Selpercatinib
Tocris Bioscience, part of Bio-Techne | Catalog # 7696
Potent and selective RET inhibitor
Key Product Details
Description
Potent and selective RET inhibitor
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
Molecular Weight
525.60
Formula
C29H31N7O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.51 | 20 |
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for Selpercatinib
For research use only
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