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首页-小分子抑制剂&激动剂-GPCR-Thyrotropin Receptor-TSHR ligand A35
TSHR ligand A35

Chemical Structure : TSHR ligand A35

CAS No.: 1352286-61-3

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TSHR ligand A35 (NCATS-SM4420, NCGC00241808)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 521.57
分子式 C31H27N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

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