SPP 86

Pricing Availability Delivery Time Qty
Cat.No. 5391 - SPP 86 | C16H15N5 | CAS No. 1357349-91-7
Description: Potent RET inhibitor
Chemical Name: 1-(1-Methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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

SPP 86 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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