Payload Information
General Information of This Payload
| Payload ID | PAY0WDWDM |
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|---|---|---|---|---|---|---|
| Name | diABZI STING agonist 3 |
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| Synonyms |
diABZI STING agonist 3
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| Target | Stimulator of interferon genes protein (STING) | |||||
| Formula | C42H51N13O7 |
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| Isosmiles | CC1=NN(CC)C(C(/N=C(N2C/C=C/CN(C3=C4C=C(C(N)=O)C=C3OC)/C(N4)=N/C(C5=CC(C)=NN5CC)=O)\NC6=C2C(OCCCN7CCOCC7)=CC(C(N)=O)=C6)=O)=C1 |
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| PubChem CID | ||||||
| InChI |
InChI=1S/C42H51N13O7/c1-6-54-31(19-25(3)49-54)39(58)47-41-45-29-21-27(37(43)56)23-33(60-5)35(29)52(41)12-8-9-13-53-36-30(46-42(53)48-40(59)32-20-26(4)50-55(32)7-2)22-28(38(44)57)24-34(36)62-16-10-11-51-14-17-61-18-15-51/h8-9,19-24H,6-7,10-18H2,1-5H3,(H2,43,56)(H2,44,57)(H,45,47,58)(H,46,48,59)
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| InChIKey |
JGLMVXWAHNTPRF-UHFFFAOYSA-N
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| Pharmaceutical Properties | Molecule Weight |
849.954 |
Polar area |
253.05 |
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Complexity |
2768.216945 |
xlogp Value |
2.34794 |
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Heavy Count |
62 |
Rot Bonds |
16 |
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Hbond acc |
14 |
Hbond Donor |
4 |
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The activity data of This Payload
| Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
|---|---|---|---|---|---|---|
| Maximum Effect (Emax) | 136.1 | % |
THP-1 cells
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Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia
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| Maximum Effect (Emax) | 1601 | % |
THP-1 cells
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Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia
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| Half Maximal Effective Concentration (EC50) | <0.1 | nM |
THP1-Blue ISG cells
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Acute monoblastic leukemia
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| Half Maximal Effective Concentration (EC50) | <0.1 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | <1 | nM |
THP1-Dual cells
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Childhood acute monocytic leukemia
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| Half Maximal Effective Concentration (EC50) | <1 | nM |
THP1-Dual cells
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Childhood acute monocytic leukemia
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| Half Maximal Effective Concentration (EC50) | >100000 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | >100000 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | >100000 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | >100000 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 11 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 11 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 130 | nM |
PBMC cells
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Normal
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| Half Maximal Effective Concentration (EC50) | 130 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 130 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 130 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 130000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 160 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 186 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 190 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 2.6 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 200 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 200 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 270 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 3.9 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 3000 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 3000 | nM |
Cancer cells
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Multiple myeloma, Plasma cell myeloma
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Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 35 | nM |
H69AR cells
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Lung small cell carcinoma
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| Half Maximal Inhibitory Concentration (IC50) | >40000 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 54 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Effective Concentration (EC50) | 55 | nM |
H69AR cells
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Lung small cell carcinoma
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| Half Maximal Inhibitory Concentration (IC50) | 7.1 | nM | Undisclosed | Undisclosed | Undisclosed |
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
TZ-dSA3-12 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
87.71%
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| Method Description |
Compared to the PBS control group, the TZ-dSA3-12 (1 and 3mg kg-1) treatment group displayed significant and sustained suppression of tumor growth with an inhibition rate of 87.71% and 89.75%
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| In Vivo Model | N87 tumor-bearing BALB/c nude mice | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
89.75%
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| Method Description |
Compared to the PBS control group, the TZ-dSA3-12 (1 and 3mg kg-1) treatment group displayed significant and sustained suppression of tumor growth with an inhibition rate of 87.71% and 89.75%
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| In Vivo Model | N87 tumor-bearing BALB/c nude mice | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.08 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).
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| In Vitro Model | Ovarian serous adenocarcinoma | SKOV-3 cells | CVCL_0532 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.11- 0.28 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.13 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).
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| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
References