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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 |
| Related RET Products |
|---|
| RPI-1
RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. |
| Pralsetinib
Pralsetinib (BLU-667) is a next generation highly potent, selective RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion. |
| Selpercatinib (LOXO-292)
Selpercatinib (LOXO-292) is a first-in-class, highly selective and potent small molecule RET inhibitor with good blood-brain barrier (BBB) penetration. and RET (G810R) with IC50 values of 14.0 nM, 24.1 nM and 530.7 nM, respectively. |
| AD80
AD80 is a multikinase inhibitor, it potently targets human RET, BRAF, S6K, and SRC. |
| AST 487
AST 487 is a RET kinase inhibitor,IC50 880 nM, inhibits RET autophosphorylation, downstream effector activation, and also inhibits Flt-3,IC50 520 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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