Bioactivity | HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET[1][2]. |
CAS | 2177298-99-4 |
Formula | C31H31ClF3N5O |
Molar Mass | 582.06 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Moccia M, et al. Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase. PLoS One. 2015 Jun 5;10(6):e0128364. [2]. De Falco V, et al. The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer. Best Pract Res Clin Endocrinol Metab. 2017 Jun;31(3):307-318. |