154589-96-5

中文名稱硫磺酰亞胺

英文名稱 StaupriMide

CAS 154589-96-5

分子式 C35H28N4O5

分子量 584.62

MOL 文件 154589-96-5.mol

更新日期 2023/03/20 15:41:19

154589-96-5 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 常見問題列表

基本信息

中文別名

抑胃酶氨酰U丙基亞胺

英文別名

Stauprimide
Stauprimide-d5
benzaMide deriv.
N-Benzoyl-7-oxostaurosporine
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-
[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

所屬類別

生物化工：胺、酸和鹽

物理化學(xué)性質(zhì)

密度1.52±0.1 g/cm3(Predicted)

儲(chǔ)存條件-20°C

溶解度二甲基亞砜：>20mg/mL

酸度系數(shù)(pKa)9.51±0.70(Predicted)

形態(tài)黃色固體

顏色白色至米色

穩(wěn)定性Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS) GHS hazard pictograms

GHS07

警示詞警告

危險(xiǎn)性描述H315-H319-H335

防范說明P261-P271-P280

WGK Germany3

海關(guān)編碼2934999090

常見問題列表

生物活性

Stauprimide 是一種促進(jìn)胚胎干細(xì)胞 (ESC) 分化的星形孢菌素類似物。Stauprimide 與 MYC 轉(zhuǎn)錄因子 NME2 結(jié)合并阻斷其在 ESC 中的核定位，導(dǎo)致 MYC 轉(zhuǎn)錄的下調(diào), 是一種非廣譜抑制劑。

體外研究

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.

體內(nèi)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.

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154589-96-5

基本信息

物理化學(xué)性質(zhì)

安全數(shù)據(jù)

常見問題列表