Selpercatinib

Name: Selpercatinib
Brand: Tocris Bioscience
SKU: 7696

Tocris Bioscience, part of Bio-Techne | Catalog # 7696

COA / SDS

Potent and selective RET inhibitor

Key Product Details

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)
Molecular Weight:	525.6

View Full Technical Details for Selpercatinib

Technical Data
Citations

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
InChi Key	XIIOFHFUYBLOLW-UHFFFAOYSA-N
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 for Selpercatinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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

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Reconstitution Calculator

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References for Selpercatinib

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