产品描述

acarbazine是三氮烯衍生物模具有抗肿瘤活性。在细胞周期的所有时期中，它烷基化DNA并与之交联，破坏DNA功能、细胞周期阻滞及凋亡；用于多种癌症治疗。

靶点（IC50 & Targe）

DNA polymerase beta

体外研究

Treatment of Dacarbazine sensitizes melanomas to lysis of peptide-specific CTL and it is is mediated through Fas-independent pathway[2].

体内研究

Treatment of combination of Axitinib and DTIC demonstrates significant antitumor activity against melanoma flank xenografts, reduces tumor cell proliferation and decreases the area of tumor necrosis and increases apoptosis. It also reduces meta-tasis-related factors and prolongs lifespan in mice[3].

细胞实验

Cell lines: UACC903 (UACC) cells

Concentrations: 20 μM

Incubation Time: 48 h

Method:Apotosis assay: UACC903 (UACC) cells treated with or without DTIC (20 μM) for 48 h are incubated with agonist anti-Fas Ab, CH-11 (500 ng/ml), for 5 and 16 h, respectively. To distinguish whether death/apoptosis is mediated by FasR, blocking anti-Fas Ab ZB4 (2 mg/ml) is added in the corresponding groups. At the end of incubation, cells are harvested and stained with propidium iodide and FITC-annexin V (BD PharMingen) for detecting apoptosis according to the instruction provided by the company. Ten thousand cells from each group are collected, and dead and apoptotic cells are analyzed without gating using CellQuest software.

(Only for Reference)

动物实验

Animal Models: B16F1 melanoma xenograft model(C57BL/6 mice background)

Formulation: 0.9% sodium chloride

Dosages: 80 mg/kg

Administration: i.p.

(Only for Reference)

参考文献

[1] Serrone L, et al. J Exp Clin Cancer Res. 2000, 19(1):21-34.

[2] Yang S, et al. J Immunol. 2004, 172(7):4599-608.

[3] Zhang XH, et al. Oncol Lett. 2013, 6(1):69-74.