Payload Information
General Information of This Payload
| Payload ID | PAY0YJUYC |
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| Name | Cyclopropylpyrroloindoline (CPI) payload |
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| Synonyms |
Cyclopropylpyrroloindoline (CPI) payload
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| Target | Human Deoxyribonucleic acid (hDNA) | |||||
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
JP2024177330A5 16D6-CPI [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) |
0.22 ng/mL
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High CD123 expression (CD123+++) | ||
| Method Description |
MOLM13 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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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) |
0.4 ng/mL
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High CD123 expression (CD123+++) | ||
| Method Description |
MV4-11 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.59 ng/mL
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Moderate CD123 expression (CD123++) | ||
| Method Description |
JVM3 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | B-cell prolymphocytic leukemia | JVM3 cells | CVCL_1320 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 105.34 ng/mL | Negative CD123 expression (CD123-) | ||
| Method Description |
HL60 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation | HL60 cells | CVCL_0002 | ||
JP2024177330A5 18G3-CPI [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) |
0.25 ng/mL
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High CD123 expression (CD123+++) | ||
| Method Description |
MOLM13 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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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) |
0.38 ng/mL
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Moderate CD123 expression (CD123++) | ||
| Method Description |
Granta519 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Mantle cell lymphoma | Granta519 cells | CVCL_1818 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.41 ng/mL
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High CD123 expression (CD123+++) | ||
| Method Description |
MV4-11 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Childhood acute monocytic leukemia | MV4-11 cells | CVCL_0064 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.69 ng/mL
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Moderate CD123 expression (CD123++) | ||
| Method Description |
JVM3 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | B-cell prolymphocytic leukemia | JVM3 cells | CVCL_1320 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
2.65 ng/mL
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Low CD123 expression (CD123+) | ||
| Method Description |
OCI-AML3 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia | OCI-AML3 cells | CVCL_1844 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
63.92 ng/mL
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Low CD123 expression (CD123+) | ||
| Method Description |
NB4 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Acute promyelocytic leukemia, Acute promyelocytic leukemia with PML-RARA | NB4 cells | CVCL_0005 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) | > 84.4 ng/mL | Negative CD123 expression (CD123-) | ||
| Method Description |
HL60 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation | HL60 cells | CVCL_0002 | ||
JP2024177330A5 20D7-CPI [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) |
0.32 ng/mL
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High CD123 expression (CD123+++) | ||
| Method Description |
MOLM13 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Adult acute myeloid leukemia | MOLM-13 cells | CVCL_2119 | ||
JP2024177330A5 3D1-CPI [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) |
0.33 ng/mL
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High CD123 expression (CD123+++) | ||
| Method Description |
MOLM13 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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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) | > 104.68 ng/mL | Negative CD123 expression (CD123-) | ||
| Method Description |
HL60 cell line cells were incubated with ADC or control at the following doses: 100 ng/ml, 25 ng/ml, 6.25 ng/ml, 1.56 ng/ml, 0.39 ng/ml, 0.09 ng/ml, 0.024 ng/ml, 0.006 ng/ml, 0.002 ng/ml and 0.0004 ng/ml. for 96 hours. Cell viability was measured with CelltiterGlo (Promega, Madison, WI), and luminescence was determined using a Victor plate reader (Perkin Elmer, Waltham, MA). 50% inhibition value (IC50) calculations were generated using XLfit (IDBS, Boston, MA) 4 parameter curve fit.
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| In Vitro Model | Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation | HL60 cells | CVCL_0002 | ||