NR2F1 agonist 1

Names

[ CAS No. ]:
374101-64-1

[ Name ]:
NR2F1 agonist 1

Biological Activity

[Description]:

NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[In Vitro]

NR2F1 agonist 1（化合物 C26）（0.5 μM，1 μM；18 小时）显着诱导 D-HEp3 细胞中的荧光素酶表达[1]。 NR2F1 agonist 1（0.5 μM；7 天）显着下调磷酸肌醇 3-激酶 (PI3K) 信号通路[1]。 NR2F1 agonist 1（0.5 μM；7 天）显着上调 SOX9、RARβ 和 p27 的 mRNA 水平[1]。 NR2F1 agonist 1（0.5 μM；48 小时）在 D-HEp3 细胞中诱导细胞周期停滞在 G0/G1 期[1]。

[In Vivo]

NR2F1 agonist 1（0.5 mg/kg/天；腹腔注射；3 周）抑制小鼠模型肺部的原发性肿瘤生长和转移性生长[1]。 Animal Model: BALB/c nu/nu mice bearing GFP-tagged T-HEp3 PDX cells[1] Dosage: 0.5 mg/kg/day Administration: Intraperitoneal injection; injected for 3 weeks or for 1 week followed by DMSO for 2 weeks Result: Did not induce apoptosis of proliferating primary tumor cells, but exhibited metastasis inhibitory effect against T-HEp3 cells.

[References]

[1]. Khalil BD, et al. An NR2F1-specific agonist suppresses metastasis by inducing cancer cell dormancy. J Exp Med. 2022 Jan 3;219(1):e20210836.  

Chemical & Physical Properties

[ Molecular Formula ]:
C28H30N4OS

[ Molecular Weight ]:
470.63

Related Compounds