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Cantrixil

CAS No. : 2135511-22-5

MCE 国际站：Cantrixil

产品活性：Cantrixil (TRX-E-002-1) 是 TRX-E-002 的活性对映异构体，是第二代超级苯并吡喃 (SBP) 化合物。Cantrixil 增加磷酸化 c-Jun 水平，导致卵巢癌细胞中半胱天冬酶介导的细胞凋亡。Cantrixil 对广泛的癌症表型具有有效的抗癌活性。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: 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.
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).
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.
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).

In Vivo: TRX-E-002-1 (100 mg/kg/day; IP; for 13-14 days) significantly inhibits tumour growth in disseminated ovarian cancer mouse model.
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.
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).
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.

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