Linker Information
General Information of This Linker
| Linker ID |
LIN0GLEQA
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| Linker Name |
CD33-11A1-v1417 (C)-#39 Linker
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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 |
C38H60N8O12S
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| Isosmiles |
CC(C)[C@@H](NC(CCOCCOCCOCCOCCOCCOCCNC(C1=CN=C(S)N=C1)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(CO)C=C2)=O)=O
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| InChI |
InChI=1S/C38H60N8O12S/c1-27(2)33(36(51)45-31(4-3-10-41-37(39)52)35(50)44-30-7-5-28(26-47)6-8-30)46-32(48)9-12-53-14-16-55-18-20-57-22-23-58-21-19-56-17-15-54-13-11-40-34(49)29-24-42-38(59)43-25-29/h5-8,24-25,27,31,33,47H,3-4,9-23,26H2,1-2H3,(H,40,49)(H,44,50)(H,45,51)(H,46,48)(H3,39,41,52)(H,42,43,59)/t31-,33+/m0/s1
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| InChIKey |
YYBBLYZMAMRLKN-CQTOTRCISA-N
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| Pharmaceutical Properties |
Molecule Weight
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853.009
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Polar area
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272.91
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Complexity
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1427.860821
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xlogp Value
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0.1899
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Heavy Count
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59
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Rot Bonds
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33
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Hbond acc
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15
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Hbond Donor
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8
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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
CD33-11A1-v1417 (C)-#39 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.85 ng/mL
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Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing NB4 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
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| In Vitro Model | Acute promyelocytic leukemia, Acute promyelocytic leukemia with PML-RARA | NB4 cells | CVCL_0005 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3.43 ng/mL
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Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing HL60 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
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| In Vitro Model | Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation | HL60 cells | CVCL_0002 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
14.17 ng/mL
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Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing HEL92.1.7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
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| In Vitro Model | Acute erythroid leukemia, Erythroleukemia | HEL92.1.7 cells | CVCL_2481 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 1000 ng/mL | Negative CD33 expression (CD33-) | ||
| Method Description |
CD33-non-expressing Raji cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 31 concentrations.
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| In Vitro Model | EBV-related Burkitt lymphoma | Raji cells | CVCL_0511 | ||
CD33-11A1-v1417 (K334C)- (K392C)-#39 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
2.81 ng/mL
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Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing HL60 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 33 concentrations.
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| In Vitro Model | Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation | HL60 cells | CVCL_0002 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3.98 ng/mL
|
Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing NB4 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 33 concentrations.
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| In Vitro Model | Acute promyelocytic leukemia, Acute promyelocytic leukemia with PML-RARA | NB4 cells | CVCL_0005 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
12.1 ng/mL
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Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing HEL92.1.7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 33 concentrations.
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| In Vitro Model | Acute erythroid leukemia, Erythroleukemia | HEL92.1.7 cells | CVCL_2481 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 6323 ng/mL | Negative CD33 expression (CD33-) | ||
| Method Description |
CD33-non-expressing Raji cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 33 concentrations.
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| In Vitro Model | EBV-related Burkitt lymphoma | Raji cells | CVCL_0511 | ||
CD33-11A1-v1417 (K290C)- (K334C)-#39 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
4.58 ng/mL
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Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing HL60 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 32 concentrations.
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| In Vitro Model | Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation | HL60 cells | CVCL_0002 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
5.21 ng/mL
|
Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing NB4 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 32 concentrations.
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| In Vitro Model | Acute promyelocytic leukemia, Acute promyelocytic leukemia with PML-RARA | NB4 cells | CVCL_0005 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
20.78 ng/mL
|
Positive CD33 expression (CD33+++/++) | ||
| Method Description |
CD33-target-expressing HEL92.1.7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 32 concentrations.
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| In Vitro Model | Acute erythroid leukemia, Erythroleukemia | HEL92.1.7 cells | CVCL_2481 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 1000 ng/mL | Negative CD33 expression (CD33-) | ||
| Method Description |
CD33-non-expressing Raji cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e., no antibody conjugated to the drug) in duplicate at 32 concentrations.
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| In Vitro Model | EBV-related Burkitt lymphoma | Raji cells | CVCL_0511 | ||
References