Stauprimide|cas:154589-96-5|西域试剂

Stauprimide,99.0%

产品编号：Bellancom-N6747| CAS NO：154589-96-5| 分子式：C₃₅H₂₈N₄O₅| 分子量：584.62

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-N6747		￥2200.00	杭州北京（现货）
Bellancom-N6747		￥7000.00	杭州北京（现货）

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Stauprimide

产品介绍

Stauprimide 是一种促进胚胎干细胞 (ESC) 分化的星形孢菌素类似物。Stauprimide 与 MYC 转录因子 NME2 结合并阻断其在 ESC 中的核定位，导致 MYC 转录的下调, 是一种非广谱抑制剂。

生物活性

Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription.

体外研究

Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC₅₀ range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%.
Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC₅₀ of 780 nM in RXF 393 cells.
Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation.
Stauprimide (4-10 μM; 6 hours) acts with different EC₅₀s and with different degrees of maximal MYC mRNA down-regulation in different cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	Renal cancer cell line RXF 393 cells
Concentration:	2 μM, 4 μM, 8 μM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Inhibited cell proliferation at concentrations of 2-8 μM.

Western Blot Analysis

Cell Line:	Renal cancer cell line RXF 393 cells and CAKI-1 cells
Concentration:	5 μM
Incubation Time:	3 hours
Result:	Decreased nuclear localized NME2.

RT-PCR

Cell Line:	CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells
Concentration:	4μM, 6μM, 8μM, 10μM
Incubation Time:	6 hours
Result:	Suppressed MYC transcription in KG1A cells with an EC₅₀ of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide.

体内研究
(In Vivo)

Stauprimide (oral administration; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice
Dosage:	50 mg/kg
Administration:	Oral administration; 50 mg/kg; once daily; 30 days, 55 days
Result:	Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice
Dosage:	50 mg/kg
Administration:	Oral administration; 50 mg/kg; once daily; 30 days, 55 days
Result:	Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice
Dosage:	50 mg/kg
Administration:	Oral administration; 50 mg/kg; once daily; 30 days, 55 days
Result:	Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.