Selpercatinib

Key Product Details

Product Description

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.

Product Specifications for Selpercatinib

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

Solubility

Preparing Stock Solutions for Selpercatinib

The following data is based on the product molecular weight 525.60.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.51 mL	47.56 mL	95.13 mL
1 mM	1.90 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	1.90 mL

Calculators

Background References

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

• Brandhuber 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
• Subbiah Selective RET kinase inhibition for patients with RET-altered cancers. Ann.Oncol. 2018 PMID: 29912274

Product Documents for Selpercatinib