Troxacitabine(Synonyms: BCH 4556; L-OddC; SPD 758)
Troxacitabine是一种具有强效抗肿瘤活性的二氧戊环类似物。
Troxacitabine Chemical Structure
CAS No. : 145918-75-8
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500 μg
￥12500
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1 mg
￥19000
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生物活性
Troxacitabine is nucleoside analog with potent anticancer activity.
体外研究 (In Vitro)
Troxacitabine has shown cutotoxicity in cancer cell lines of hepatocellular (HepG2), prostate (PC3, DUI45), non-small cell lung (NCI-H460, NCr-322M) colon (HT29), renal (CAK-l, A498, RXF-393, SNI2-C) and pancreatic origin (Pnac-Ol, MiaPa Ca) with IC50s range from 15-35 μM[1][2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Troxacitabine is highly active against the Panc-01 model, with TGI levels of 88.5% and 84.3% at the 10 and 25 mg/kg doses, respectively. The mean final tumor weights for animals given troxacitabine are also significantly smaller compared with vehicle controls. Troxacitabine has less activity against the MiaPaCa model[3]. Troxacitabine is very effective in human RCC tumor xenograft models, including CAM-i, A498, RXF-393, and SN12C carcinomas. Very good responses are ob served in animals bearing CAM-i, A498, and RXF-393 RCC tumors given i.p. doses of 10, 25, and 50 mg/kg twice a day for 5 days[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
213.19
Formula
C8H11N3O4
CAS 号
145918-75-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gourdeau H, et al. Antitumor activity of troxacitabine (Troxatyl) against anthracycline-resistant human xenografts. Cancer Chemother Pharmacol. 2002 Dec;50(6):490-6.
[2]. Kadhim SA, et al. Potent antitumor activity of a novel nucleoside analogue, BCH-4556 (beta-L-dioxolane-cytidine), in human renal cell carcinoma xenograft tumor models. Cancer Res. 1997 Nov 1;57(21):4803-10.
[3]. Weitman S, et al. The new dioxolane, (-)-2′-deoxy-3′-oxacytidine (BCH-4556, troxacitabine), has activity againstpancreatic human tumor xenografts. Clin Cancer Res. 2000 Apr;6(4):1574-8.
Animal Administration [3]
Mice[3]
Troxacitabine is administered i.v. to the animals at doses of 10 and 25 mg/kg on a daily 3 5 regimen. Gemcitabine is used as a positive control. The end points for the study included tumor growth inhibition (TGI), final weight, and the number of partial and complete tumor responses in the animals[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Gourdeau H, et al. Antitumor activity of troxacitabine (Troxatyl) against anthracycline-resistant human xenografts. Cancer Chemother Pharmacol. 2002 Dec;50(6):490-6.
[2]. Kadhim SA, et al. Potent antitumor activity of a novel nucleoside analogue, BCH-4556 (beta-L-dioxolane-cytidine), in human renal cell carcinoma xenograft tumor models. Cancer Res. 1997 Nov 1;57(21):4803-10.
[3]. Weitman S, et al. The new dioxolane, (-)-2′-deoxy-3′-oxacytidine (BCH-4556, troxacitabine), has activity againstpancreatic human tumor xenografts. Clin Cancer Res. 2000 Apr;6(4):1574-8.
LAT1-IN-1 (BCH) 是 L 型氨基酸转运蛋白 1 (LAT1) 的选择性竞争性抑制剂，可显著抑制细胞对氨基酸的摄取和 mTOR 磷酸化，从而抑制癌细胞生长并诱导细胞凋亡。
LAT1-IN-1 Chemical Structure
CAS No. : 20448-79-7
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Free Sample (0.1-0.5 mg)
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10 mM * 1 mL in Water
￥660
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50 mg
￥600
In-stock
100 mg
￥1000
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200 mg
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500 mg
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LAT1-IN-1 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Targeted Diversity Library
生物活性
LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis[1][2][3].
IC50 & Target
LAT1[1]
体外研究 (In Vitro)
LAT1-IN-1 (1-100 mM; 3 days; KYSE30 and KYSE150 esophageal cancer cells) treatment suppresses cell proliferation in a dose-dependent manner[1]. LAT1-IN-1 (30 mM; 24 and 48 hours; KYSE30 and KYSE150 cells) treatment significantly increases cell population in the G0/G1 phase in both KYSE30 and KYSE150 cells, indicating that LAT1-IN-1 induces cell cycle arrest at G1 phase[1]. LAT1-IN-1 (30 mM; 0-24 hours; KYSE30 and KYSE150 cells) treatment decreases phosphorylation of 4E-BP1 and p70S6K at 30 minutes and the decrease is continued for 24 hours. The amount of mTOR, 4E-BP1, and p70S6K proteins is slightly decreased[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
KYSE30 and KYSE150 esophageal cancer cells
Concentration:
1 mM, 3 mM, 5 mM, 10 mM, 20 mM, 30 mM, 40 mM, 50 mM, or 100 mM
Incubation Time:
3 days
Result:
Cell proliferation was suppressed in a dose-dependent manner.
[1]. Ohshima Y, et al. Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma. Cancer Sci. 2016 Oct;107(10):1499-1505.
[2]. Singh N, et al. Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods. Int J Mol Sci. 2018 Dec 21;20(1).
[3]. Wang Q, et al. L-type amino acid transport and cancer: targeting the mTORC1 pathway to inhibit neoplasia. Am J Cancer Res. 2015 Mar 15;5(4):1281-94. eCollection 2015.
