Selpercatinib

• CAT Number: I019594
• CAS Number: 2152628-33-4
• Molecular Formula: C29H31N7O3
• Molecular Weight: 525.60
• Purity: 98%
• Synonyms: 6-(2-hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxypyridin-3-yl)methyl]-3,6-diazabicyclo[3.1.1]heptan-3-yl]pyridin-3-yl]pyrazolo[1,5-a]pyridine-3-carbonitrile
• Target: RET
• Target Protein: P07949
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: IC50: 14.0 nM (RETWT), 24.1 nM (RETV804M), and 530.7 nM (RETG810R)
• InChI: InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3
• InChIKey: XIIOFHFUYBLOLW-UHFFFAOYSA-N
• SMILES: CC(C)(COC1=CN2C(=C(C=N2)C#N)C(=C1)C3=CN=C(C=C3)N4CC5CC(C4)N5CC6=CN=C(C=C6)OC)O

Selpercatinib（Cat No.:I019594）is a highly selective RET kinase inhibitor used to treat cancers driven by RET gene alterations, including non-small cell lung cancer (NSCLC), medullary thyroid cancer, and other solid tumors. By specifically targeting RET fusions and mutations, Selpercatinib disrupts cancer cell proliferation and survival with minimal impact on normal cells. Its precision therapy approach results in fewer off-target effects and better tolerability. Selpercatinib has demonstrated significant clinical efficacy in patients with RET-driven cancers, particularly those resistant to traditional treatments, improving outcomes and offering a promising targeted cancer therapy option.

Reference

[1]. Şentürk R, et, al. Quantitative bioanalytical assay for the selective RET inhibitors selpercatinib and pralsetinib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Jun 15;1147:122131.
[Content Brief]

[2]. Steven W. Andrews, et al. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors. WO2018071447A1.