TSHR ligand A35 (NCATS-SM4420, NCGC00241808) is a specific Thyroid-stimulating hormone receptor (Thyrotropin receptor, TSHR) inhibitor/ ligand, selectively activates TSHR-mediated cAMP accumulation in HEK-TSHR with EC50 of 240 nM, and inhibits thyroid cancer (TC) cell proliferation and metastasis.
A35 (NCATS-SM4420, NCGC00241808) does not inhibits proliferation of any cancer cells in the NCI-60 screen.
A35 (NCATS-SM4420, NCGC00241808) shows no detectable stimulatory activity at the closely related LH receptor (LHR) or FSH receptor (FSHR).
A35 (NCATS-SM4420, NCGC00241808) exertsan agonistic effect on the cAMP generation in normal thyrocytes with EC50 of 275 nM.
A35 (NCATS-SM4420, NCGC00241808) shows antiproliferative effects on thyroid cancer (TC) cells with IC50 values of 0.71 µM and 0.38 µM for MDA-T32 and MDA-T85, respectively.
A35 (NCATS-SM4420, NCGC00241808) inhibits pulmonary metastasis of MDA-T85F1 in mice.
A35 (NCATS-SM4420, NCGC00241808) is efficacious for CDX tumor growth inhibtion without decreases in mouse weights and liver function, reduces levels of Ki67 in the tumors and metastatic markers in lung tissues.