| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S84817-5mg买3赠1 |
99.10% | ￥450.00 |
7 | - | - | - | - |
|
S84817-10mg促销 |
99.10% | ￥580.00 ￥464.00 |
5 | - | - | - | - |
|
S84817-50mg促销 |
99.10% | ￥1970.00 ￥1570.00 |
2 | - | - | - | - |
|
| 产品描述： | AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research | ||||||||||||||||||||
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| 靶点： | Arenavirus;DNA/RNA Synthesis;Apoptosis;Caspase;Bcl-2 Family;Dehydrogenase | ||||||||||||||||||||
| 体外研究： | AVN-944 (0-1 μM, 48 h) inhibits growth of human multiple myeloma (MM) cell lines in a dose-dependent manner. AVN-944 (800 nM, 0-72 h) induces apoptosis in MM cell lines via a caspase-independent, Bax/AIF/Endo G pathway. AVN-944 (0-200 nM) enhances the cytotoxicity of Doxorubicin (HY-15142A) and Melphalan (HY-17575). AVN-944 inhibits the proliferation of the human MV-4-11 and murine Ba/F3-Flt3-ITD-dependent cell lines with IC50 values of 26 and 30 nM, respectively. AVN-944 (0-32 μM, 48 h) shows good activity against arenavirus infection at low doses (7.5 μM) with less cytotoxicity. AVN-944 (0-6.4 μM, 48 h) does not reduce the viability of peripheral blood mononuclear cells (PBMNCs). Cell Proliferation Assay Cell Line: RPMI8226, MM.1S, and U266 cells Concentration: 0, 100, 200, 300, 400, 600, 1000 nM Incubation Time: 48 h Result: Significantly inhibited the growth of RPMI8226, MM.1S, and U266 cells in a dose-dependent fashion, with 50% inhibition (IC50) values at 48 h of 450, 450, and 600 nM, respectively. Inhibited growth of drug-resistant cell lines, including Doxorubicin (Dox)-resistant RPMI8226-Dox40, Melphalan (Mel) resistant RPMI8226-LR5, and Dex (Dexamethasone) resistant MM.1R cells, with IC50 values similar to the parental drug-sensitive cell lines. Apoptosis Analysis Cell Line: MM.1S and RPMI8226 cells Concentration: 800 nM Incubation Time: 48 and 72 h Result: Induced apoptosis in MM cell lines. Western Blot Analysis Cell Line: MM.1S and RPMI8226 cells Concentration: 800 nM | ||||||||||||||||||||
| 体内研究： | AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice. Animal Model: Balb/c mice (leukemia model, using Ba/F3 cells transduced with an activating human Flt-3 mutation injected into mice) Dosage: 75 or 150 mg/kg Administration: Orally, twice daily Result: Provided a significant increase in median survival time. Three of the 12 mice treated with 150 mg/kg AVN-944 were still alive on Day 35 when the study was terminated. | ||||||||||||||||||||
| 参考文献： | 1. Zimmermann AG, et al. Inosine-5'-monophosphate dehydrogenase: regulation of expression and role in cellular proliferation and T lymphocyte activation. Prog Nucleic Acid Res Mol Biol. 1998;61:181-209. 2. Huang M, et al. Guanine nucleotide depletion inhibits pre-ribosomal RNA synthesis and causes nucleolar disruption. Leuk Res. 2008 Jan;32(1):131-41. 3. Floryk D, et al. Antiproliferative effects of AVN944, a novel inosine 5-monophosphate dehydrogenase inhibitor, in prostate cancer cells. Int J Cancer. 2008 Nov 15;123(10):2294-302. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 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。 |
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北京