FHND5071 is a RET Inhibitor. FHND5071 demonstrated potent inhibitory activities against various RET kinases and related cell lines. The pharmacokinetic results showed that compound FHND5071 had a targeted distribution in lung, liver, and brain tissues, exhibited high central nervous system penetration, and enhanced pharmacokinetics and pharmacodynamics. Western blot analysis indicated that compound FHND5071 significantly inhibited the phosphorylation of RET and downstream molecules ERK and AKT in tumor tissues. Furthermore, compound FHND5071 markedly inhibited tumor growth, showing good in vivo efficacy and significant intracranial antitumor activity.
MedKoo Cat#: 129088
Name: FHND5071
CAS#: 2761152-16-1
Chemical Formula: C30H30D3N9O
Exact Mass: 538.2996
Molecular Weight: 538.67
Elemental Analysis: C, 66.89; H, 6.74; N, 23.40; O, 2.97
The following data is based on the product molecular weight 538.67 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 |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Han Y, Wen T, Wang J, Shi J, Zhu Y. Preclinical Pharmacokinetics and in vitro
Metabolism of FHND5071, a Novel Selective RET Kinase Inhibitor. Eur J Drug Metab
Pharmacokinet. 2023 Sep;48(5):595-614. doi: 10.1007/s13318-023-00844-6. Epub
2023 Aug 2. PMID: 37528327.
2: Wang X, Miao H, Ye X, Shi J, Jiang C, Long Z, Wen T, Lei M, Zhu Y. Design and
Discovery of Novel Selective RET Inhibitors with High Central Nervous System
Penetration, Enhanced Pharmacokinetics, and Pharmacodynamics. J Med Chem. 2025
Jun 25. doi: 10.1021/acs.jmedchem.5c01109. Epub ahead of print. PMID: 40556477.