A RET inhibitor
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SPP 86

Item No. 37390

Product Insert (PDF)
Technical Information
Formal Name
1-(1-methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS Number
1357349-91-7
Molecular Formula
C16H15N5
Formula Weight
277.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
NC1=C2C(C#CC3=CC=CC=C3)=NN(C(C)C)C2=NC=N1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $125

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    10 mg

    $207

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    25 mg

    $413

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    Product Description

    SPP 86 is a RET inhibitor (IC50 = 0.008 µM).1 It is selective for RET over a panel of 44 serine/threonine/tyrosine kinases at 10 µM but does inhibit nine by greater than 75%. SPP 86 is also selective for RET over a panel of 63 receptor and non-receptor tyrosine kinases at 0.4 µM but does inhibit six, including RET, by greater than 75%. SPP 86 reduces the proliferation of HCT116 colon cancer and TPC-1 thyroid carcinoma cells (EC50s = 2.4 and 3.3 µM, respectively). It inhibits viral replication in BHK-21 cells infected with foot-and-mouth disease virus (FMDV) when used at a concentration of 5 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dinér, P., Alao, J.P., Söderlund, J., et al. Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors. J. Med. Chem. 55(10), 4872-4876 (2012).

    2. Wang, X., Liao, Y., Abdullah, S.W., et al. FGFR1-mediated enhancement of foot-and-mouth disease virus entry. Vet. Microbiol. 298:110237, (2024).