Biochem/physiol Actions
SPP86 is a potent cell permeable inihbitor of RET tyrosine kinase with an IC50 value of 8 nM and with some inhibitory activity at EphA1, FGFR1, Flt4, Lck and Yes. SPP86 does not inhibit p38, CSK, KIT, PDGF, Src or BCR-ABL. SPP86 inhibited RET-mediated activation of the PI3K/Akt and MAPK pathways at doses of 0.1- 1 µM in a cell line expressing oncogenic RET and inhibited RET-induced ERα phosphorylation and proliferation in MCF7 cells with an IC50 value of 1.0 µM, similar to tamoxifen.
Packaging
5, 25 mg in glass bottle
| Colour | white to beige |
|---|---|
| Quality Level | 100 |
| InChI key | JQOIRTDBHMDWMT-UHFFFAOYSA-N |
| InChI | 1S/C16H15N5/c1-11(2)21-16-14(15(17)18-10-19-16)13(20-21)9-8-12-6-4-3-5-7-12/h3-7,10-11H,1-2H3,(H2,17,18,19) |
| Manufacturer | SIGMA-ALDRICH |
| Solubility | DMSO: 10 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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