Stauprimide

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Stauprimide 

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。

Stauprimide

Stauprimide Chemical Structure

CAS No. : 154589-96-5

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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[1].

体外研究
(In Vitro)

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%[1].
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[1].
Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation[1].
Stauprimide (4-10 μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

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[1]

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[1].

Shanghai Jinpan Biotech Co Ltd 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[1]
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.

分子量

584.62

Formula

C35H28N4O5
CAS 号

154589-96-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献

  • [1]. Bouvard C, et al. Small molecule selectively suppresses MYC transcription in cancer cells. Proc Natl Acad Sci USA. 2017 Mar 28;114(13):3497-3502.

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