STAUPRIMIDE

中文名称:

STAUPRIMIDE

中文同义词:

抑胃酶氨酰U丙基亚胺

英文名称:

StaupriMide

英文同义词:

Stauprimide;[9S-(9α,10β,11β,13α)]-N-(2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3,2,1-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-N-methylbenzamide;N-Benzoyl-7-oxostaurosporine;benzaMide deriv.;Stauprimide - CAS 154589-96-5 - Calbiochem;Benzamide, N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3,2,1-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-;Stauprimide-d5

CAS号:

154589-96-5

分子式:

C35H28N4O5

分子量:

584.62

EINECS号:

相关类别:

微生物代谢物;抗生素;Antibiotic;Chiral Reagents;Intermediates Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds

Mol文件:

154589-96-5.mol

密度 

1.52±0.1 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

DMSO: >20mg/mL

形态

Yellow solid

酸度系数(pKa)

9.51±0.70(Predicted)

颜色

white to beige

生物活性

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。

体外研究

Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC 50 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 IC 50 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 EC 50 s and with different degrees of maximal MYC mRNA down-regulation in different cell lines. 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 EC 50 of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide.

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.

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.

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 EC 50 of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide.

体内研究

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. 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.

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.

WGK Germany 

3