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Troxacitabine (BCH 4556) Sale

(Synonyms: 4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮,BCH 4556; L-OddC; SPD 758) 目录号 : GC34184

Troxacitabine (BCH 4556) 是具有有效抗癌活性的核苷类似物。

Troxacitabine (BCH 4556) Chemical Structure

Cas No.:145918-75-8

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Sample solution is provided at 25 µL, 10mM.

Description

Troxacitabine is nucleoside analog with potent anticancer activity.

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].

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].

[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.

实验参考方法

Animal experiment:

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].

References:

[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.

化学性质

Cas No. 145918-75-8 SDF
别名 4-氨基-1-[(2S)-2-(羟甲基)-1,3-二氧杂环戊-4-基]嘧啶-2-酮,BCH 4556; L-OddC; SPD 758
Canonical SMILES O=C1N=C(N)C=CN1[C@H]2O[C@@H](CO)OC2
分子式 C8H11N3O4 分子量 213.19
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.6907 mL 23.4533 mL 46.9065 mL
5 mM 0.9381 mL 4.6907 mL 9.3813 mL
10 mM 0.4691 mL 2.3453 mL 4.6907 mL
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