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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.
SPP86 is a potent cell permeable inihbitor of RET tyrosine kinase.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 10 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | NC1=NC=NC2=C1C(C#CC3=CC=CC=C3)=NN2C(C)C |
| 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) |
| InChI key | JQOIRTDBHMDWMT-UHFFFAOYSA-N |
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¥ 2528.88
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¥ 2013.69
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¥ 1779.22
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¥ 4039.86
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¥ 6330.00
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¥ 4404.38
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¥ 2573.97
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¥ 3319.60
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¥ 1749.15
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¥ 745.60
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