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Cantrixil (Synonyms: TRX-E-002-1)
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。
Cantrixil Chemical Structure
CAS No. : 2135511-22-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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| 500 mg |
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* Please select Quantity before adding items.
| 生物活性 |
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].
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体外研究
(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[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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[2]
| Cell Line: |
Ovarian cancer stem cells (OCSCs) |
| Concentration: |
0.2 μM |
| Incubation Time: |
2, 4, 8, 16, 24 hours |
| Result: |
Showed higher levels of phosphorylated c-Jun (p-c-Jun) and lower levels of phosphorylated-ERK (p-ERK).
Showed a time-dependent increase in p-c-Jun accompanied by a time-dependent increase in total c-Jun. |
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体内研究
(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[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 T1/2 of 2.5 hours, a Cmax of 8355 ng/mL and an AUC0-∞ of 40600 ng•h/mL[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Disseminated ovarian cancer mouse model[1] |
| Dosage: |
100 mg/kg (dissolved in 20% SBECD) |
| Administration: |
IP; once daily; for 13-14 days |
| Result: |
Significantly inhibited tumour growth and reduced excised tumour weight at termination by 50-72%. |
| Animal Model: |
Male female Sprague-Dawley rats[1] |
| Dosage: |
100 mg/kg (Pharmacokinetic Analysis) |
| Administration: |
IP |
| Result: |
Had a T1/2 of 2.5 hours, a Cmax of 8355 ng/mL and an AUC0-∞ of 40600 ng•h/mL. |
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| Clinical Trial |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
[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.
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