| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Cell lines | Leukemic cell lines(HL60, KG1a, U937) |
Preparation Method | To evaluate the effect of Guadecitabine treatment on Cancer Testis Antigen methylation, HL60, U937, and KG1a leukemic cell lines were treated with Guadecitabine and harvested on day 5. |
Reaction Conditions | Leukemic cell line were treated with Guadecitabine ( 0.1, 1.0 and 5μM) for 5 days. |
Applications | Guadecitabine treatment resulted in significant reductions of LINE-1 and NY-ESO-1 promoter methylation in HL60, U937 and KG1a cells, as determined by quantitative bisulfite pyrosequencing.MAGE-A3/6 was also hypomethylated following Guadecitabine treatment in all cell lines. |
Animal models | SCID mice |
Preparation Method | OVCAR3 cells were implanted into the hindquarters of SCID mice. After 2–3 weeks, when macroscopic tumors were formed, mice were treated with Guadecitabine for 5day. |
Dosage form | 3 mg/kg/day, subcutaneous treatment |
Applications | OVCAR3 tumors were treated with 3 mg/kg/d, 5 days Guadecitabine or vehicle control subcutaneously, 3 days later, injected with NY-ESO-1-specific CD8+ T-cells or vehicle control (PBS) intra-tumorally. The combination of Guadecitabine and NY-ESO-1 specific T-cells showed delayed tumor growth in comparison with mice treated with Guadecitabine or NY-ESO-1-specific CD8 +T-cells alone.these data suggest Guadecitabine treatment enhances NY-ESO-1-specific antitumor responses in vivo. |
| 产品描述 | Guadecitabine is a novel hypomethylating dinucleotide of decitabine and deoxyguanosine that is resistant to degradation by cytidine deaminase. Guadecitabine Sodium is the easily dissolved form of Guadecitabine[1]. Guadecitabine (0.1, 0.3, 1, 5μM, 48h) increased sensitivity to cisplatin for both the parental and the resistant A2780 cells. Although among other ovarian cancer cell lines, the parental A2780- cisplatin resistant cells is considered to be cisplatin “sensitive”, it has a relatively high IC50 for the drug[2]. Guadecitabine (50nM-2μM, 24h) pretreatment synergistically interacted with ASTX660 to induce cell death in five AML cell lines (MOLM-13, ML-2, MV4-11, PLB-985, KG-1) with various genetic backgrounds and representing different AML subtypes [3]. Tumor-bearing immune-deficient mice were exposed subcutaneously to Guadecitabine at doses of 3, 6.1, or 10 mg/kg, daily for 5 days, with tumors harvested on day 7. Most mice treated on the 5 day schedule with 10mg/kg/day Guadecitabine died; all mice treated with 6.1mg/kg/day Guadecitabine developed gastrointestinal toxicity. Minimal toxicity was observed in mice treated with 3mg/kg/day. Guadecitabine treatment caused hypomethylation of LINE-1 and NY-ESO-1 at all doses[4]. References: |
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