Cantrixil  (Synonyms: TRX-E-002-1)

Cantrixil (TRX-E-002-1), an active enantiomer of TRX-E-002, is a second-generation super-benzopyran (SBP) compound. Cantrixil increases phosphorylated c-Jun levels resulting in caspase-mediated apoptosis in ovarian cancer cells. Cantrixil has potent pan anti-cancer activity against a broad range of cancer phenotypes^[1][2].

TRX-E-002-1 shows broad cytotoxic activity against ovarian, prostate and lung cancer cells, with IC₅₀ values of ≤0.1 μM (SK-OV-3, JAM, OVCAR-3 cells: IC₅₀=0.023-0.065 μM; DU145, PC3; C4-2B cells: IC₅₀=0.014-0.096 μM; A549 cells: IC₅₀=0.058 μM). Activity in pancreatic and colorectal cancer cells and glioblastoma cells are more variable^[1].
Cantrixil (0.2 μM; 2-24 hours) shows high levels of phosphorylated c-Jun (p-c-Jun) and low levels of phosphorylated-ERK (p-ERK)^[2].
Cantrixil (2.45 μM; 2-24 hours) induces a significant increase in both caspase-3/7 and caspase-9 activity at 16 and 24 hours^[2].
TRX-E-002-1 inhibits multiple cytochrome P450 drug-metabolizing enzymes, including CYP2C9, CYP2C8, CYP2C19, CYP2B6, CYP3A4, CYP2D6, CYP2A6 and CYP1A2. IC₅₀ values ranges from 1.5 to 75 μM (612-30,600 ng/mL)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TRX-E-002-1 (100 mg/kg/day; IP; for 13-14 days) significantly inhibits tumour growth in disseminated ovarian cancer mouse model^[1].
TRX-E-002-1 (100 mg/kg/day; IP; for 4 weeks) inhibits tumour growth and reduces terminal tumour burden by 77% in the recurrent ovarian cancer mouse model^[1].
TRX-E-002-1 (100 mg/kg/day; IP; for 18 days) significantly reduces terminal pancreatic tumour burden in a mouse model of pancreatic cancer (human Panc-1 pancreatic tumour cells implanted orthotopically into female NOD-SCID mice)^[1].
TRX-E-002-1 (100 mg/kg; IP) has a T_1/2 of 2.5 hours, a C_max of 8355 ng/mL and an AUC_0-∞ of 40600 ng•h/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

408.44

C₂₄H₂₄O₆

2135511-22-5

Solid

Off-white to light brown

OC1=CC=C([C@H](C2=CC=C(O)C=C2)[C@H](C3=CC(OC)=C(O)C(OC)=C3)CO4)C4=C1C

Room temperature in continental US; may vary elsewhere.

• [1]. Muhammad Wasif Saif, et al. Pharmacology and toxicology of the novel investigational agent Cantrixil (TRX-E-002-1). Cancer Chemother Pharmacol. 2017 Feb;79(2):303-314.  [Content Brief]

  [2]. Ayesha B Alvero, et al. TRX-E-002-1 Induces c-Jun-Dependent Apoptosis in Ovarian Cancer Stem Cells and Prevents Recurrence In Vivo. Mol Cancer Ther. 2016 Jun;15(6):1279-90.  [Content Brief]