Description
PRGL493 is a potent and selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor. PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. PRGL493 is used for cancer research.
Product information
CAS Number: 2479378-45-3
Molecular Weight: 451.48
Formula: C25H21N7O2
Chemical Name: N-{13-[3-(5-methylfuran-2-yl)-1-phenyl-1H-pyrazol-4-yl]-1,8,10,12-tetraazatricyclo[7.4.0.0²,⁷]trideca-2,4,6,8,11-pentaen-11-yl}acetamide
Smiles: CC1=CC=C(O1)C1=NN(C=C1C1N=C(NC2=NC3=CC=CC=C3N21)NC(C)=O)C1C=CC=CC=1
InChiKey: QNWGOBIYAPLFMK-UHFFFAOYSA-N
InChi: InChI=1S/C25H21N7O2/c1-15-12-13-21(34-15)22-18(14-31(30-22)17-8-4-3-5-9-17)23-28-24(26-16(2)33)29-25-27-19-10-6-7-11-20(19)32(23)25/h3-14,23H,1-2H3,(H2,26,27,28,29,33)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 5 mg/mL (11.07 mM; ultrasonic and warming and heat to 60°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Acyl-CoA synthetase 4 (ACSL4) is an isoenzyme of the fatty acid ligase-coenzyme-A family taking part in arachidonic acid metabolism and steroidogenesis. PRGL493 ([3H]-AA (0.5 µCi/ml in serumfree medium) for 3 h; 48 hours) signifcantly inhibits the activity of ACSL4 in all three cell lines (MDA-MB-231, PC-3 and MA-10 Leydig cells), as evidenced by a reduction in AA-CoA levels.But PRGL493 has no effects on ACSL4 protein expression. PRGL493 (20-100 μM; 72 hours) inhibits the proliferation of highly aggressive breast and prostate cancer cells at an IC50 of 23 µM and 27 µM, respectively.
In Vivo:
PRGL493 (intraperitoneal injection; 250 μg/Kg; 43 and 34 consecutive days) decreases tumor volumes and inhibits tumor growth. Additionally, this compound results in a decrease in Ki67 protein expression and increases ER and AR expression in breast and prostate xenograft tumors, respectively.
Products are for research use only. Not for human use.
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