| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S85344-5mg促销 |
≥98%(HPLC) | ￥1750.00 ￥1570.00 |
7 | - | - | - | - |
|
S85344-10mg促销 |
≥98%(HPLC) | ￥2180.00 ￥1960.00 |
6 | - | - | - | - |
|
S85344-25mg促销 |
≥98%(HPLC) | ￥4820.00 ￥4330.00 |
3 | - | - | - | - |
|
S85344-50mg促销 |
≥98%(HPLC) | ￥6750.00 ￥6070.00 |
2 | - | - | - | - |
|
S85344-100mg促销 |
≥98%(HPLC) | ￥10000.00 ￥9000.00 |
3 | - | - | - | - |
|
| 产品描述： | PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells | ||||||||||||||||||||
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| 靶点： | IC50: 20 μM (ubiquitin-activating enzyme UBA1);E1/E2/E3Enzyme | ||||||||||||||||||||
| 体外研究： | PYZD-4409 (10-40 μM; 72 hours; myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells) induces cell death with a LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM. PYZD-4409 is preferentially cytotoxic to malignant cells over normal hematopoietic cells. PYZD-4409 (50 μM; 4 hours; K562 leukemia cells) treatment blocks the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34. PYZD-4] protein levels of Grp78 and Hsp70. In addition, PYZD-4409 increases levels of phospho-JNK and phospho-p38 mitogen-activated protein kinase, which have also been linked to ER stress and the unfolded protein response. Cell Cytotoxicity Assay Cell Line: Myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells Concentration: 10 μM, 20 μM, 30 μM, 40 μM Incubation Time: 72 hours Result: Induced cell death with a LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM. Western Blot Analysis Cell Line: K562 leukemia cells Concentration: 50 μM Incubation Time: 4 hours Result: Blocked the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34. RT-PCR Cell Line: K562 cellsConcentration: 0 μM, 10 μM, 25 μMIncubation Time: 24 hoursResult: Significantly increased both mRNA and protein levels of Grp78 and Hsp70. | ||||||||||||||||||||
| 体内研究： | PYZD-4409 (10 mg/kg; intraperitoneal injection; daily on alternate days; for 16 days; male severe combined immunodeficient mice) decreases tumor weight and volume without untoward toxicity. Animal Model: Male severe combined immunodeficient (SCID) mice with MDAY-D2 murine leukemia cells Dosage: 10 mg/kg Administration: Intraperitoneal injection; daily on alternate days; for 16 days Result: Delayed tumor growth and decreased tumor weight without untoward toxicity. | ||||||||||||||||||||
| 参考文献： | 1. Xu GW, et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010 Mar 18;115(11):2251-9. | ||||||||||||||||||||
| 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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