- 产品描述: CNDAC hydrochloride is a metabolite of the orally active agent Sapacitabine (HY-16445), and a nucleoside analog. CNDAC hydrochloride induces DNA damage and apoptosis
- 体外研究:
CNDAC 有一个独特的作用机制: 进入 DNA 后,它诱导单链断裂 (SSBs),当细胞经历第二个 S 期时,单链断裂 (SSBs) 转化为双链断裂 (DSBs)。 缺乏 Rad51D 和 XRCC3 可使细胞对 CNDAC (0-1 μM; 24 h) 敏感。 CNDAC (0-100 μM; 3 days) 抑制 HL-60 和 THP-1 细胞的增殖。 CNDAC (0-10 μM; 3-6 days) 诱导 HL-60 和 THP-1 细胞的凋亡。 CNDAC (6 μM; 48 h) 诱导 HCT116 细胞在延迟 S 期后的 G2 期停止细胞周期。 Cell Viability Assay Cell Line: Rad51D-deficient 51D1, Rad51D-complemented 51D1.3, wild-type AA8 and XRCC3-deficient irs1SF CHO cells Concentration: 0-1 μM Incubation Time: 24 h Result: Inhibited cell survival with IC50s of 0.006, 0.32, 0.48 and 0.0053 μM against Rad51D-deficient 51D1, Rad51D-complemented 51D1.3, wild-type AA8 and XRCC3-deficient irs1SF cell lines, respectively. Cell Proliferation Assay Cell Line: HL-60 and THP-1 cells Concentration: 0-100 μM Incubation Time: 3 days Result: Inhibited proliferation with IC50s of 1.5832 μM and 0.84 μM against HL-60 and THP-1 cells, respectively. Apoptosis Analysis Cell Line: HL-60 and THP-1 cells Concentration: 0, 0.5, 1, 2, 3, 4, 5 and 10 μM Incubation Time: 3, 4, 5, and 6 days Result: Induced apoptosis in both cells. Cell Cycle Analysis Cell Line: HCT116 Concentration: 6 μM Incubation Time: 48 h Result: 36 and 36% of cells were arrested in late-S and G2/M phases, respectively.
- 体内研究:
CNDAC (20mg/kg; i.p.; daily for 10 days) 显示小鼠抗肿瘤活性。 Animal Model: CDF1 mice, P388 tumor model Dosage: 20 mg/kg Administration: Intraperitoneal injection, daily for 10 days Result: Greatly increased the survival time and survival rate.
- 参考文献:
1. Liu XJ, et al. Sapacitabine, the prodrug of CNDAC, is a nucleoside analog with a unique action mechanism of inducing DNA strand breaks. Chin J Cancer. 2012 Aug;31(8):373-80. 2. Jagan S, et al. Bone Marrow and Peripheral Blood AML Cells Are Highly Sensitive to CNDAC, the Active Form of Sapacitabine. Adv Hematol. 2012;2012:727683. 3. Serova M, et al. Antiproliferative effects of sapacitabine (CYC682), a novel 2'-deoxycytidine-derivative, in human cancer cells. Br J Cancer. 2007 Sep 3;97(5):628-36. 4. Azuma A, et al. Nucleosides and nucleotides. 122. 2'-C-cyano-2'-deoxy-1-beta-D-arabinofuranosylcytosine and its derivatives. A new class of nucleoside with a broad antitumor spectrum. J Med Chem. 1993 Dec 24;36(26):4183-9.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.965 ml 19.823 ml 39.647 ml 5 mM 0.793 ml 3.965 ml 7.929 ml 10 mM 0.396 ml 1.982 ml 3.965 ml 50 mM 0.079 ml 0.396 ml 0.793 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)