DHODH inhibitor M62

Chemical Structure : DHODH inhibitor M62

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货号: PC-49788Not For Human Use, Lab Use Only.

DHODH inhibitor M62 is a potent, selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 6.9 nM.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote
1 g		Get quote

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生物&药学活性

DHODH inhibitor M62 is a potent, selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 6.9 nM.
M62 inhibits the proliferation of human CRC cells in vitro with IC50 values ranging from 10.61 to 72.30 nM, HCT116 and HT29 cells are most sensitive (IC50 values of 10.61 and 23.84 nM, respectively).
M62 shows slightly cytotoxicity against human normal colon endothelial cells (NCM460 and HCoEpiC cells IC50 of 238.77 and 263.60 nM, respectively).
M62 induces S phase arrest in CRC cells, modulates multiple gene expression changes in CRC cells, significantly upregulates genes DDB2, DDIT3, GADD45A and TP53, downregulates EIF4B, HSP90AB, and RPS6 gene.
M62 induces the generation of ROS and mitochondrial superoxide, and decreases the production of ΔΨm and ATP, induces DNA damage in CRC cells.
M62 inhibits the expression of DNA repair proteins (ATM, RAD51, BRCA1, and 53BP1) and inhibits the PI3K/AKT/mTOR signaling pathway in CRC cells.
M62 (40 mg/kg, once daily oral gavage) inhibits subcutaneous CRC tumor growth in HCT116 xenograft models.

物理化学性质&存储条件

分子量	503.81
分子式	C21H15ClF5N3O4
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	(S,Z)-N-(2-chloro-6-fluorophenyl)-4-(2-cyano-3-hydroxybut-2-enamido)-5-fluoro-2-((1,1,1-trifluoropropan-2-yl)oxy)benzamide

参考文献

1. Li C, et al. Design, synthesis, and biological evaluation of a novel series of teriflunomide derivatives as potent human dihydroorotate dehydrogenase inhibitors for malignancy treatment. J Med Chem. 2021;64(24):18175-18192.

2. Xiaowei Yang, et al. A novel and potent dihydroorotate dehydrogenase inhibitor suppresses the proliferation of colorectal cancer by inducing mitochondrial dysfunction and DNA damage. https://doi.org/10.1002/mog2.6