Linker Information
General Information of This Linker
| Linker ID |
LIN0DHDKU
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| Linker Name |
CN110072556B+Conjugate1+Linker
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| Linker Type |
Unclear
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C13H20N4O7
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| Isosmiles |
O=C(O)CC[C@@H](NC(CNC(/C=C\C(O)=O)=O)=O)C(NCCN)=O
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| InChI |
InChI=1S/C13H20N4O7/c14-5-6-15-13(24)8(1-3-11(20)21)17-10(19)7-16-9(18)2-4-12(22)23/h2,4,8H,1,3,5-7,14H2,(H,15,24)(H,16,18)(H,17,19)(H,20,21)(H,22,23)/b4-2-/t8-/m1/s1
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| InChIKey |
BEYYXUJYCYBEMZ-DLRBJTRDSA-N
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| Pharmaceutical Properties |
Molecule Weight
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344.324
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Polar area
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187.92
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Complexity
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484.1677
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xlogp Value
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-2.8321
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Heavy Count
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24
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Rot Bonds
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11
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Hbond acc
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6
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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
CN110072556B 1c-9476 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC53) |
0.285 nM
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Positive CD123 expression (CD123+++/++) | ||
| Method Description |
MOLM-13, 2000cell/well were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
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| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
2.78 nM
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Positive CD123 expression (CD123+++/++) | ||
| Method Description |
MV-4-11, 5000cell/well were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
CN110072556B 1c-8988 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC52) |
0.0302 nM
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Positive CD123 expression (CD123+++/++) | ||
| Method Description |
MOLM-13, 2000cell/well were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
Click to Show/Hide
|
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| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
29.4 nM
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Positive CD123 expression (CD123+++/++) | ||
| Method Description |
MV-4-11, 5000cell/well were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
Click to Show/Hide
|
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
CN110072556B 1c-8987 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC51) |
0.21 nM
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Positive CD123 expression (CD123+++/++) | ||
| Method Description |
MOLM-13, 2000cell/well were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
Click to Show/Hide
|
||||
| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.26 nM
|
Positive CD123 expression (CD123+++/++) | ||
| Method Description |
MV-4-11, 5000cell/well were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
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|
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
CN110072556B 1x-9574 [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) |
0.0294 nM
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Positive CXCR5 expression (CXCR5+++/++) | ||
| Method Description |
Cell line Rec-1 were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
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|
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| In Vitro Model | Mantle cell lymphoma | REC-1 cells | CVCL_1884 | ||
CN110072556B 1x-9024 [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) |
0.134 nM
|
Positive CXCR5 expression (CXCR5+++/++) | ||
| Method Description |
Cell line Rec-1 were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
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|
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| In Vitro Model | Mantle cell lymphoma | REC-1 cells | CVCL_1884 | ||
CN110072556B 1x-9580 [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) |
2.78 nM
|
Positive CXCR5 expression (CXCR5+++/++) | ||
| Method Description |
Cell line Rec-1 were plated at set initial densities in 96-well culture plate with white bottom in the appropriate growth media. 48hours later, the medium was replaced. The ADCs in 10 ul of culture medium inconcentrations from 10-5M to 10-13M were then pipetted to the cells. After 6 hours of incubation at 37°C and 5%carbon dioxide, the medium was changed and the antibody-drug conjugates or metabolites were added by pipette in 10 ul of culture medium in concentrations of 10-5M to 10-13M to the cells (triplicates) in 90 ul. After 96 h, the cell proliferation was detected using the MTT assay (ATCC, Manassas, Virginia, USA, catalogue No. 30-1010K). To this end, the MTT reagent was incubated with the cells for 4 h, followed by lysis of the cells overnight byaddition of the detergent. The dye formed was detected at 570 nm (Infinite M1000 proTecan). The measured data were used to calculate the ICso of the growth inhibition usingthe DRC (dose response curve). The proliferation of cells which were not treated with testsubstance but were otherwise identically treated was defined as the 100% figure.
Click to Show/Hide
|
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| In Vitro Model | Mantle cell lymphoma | REC-1 cells | CVCL_1884 | ||
