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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[1][2].

Product Specifications

CAS Number

2177298-99-4

UNSPSC

12352005

Target

RET

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/hg-6-63-01.html

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

Molecular Formula

C31H31ClF3N5O

Molecular Weight

582.06

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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