2177298-99-4
Chemical Structure
HG-6-63-01
- CAS No.: 2177298-99-4
- Formula:C31H31ClF3N5O
- Molecular Weight:582.06
InChIKey: QOGSFSFOXBJBFQ-VOTSOKGWSA-N
SMILES: CC1=CC=C(C(NC2=CC=C(CN3CCN(CC)CC3)C(C(F)(F)F)=C2)=O)C=C1/C=C/C4=C(Cl)C(C=CN5)=C5N=C4
Biological Activity: 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].
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HG-6-63-01 | 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. | |||||||||||||||||||||
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References
- [1]. Moccia M, et al. Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase. PLoS One. 2015 Jun 5;10(6):e0128364. [Content Brief]
- [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. [Content Brief]
