Payload Information
General Information of This Payload
| Payload ID | PAY0HIZMH |
|||||
|---|---|---|---|---|---|---|
| Name | 5-[ (4-{[ (2S)-2- (fluoromethyl)piperazin-1-yl]methyl}-2-methoxyphenyl)methyl|]-N4-pentyl-5H-pyrrolo[3,2-d]pyrimidine-2,4-diamine |
|||||
| Synonyms |
5-[ (4-{[ (2S)-2- (fluoromethyl)piperazin-1-yl]methyl}-2-methoxyphenyl)methyl|]-N4-pentyl-5H-pyrrolo[3,2-d]pyrimidine-2,4-diamine
Click to Show/Hide
|
|||||
| Target | Toll-like receptor 7 (TLR7); Toll-like receptor 8 (TLR8) | |||||
| Structure |
|
|||||
| Formula | C25H36FN7O |
|||||
| Isosmiles | FC[C@@H]1CNCCN1CC(C=C2)=CC(OC)=C2CN3C(C(NCCCCC)=NC(N)=N4)=C4C=C3 |
|||||
| PubChem CID | ||||||
| InChI |
InChI=1S/C25H36FN7O/c1-3-4-5-9-29-24-23-21(30-25(27)31-24)8-11-33(23)17-19-7-6-18(13-22(19)34-2)16-32-12-10-28-15-20(32)14-26/h6-8,11,13,20,28H,3-5,9-10,12,14-17H2,1-2H3,(H3,27,29,30,31)/t20-/m1/s1
|
|||||
| InChIKey |
PPCZDQOHPSXCHC-HXUWFJFHSA-N
|
|||||
| Pharmaceutical Properties | Molecule Weight |
469.609 |
Polar area |
93.26 |
||
Complexity |
1049.330714 |
xlogp Value |
3.4158 |
|||
Heavy Count |
34 |
Rot Bonds |
11 |
|||
Hbond acc |
8 |
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
US20250025567A1 ExL1A1 [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) | > 50% | Positive CLDN6 expression (CLDN6+++/++) | ||
| Method Description |
ExL1A1 was tested in SCID mice that subcutaneously transplanted NUGC33, 3 mg/kg was administeredthrough the tail vein of the tumor-bearing mice.
|
||||
| In Vivo Model | NUGC-3 cells SCID mice model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | The ADC concentration required to produce 10,000 pg/mL TNF-alpha was evaluated. |
100- 1000 nM
|
Positive CLDN6 expression (CLDN6+++/++) | ||
| Method Description |
ExL1A1 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
|
||||
| In Vitro Model | Normal; Gastric adenocarcinoma | PBMC cells; NUGC3 cells | .;CVCL_1612 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | The ADC concentration required to produce 10,000 pg/mL INF-Gamma was evaluated. |
10- 100 nM
|
Positive CLDN6 expression (CLDN6+++/++) | ||
| Method Description |
ExL1A1 was tested in co-culture system consisting of Human peripheral blood mononuclear cells (PBMCs) and NUGC33 cells, with the concentration range of 5.5 uM to 0.97 uM,TNF-a and INF-y productions were measured.
|
||||
| In Vitro Model | Normal; Gastric adenocarcinoma | PBMC cells; NUGC3 cells | .;CVCL_1612 | ||