Glo and luminescence was measured on a plate reader.
Click to Show/Hide
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| In Vitro Model | Hodgkin lymphoma | L-428 cells | CVCL_1361 | ||
References
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