MedKoo Cat#: 206594 | Name: Giripladib

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Giripladib
Giripladib
CAS#865200-20-0

Theoretical Analysis

MedKoo Cat#: 206594

Name: Giripladib

CAS#: 865200-20-0

Chemical Formula: C41H36ClF3N2O4S

Exact Mass: 744.2036

Molecular Weight: 745.25

Elemental Analysis: C, 66.08; H, 4.87; Cl, 4.76; F, 7.65; N, 3.76; O, 8.59; S, 4.30

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
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.