General Information of This Payload
Payload ID
PAY0CVJDO
Name
CD33-11A1-v1417 (C)-#39 Payload
Synonyms
CD33-11A1-v1417 (C)-#39 Payload
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Structure
Formula
C39H39Cl2N4O8P
Isosmiles
CNCCN(C)C(OC1=CC2=C([C@@H](CN2C(C34CC35CC5(C(N6C[C@H](C7=C6C=C(OP(O)(O)=O)C8=CC=CC=C78)CCl)=O)C4)=O)CCl)C9=CC=CC=C91)=O
InChI
InChI=1S/C39H39Cl2N4O8P/c1-42-11-12-43(2)36(48)52-30-13-28-32(26-9-5-3-7-24(26)30)22(15-40)17-44(28)34(46)37-19-38(21-39(37,38)20-37)35(47)45-18-23(16-41)33-27-10-6-4-8-25(27)31(14-29(33)45)53-54(49,50)51/h3-10,13-14,22-23,42H,11-12,15-21H2,1-2H3,(H2,49,50,51)/t22-,23-,37?,38?,39?/m1/s1
InChIKey
BGXPTLTVCACSPS-OJOJXYPESA-N
Pharmaceutical Properties
Molecule Weight
793.641
Polar area
148.95
Complexity
2285.942689
xlogp Value
6.323
Heavy Count
54
Rot Bonds
10
Hbond acc
7
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
CD33-11A1-v1417 (C)-#39 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.85 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 31 concentrations.
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
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.
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
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.
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.
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
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2.81 ng/mL
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.
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.
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
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.
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.
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
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
4.58 ng/mL
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.
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.
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.
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.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
References
Ref 1 Heteroaryl sulfone-based conjugation handles, methods for their preparation, and their use in synthesizing antibody drug conjugates