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TSHR ligand A35

Chemical Structure : TSHR ligand A35

CAS No.: 1352286-61-3

TSHR ligand A35 (NCATS-SM4420, NCGC00241808)

Catalog No.: PC-21867Not For Human Use, Lab Use Only.

TSHR ligand A35 (NCATS-SM4420, NCGC00241808) is a specific Thyroid-stimulating hormone receptor (Thyrotropin receptor, TSHR) ligand, selectively activates TSHR-mediated cAMP accumulation in HEK-TSHR with EC50 of 240 nM, inhibits thyroid cancer (TC) cell proliferation and metastasis.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 521.57
Formula C31H27N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-((5-(3-benzyl-5-hydroxy-4-oxo-3,4-dihydroquinazolin-2-yl)-2-methoxybenzyl)oxy)phenyl)acetamide

References

1. Rhitajit Sarkar, et al. J Clin Endocrinol Metab. 2024 Feb 29:dgae114.

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