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Stauprimide (Synonyms: NBenzoyl7oxo Staurosporine)

Catalog No.GC17839

Stauprimide는 배아줄기세포(ESC) 분화를 촉진하는 스타우로스포린 유사체입니다. Stauprimide는 MYC 전사 인자 NME2에 결합하고 ESC에서 핵 국소화를 차단하여 MYC 전사의 하향 조절을 초래하는 비광역 스펙트럼 억제제입니다.

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Stauprimide Chemical Structure

Cas No.: 154589-96-5

Size 가격 재고 수량
500ug
US$87.00
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1mg
US$160.00
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5mg
US$421.00
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Sample solution is provided at 25 µL, 10mM.

Description of Stauprimide

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].

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].

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].

References:
[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.

Chemical Properties of Stauprimide

Cas No. 154589-96-5 SDF
Synonyms NBenzoyl7oxo Staurosporine
Chemical Name N-((5S,6S,7R,9S)-6-methoxy-5-methyl-14,16-dioxo-5,6,7,8,9,14,15,16-octahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
Canonical SMILES O=C(C1=C2C3=C(C4=C15)N(C6=CC=CC=C46)[C@H]7O[C@]([C@H]([C@@H](C7)N(C(C8=CC=CC=C8)=O)C)OC)(C)N3C9=CC=CC=C29)NC5=O
Formula C35H28N4O5 M.Wt 584.62
Solubility DMF: 25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.2 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Stauprimide

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1 mg 5 mg 10 mg
1 mM 1.7105 mL 8.5526 mL 17.1051 mL
5 mM 0.3421 mL 1.7105 mL 3.421 mL
10 mM 0.1711 mL 0.8553 mL 1.7105 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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