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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.
| Molecular Weight | 277.32 |
| Formula | C16H15N5 |
| CAS Number | 1357349-91-7 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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