[CAS NO. 154589-96-5] Stauprimide
PRODUCTS SPECIFICATIONS [154589-96-5]
DESCRIPTION [154589-96-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 584.62 |
| Molecular Formula | C35H28N4O5 |
| SMILES | C[C@@]([C@@H]1OC)(O[C@](N2C3=CC=CC=C43)([H])C[C@H]1N(C)C(C5=CC=CC=C5)=O)N6C(C2=C4C(C7=O)=C8C(N7)=O)=C8C9=C6C=CC=C9 |
Summary
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 EC
50
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 IC
50
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 EC
50
s and with different degrees of maximal MYC mRNA down-regulation in different cell lines
[1]
.
MCE 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 EC 50 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] .
MCE 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Synonyms