| 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 |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |