1357349-91-7

SPP 86 is a potent RET Kinase inhibitor.

SPP86 is a potent cell permeable inihbitor of RET tyrosine kinase with an IC50 value of 8 nM and with some inhibitory activity at EphA1FGFR1Flt4Lck and Yes. SPP86 does not inhibit p38CSKKITPDGFSrc 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 μMsimilar to tamoxifen.

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