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Description: Potent and selective RET inhibitor
Chemical Name: 6-(2-Hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxy-3-pyridinyl)methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]pyrazolo[1,5-a]pyridine-3-carbonitrile
Purity: ≥98% (HPLC)

Biological Activity for Selpercatinib

Selpercatinib, is a potent and selective receptor tyrosine kinase RET inhibitor (EC50 = 4 nM). It shows > 100-fold selectivity for > 95% of 228 purified kinase domains in radiometric assays. In vitro, it inhibits proliferation of cancer cell lines containing RET mutations or gene fusions. In vivo, it inhibits tumor growth in diverse RET mouse models. Selpercatinib is orally bioavailable.

Compound Libraries for Selpercatinib

Selpercatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Selpercatinib

M. Wt 525.6
Formula C29H31N7O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2152628-33-4
PubChem ID 134436906
Smiles N#CC=1C=NN2C=C(OCC(O)(C)C)C=C(C=3C=NC(=CC3)N4CC5N(CC6=CN=C(OC)C=C6)C(C4)C5)C12

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 Selpercatinib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 10.51 20

Preparing Stock Solutions for Selpercatinib

The following data is based on the product molecular weight 525.6. 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
0.2 mM 9.51 mL 47.56 mL 95.13 mL
1 mM 1.9 mL 9.51 mL 19.03 mL
2 mM 0.95 mL 4.76 mL 9.51 mL
10 mM 0.19 mL 0.95 mL 1.9 mL

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Product Datasheets for Selpercatinib

References for Selpercatinib

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

Subbiah et al (2018) Selective RET kinase inhibition for patients with RET-altered cancers. Ann.Oncol. 29 1869 PMID: 29912274

Brandhuber et al (2016) The development of LOXO-292, a potent, KDR/VEGFR2-sparing RET kinase inhibitor for treating patients with RET-dependent cancers. International Conference on Molecular Targets and Cancer Therapeutics

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

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Keywords: Selpercatinib, Selpercatinib supplier, RET, tyrosine, kinases, selective, potent, inhibitors, inhibits, orally, bioavailable, Other, RTKs, 7696, Tocris Bioscience

Citations for Selpercatinib

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