General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0QMWKP
ADC Name
JP2024177330A5 18G3-CPI
Synonyms
18G3-CPI;CD123-18G3-CPI
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Organization
Pfizer Inc.
Drug Status
Investigative
Drug-to-Antibody Ratio
2
Antibody Name
18G3
 Antibody Info 
Antigen Name
Interleukin-3 receptor subunit alpha (IL3RA)
 Antigen Info 
Payload Name
Cyclopropylpyrroloindoline (CPI) payload
 Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Undisclosed
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.25
ng/mL
CVCL_2119
Adult acute myeloid leukemia
Half Maximal inhibitory Concentration (lC50) 
0.38
ng/mL
CVCL_1818
Mantle cell lymphoma
Half Maximal inhibitory Concentration (lC50) 
0.41
ng/mL
CVCL_0064
Childhood acute monocytic leukemia
Half Maximal inhibitory Concentration (lC50) 
0.69
ng/mL
CVCL_1320
B-cell prolymphocytic leukemia
Half Maximal inhibitory Concentration (lC50) 
2.65
ng/mL
CVCL_1844
Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia
Half Maximal inhibitory Concentration (lC50) 
63.92
ng/mL
CVCL_0005
Acute promyelocytic leukemia, Acute promyelocytic leukemia with PML-RARA
Half Maximal inhibitory Concentration (lC50) 
> 84.4
ng/mL
CVCL_0002
Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.25 ng/mL 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 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 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 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 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 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
References
Ref 1 JP2024177330A5 - Google Patents