1357349-91-7

1357349-91-7 - Names and Identifiers

Name	1-(1-Methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Synonyms	SPP-86 SPP 86 1-(1-Methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-(1-methylethyl)-3-(2-phenylethynyl)-
CAS	1357349-91-7

1357349-91-7 - Physico-chemical Properties

Molecular Formula	C16H15N5
Molar Mass	277.32
Solubility	Soluble in DMSO
Storage Condition	-20℃
Use	SPP-86 is a potent inhibitor of selective RET tyrosine kinase with an IC50 value of 8 nM. SPP-86 inhibit RET-induced activation of PI3K/Akt and MAPK signaling pathways in MCF7 cells, and also inhibit RET-induced ERα phosphorylation.
Target	RET

1357349-91-7 - Reference

Reference

1: Alao JP, Michlikova S, Dinér P, Grøtli M, Sunnerhagen P. Selective inhibition of RET mediated cell proliferation in vitro by the kinase inhibitor SPP86. BMC Cancer. 2014 Nov 20;14:853. doi: 10.1186/1471-2407-14-853. PubMed PMID: 25409876; PubMed Central PMCID: PMC4252022.

1357349-91-7 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	3.606 ml	18.029 ml	36.058 ml
5 mM	0.721 ml	3.606 ml	7.212 ml
10 mM	0.361 ml	1.803 ml	3.606 ml
5 mM	0.072 ml	0.361 ml	0.721 ml

Last Update：2024-01-02 23:10:35

1357349-91-7 - Reference Information

biological activity	SPP-86 is a selective potent inhibitor of RET tyrosine kinase with an IC50 value of 8 nM. SPP-86 inhibition of RET-induced activation of PI3K/Akt and MAPK signaling pathways in MCF7 cells can also inhibit RET-induced ERα phosphorylation.
Target	IC50: 8 nM (RET).
Cell Line:	Thyroid cancer derived cell lines expressing the RET/PTC1 rearrangement (TPC1), BRAF V600E (8505C) or RAS G13R (C643) mutations. MCF7 cells (human breast cancer).
Concentration:	0-10 μM. 0-10 μM.
Incubation Time:	90 min. 30 min.
Result:	Inhibited RET- induced ERK1/2 phosphorylation in thyroid cancer cell lines. Inhibited RET- induced ERα phosphorylation and proliferation in MCF7 cells.