WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206594
CAS#: 865200-20-0
Description: Giripladib, also known as PLX-695, is a cPLA2 specific inhibitor. Treatment with PLA-695 attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. PLA-695 in combination with irradiation (IR) significantly reduced migration and proliferation in endothelial cells (HUVEC & bEND3) and induced cell death and attenuated invasion by tumor cells (LLC &A549). In a heterotopic tumor model, the combination of PLA-695 and radiation delayed growth in both LLC and A549 tumors. LLC and A549 tumors treated with a combination of PLA-695 and radiation displayed reduced tumor vasculature.
Hodoodo Cat#: H206594
Name: Giripladib
CAS#: 865200-20-0
Chemical Formula: C41H36ClF3N2O4S
Exact Mass: 744.20
Molecular Weight: 745.254
Elemental Analysis: C, 66.08; H, 4.87; Cl, 4.76; F, 7.65; N, 3.76; O, 8.59; S, 4.30
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Synonym: PLA-695; PLA 695; PLA695; Giripladib
IUPAC/Chemical Name: 4-(3-(1-benzhydryl-5-chloro-2-(2-(((2-(trifluoromethyl)phenyl)methyl)sulfonamido)ethyl)-1H-indol-3-yl)propyl)benzoic acid
InChi Key: NHHBNHIPCSPSHQ-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(O)C1=CC=C(CCCC2=C(CCNS(=O)(CC3=CC=CC=C3C(F)(F)F)=O)N(C(C4=CC=CC=C4)C5=CC=CC=C5)C6=C2C=C(Cl)C=C6)C=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 745.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Duvernay MT, Matafonov A, Lindsley CW, Hamm HE. Platelet Lipidomic Profiling:
Novel Insight into Cytosolic Phospholipase A2α Activity and Its Role in Human
Platelet Activation. Biochemistry. 2015 Sep 15;54(36):5578-88. doi:
10.1021/acs.biochem.5b00549. Epub 2015 Sep 1. PubMed PMID: 26295742.
2: Thotala D, Craft JM, Ferraro DJ, Kotipatruni RP, Bhave SR, Jaboin JJ, Hallahan
DE. Cytosolic phospholipaseA2 inhibition with PLA-695 radiosensitizes tumors in
lung cancer animal models. PLoS One. 2013 Jul 19;8(7):e69688. doi:
10.1371/journal.pone.0069688. Print 2013. PubMed PMID: 23894523; PubMed Central
PMCID: PMC3716600.
