Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C41H36ClF3N2O4S |
| Molecular Weight | 745.249 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)C1=CC=C(CCCC2=C(CCNS(=O)(=O)CC3=CC=CC=C3C(F)(F)F)N(C(C4=CC=CC=C4)C5=CC=CC=C5)C6=CC=C(Cl)C=C26)C=C1
InChI
InChIKey=NHHBNHIPCSPSHQ-UHFFFAOYSA-N
InChI=1S/C41H36ClF3N2O4S/c42-33-22-23-37-35(26-33)34(16-9-10-28-18-20-31(21-19-28)40(48)49)38(47(37)39(29-11-3-1-4-12-29)30-13-5-2-6-14-30)24-25-46-52(50,51)27-32-15-7-8-17-36(32)41(43,44)45/h1-8,11-15,17-23,26,39,46H,9-10,16,24-25,27H2,(H,48,49)
| Molecular Formula | C41H36ClF3N2O4S |
| Molecular Weight | 745.249 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Giripladib (PLA 695) is a Cytosolic phospholipase A2 (cPLA2) inhibitor. cPLA2 is associated with tumor progression and radioresistance in mouse tumor models. In these models, treatment with giripladib attenuates radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Combined with irradiation, giripladib reduces migration and proliferation in endothelial cells (HUVEC & bEND3) and induces cell death and attenuated invasion by tumor cells (LLC &A549). The combination treatment of giripladib and irradiation also delayes growth in both LLC and A549 tumors and results in reduced tumor vasculature. Phase I studies have been conducted to test the gastrointestinal safety of giripladib, and potential pharmacokinetic interaction with other compounds. A phase II study was terminated.
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 18:27:49 GMT 2023
by
admin
on
Fri Dec 15 18:27:49 GMT 2023
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| Record UNII |
1W10Q5H7WD
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| Record Status |
Validated (UNII)
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| Record Version |
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11721842
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8810
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CHEMBL2104969
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DB15426
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300000034212
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865200-20-0
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