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ROR1 inhibitor 24d

Chemical Structure : ROR1 inhibitor 24d

CAS No.:

ROR1 inhibitor 24d

货号: PC-24712Not For Human Use, Lab Use Only.

ROR1 inhibitor 24d is a potent, selective inhibitor of receptor tyrosine kinase-like orphan receptor ROR with IC50 of 17.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ROR1 inhibitor 24d is a potent, selective inhibitor of receptor tyrosine kinase-like orphan receptor ROR with IC50 of 17.6 nM.
ROR1 inhibitor 24d shows no activity against ROR2 (a homologous subtype of ROR1), also exhibits favorable selectivity on kinase profiling (126-kinase panel).
ROR1 inhibitor 24d demonstrates potent growth inhibition in ROR1-overexpressing cancer cell lines, including lung cancer cells (A549 and H1975) and breast cancer cells (MDA-MB-231) with IC50 of 0.47-0.64 uM.
ROR1 inhibitor 24d outperforms LDR102 in both kinase inhibition and cellular efficacy.
ROR1 inhibitor 24d effectively reduced colony formation in H1975, A549, and MDA-MB-231 cells in a dose-dependent manner.
ROR1 inhibitor 24d inhibited ROR1 downstream AKT/mTOR and NF-κB signaling pathways, ROR1 inhibitor 24d (5 uM) significantly reduced phospho-p65 levels in A549, MDA-MB-231, and H1975 cells.
ROR1 inhibitor 24d (5 mg/kg) demonstrates in vivo antitumor activity in A549 mouse xenograft models.

物理化学性质&存储条件

分子量 596.69
分子式 C36H32N6O3
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

3-((4-(4-Cyclopropoxyphenyl)pyrimidin-2-yl)amino)-N-(3-(6-methoxypyridin-3-yl)-1-methyl-1H-indol-6-yl)-4-methylbenzamide

参考文献

1. Qingquan Zheng, et al. J Med Chem. 2025 Jun 2. doi: 10.1021/acs.jmedchem.5c00189.

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