Payload Information
General Information of This Payload
| Payload ID | PAY0HBJLF |
|||||
|---|---|---|---|---|---|---|
| Name | CN115429893A ADC1 Payload |
|||||
| Synonyms |
CN115429893A ADC1 Payload
Click to Show/Hide
|
|||||
| Structure |
|
|||||
| Formula | C25H22FN3O6 |
|||||
| Isosmiles | CC(C(F)=C1)=C2CC[C@H](NC(O)=O)C3=C2C1=NC(C4=CC([C@@]5(O)CC)=C6COC5=O)=C3CN4C6=O |
|||||
| InChI |
InChI=1S/C25H22FN3O6/c1-3-25(34)14-6-18-21-12(8-29(18)22(30)13(14)9-35-23(25)31)20-16(28-24(32)33)5-4-11-10(2)15(26)7-17(27-21)19(11)20/h6-7,16,28,34H,3-5,8-9H2,1-2H3,(H,32,33)/t16-,25-/m0/s1
|
|||||
| InChIKey |
QYYIJXHUUIMSES-LMKMVOKYSA-N
|
|||||
| Pharmaceutical Properties | Molecule Weight |
479.464 |
Polar area |
130.75 |
||
Complexity |
1518.594434 |
xlogp Value |
2.78202 |
|||
Heavy Count |
35 |
Rot Bonds |
2 |
|||
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
CN115429893A ADC17 [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) |
71.59%
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
In the OV3756 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | OV3756 xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
71.59%
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
In the OV3756 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | OV3756 xenograft model | ||||
CN115429893A ADC4 [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) |
86.48%
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
In the MX-1 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
|
||||
| In Vivo Model | MX-1 xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
86.48%
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
In the MX-1 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
|
||||
| In Vivo Model | MX-1 xenograft model | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
109.48%
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
In the MX-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | MX-1 xenograft model | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
109.48%
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
In the MX-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | MX-1 xenograft model | ||||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
114.40%
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
In the Capan-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | Capan-1 xenograft model | ||||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
114.40%
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
In the Capan-1 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | Capan-1 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
157.8 ng/mL
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
MDA-MB-468 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
233 ng/mL
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
MX-1 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
|
||||
| In Vitro Model | Breast carcinoma | MX-1 cells | CVCL_4774 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
640 ng/mL
|
Positive Trop2 expression (Trop2+++/++) | ||
| Method Description |
MDA-MB-453 were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 15000 ng/mL | Negative Trop2 expression (Trop2-) | ||
| Method Description |
HGC27 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC4 for 120 h.
|
||||
| In Vitro Model | Gastric carcinoma | HGC27 cells | CVCL_1279 | ||
CN115429893A ADC16 [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) |
86.81%
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
In the OV3756 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
|
||||
| In Vivo Model | OV3756 xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
86.81%
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
In the OV3756 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
|
||||
| In Vivo Model | OV3756 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.645 nM
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
MCF-7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 250 nM) for 5 days.
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.645 nM
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
MCF-7 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 250 nM) for 5 days.
|
||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3.611 nM
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
JEG-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 1000 nM) for 5 days.
|
||||
| In Vitro Model | Gestational choriocarcinoma | JEG-3 cells | CVCL_0363 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
3.611 nM
|
Positive FR-alpha expression (FR-alpha+++/++) | ||
| Method Description |
JEG-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC16 (4x the first top concentration at 1000 nM) for 5 days.
|
||||
| In Vitro Model | Gestational choriocarcinoma | JEG-3 cells | CVCL_0363 | ||
CN115429893A ADC14 [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) |
93.86%
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
In the Hep-3 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
|
||||
| In Vivo Model | Hep-3 xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
93.86%
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
In the Hep-3 xenograft model, the ADCs were administered at 2.5 mg/kg (once, IV).
|
||||
| In Vivo Model | Hep-3 xenograft model | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
98.66%
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
In the Hep-3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | Hep-3 xenograft model | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
98.66%
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
In the Hep-3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | Hep-3 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
. nM
|
Negative B7H3 expression (B7H3-) | ||
| Method Description |
5000 CHO-K1 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
|
||||
| In Vitro Model | Normal | CHO-K1 cells | CVCL_0214 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.35 nM
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
5000 CHO-K1-B7-H3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
|
||||
| In Vitro Model | Normal | CHO-K1-B7-H3 cells | CVCL_0214 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.35 nM
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
5000 CHO-K1-B7-H3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
|
||||
| In Vitro Model | Normal | CHO-K1-B7-H3 cells | CVCL_0214 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
16.32 nM
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
5000 Calu-6 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
|
||||
| In Vitro Model | Lung adenocarcinoma | Calu-6 cells | CVCL_0236 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
16.32 nM
|
Positive B7H3 expression (B7H3+++/++) | ||
| Method Description |
5000 Calu-6 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC14 (4x the first top concentration at 200 ug/mL) for 7 days.
|
||||
| In Vitro Model | Lung adenocarcinoma | Calu-6 cells | CVCL_0236 | ||
CN115429893A ADC1 [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) |
105.80%
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | SKOV3 xenograft model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
105.80%
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
|
||||
| In Vivo Model | SKOV3 xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
36 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
MDA-MB-453 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
43 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
SK-BR-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
|
||||
| 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) |
62 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
BT-474 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
|
||||
| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
82 ng/mL
|
Positive HER2 expression (HER2+++/++) | ||
| Method Description |
NCI-N87 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10000 ng/mL | Negative HER2 expression (HER2-) | ||
| Method Description |
MDA-MB-468 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-468 cells | CVCL_0419 | ||