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产品总数：60957
| 中文名称 |
CSRM617 hydrochloride
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|---|---|
| 中文别名 |
盐酸苄丝肼杂质C
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| 英文名称 |
CSRM617 hydrochloride
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| 英文别名 |
2-Amino-3-hydroxy-N'-(2,3,4-trihydroxybenzylidene)propanehydrazide hydrochloride (1:1);Dtxsid501019548;CSRM617 hydrochloride
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| Cas No. |
1353749-74-2
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| 分子式 |
C10H14ClN3O5
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| 分子量 |
291.69
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| 包装储存 |
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 产品详情 |
CSRM617 hydrochloride 是转录因子 ONECUT2 (OC2，雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂，在 SPR 测定中 Kd 为 7.43 uM，直接与 OC2-HOX 结构域结合。CSRM617 hydrochloride 通过切割 Caspase-3 和 PARP 诱导细胞凋亡 (apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中耐受性良好。
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| 生物活性 |
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a K d of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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| 性状 |
Solid
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| 体外研究(In Vitro) |
CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells.CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion.CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: SCID mice with 22Rv1 xenograft
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 参考文献 |
[1]. Rotinen M, et, al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24(12):1887-1898.
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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