CSRM617 hydrochloride,99.0%
产品编号：Bellancom-122611A| CAS NO：1353749-74-2| 分子式：C10H14ClN3O5| 分子量：291.69
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CSRM617 hydrochloride
| 产品介绍 | 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 Kd 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 | ||||||||
| 体外研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||
| 体内研究 |
CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究 |
CSRM617 (50 mg/kg; p.o.; daily, for 20 d) inhibits tumor growth in SCID mice with 22Rv1 xenograft. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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| 性状 | Solid | ||||||||
| 溶解性数据 | |||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||
| 储存方式 |
-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||
| 参考文献 |
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