| CAS NO: | 839707-37-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 550.53 |
|---|---|
| Formula | C27H25F3N8O2 |
| CAS No. | 839707-37-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (181.6 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC(C)=NN4C)N=C3N(C)C2=O)=C1)C5=CC=CC(C(F)(F)F)=C5 |
| Synonyms | SC-1; SC 1; SC1 |
| In Vitro | In vitro activity: SC1 is a dual function small molecule inhibitor of both ERK1 and RasGAP and that simultaneous inhibition of both protein activities is required and sufficient for SC1’s effects on mES cells. SC1 activates Ras by inhibition of RasGAP function. SC1 improved the derivation efficiency and pluripotency of ES cells from C57BL/6. Three types of pluripotent stem cells (fES, ntES, and iPS cells) of the C57BL/6 background could generate full-term pups with high efficiency when cultured with SC1. Kinase Assay: Pluripotin (SC-1) inhibits in vitro kinase activity of RSK2 with EC50 of 2.5±1.8 μM. The RSK2 in vitro kinase inhibition assay utilized was a modification of protocols established by Nguyen et al. Additional protocols that confirmed the results depicted in Figure 4 and evaluated kinase inhibitory activity in a random selection of protein kinases were conducted at Reaction Biology Corporation (Malvern, PA). This was a miniaturized 33P-based screening assay. Cell Assay: Pluripotin, a dual kinase and GTPase inhibitor that promotes self-renewal, and then examined for tumorigenicity under limiting dilution conditions and clonogenic activity in soft agar. Pluripotin is inhibitory for p70S6K (IC50 = 1.4 μM ). |
|---|---|
| In Vivo | Six week old female NOD.SCID mice were randomly assigned to each of 20 treatment arms (n = 5/group). Treated and control colon tumor lines were enzymatically harvested and counted prior to dilution in RPMI 1640 (at 10, 100, 1,000, 10,000 cells/inoculum) for subcutaneous injection into the axillary region using a volume of 1 ml/mouse. Positive control groups were established such that tumor formation occurred in all mice in approximately one week thus confirming that all tumor lines studied were tumorigenic. Cell inocula for the positive control groups ranged from 1×106 to 2.5×106. Cell viability of the cell stocks was assessed by trypan blue exclusion prior to dilution for injection and was routinely found to be>95%. Tumor formation was monitored weekly using caliper measurements and the tumor mass was calculated as weight in mg = 1/2×(tumor length)×(tumor width)2. All experiments were terminated at 120 days or when tumor weight exceeded 2000 mg for any individual mouse. In selected studies, tumor cells were resuspended in Matrigel (50% concentration, BD Biosciences) prior to injection. |
| Animal model | Female NOD.SCID mice |
| Formulation & Dosage | NA |
| References | Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17266-71; PLoS One. 2014 Sep 11;9(9):e106916. |
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