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SPP 86

Cat. No. 5391 Submit a Review Datasheet / COA / SDS
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Description: Potent RET inhibitor
Chemical Name: 1-(1-Methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥98% (HPLC)
Datasheet
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for SPP 86

SPP 86 is a potent RET inhibitor (IC50 = 8 nM). Also exhibits inhibitory activity at EphA1, FGFR1, Flt4, Lck and Yes. Inhibits proliferation of HCT 116 and TPC1 cells in vitro. Cell permeable.

Compound Libraries for SPP 86

SPP 86 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SPP 86

M. Wt 277.32
Formula C16H15N5
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1357349-91-7
PubChem ID 66549796
InChI Key JQOIRTDBHMDWMT-UHFFFAOYSA-N
Smiles CC(C)N1N=C(C#CC3=CC=CC=C3)C2=C1N=CN=C2N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SPP 86

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 27.73 100
ethanol 5.55 20

Preparing Stock Solutions for SPP 86

The following data is based on the product molecular weight 277.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.61 mL 18.03 mL 36.06 mL
5 mM 0.72 mL 3.61 mL 7.21 mL
10 mM 0.36 mL 1.8 mL 3.61 mL
50 mM 0.07 mL 0.36 mL 0.72 mL

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References for SPP 86

References are publications that support the biological activity of the product.

Dinér et al (2012) Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors. J.Med.Chem. 55 4872 PMID: 22559926

Klein et al (2011) Design, synthesis and characterization of a highly effective inhibitor for analog-sensitive (as) kinases. PLoS ONE 6 e20789 PMID: 21698101

If you know of a relevant reference for SPP 86, please let us know.

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Citations for SPP 86

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