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  3. Stauprimide

Stauprimide 

Cat. No.: HY-N6747
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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.

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Stauprimide Chemical Structure

Stauprimide Chemical Structure

CAS No. : 154589-96-5

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Description

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].

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].

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.
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].

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.
Molecular Weight

584.62

Formula

C₃₅H₂₈N₄O₅

CAS No.

154589-96-5

SMILES

C[[email protected]@]([[email protected]@H]1OC)(O[[email protected]](N2C3=CC=CC=C43)([H])C[[email protected]]1N(C)C(C5=CC=CC=C5)=O)N6C(C2=C4C(C7=O)=C8C(N7)=O)=C8C9=C6C=CC=C9

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