Chemical Structure : CSF1R-IN-3
CAS No.: 2760584-90-3
货号: PC-24733Not For Human Use, Lab Use Only.
CSF1R-IN-3 is a potent, selective and orally bioavailable CSF-1R inhibitor with IC50 of 2.1 nM.
规格 | 价格 | 库存 | 数量 |
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5 mg | ¥2480 | In stock | |
10 mg | ¥3980 | In stock | |
25 mg | ¥5980 | In stock | |
50 mg | Get quote | ||
100 mg | Get quote |
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CSF1R-IN-3 is a potent, selective and orally bioavailable CSF-1R inhibitor with IC50 of 2.1 nM.
CSF1R-IN-3 concentration-dependently inhibited the phosphorylation of CSF-1R and AKT in both BMDMs and PMA-differentiated THP-1 cells.
CSF1R-IN-3 shows high binding affinity to CSF-1R with a dissociation constant (KD) of 3.4 nM in SPR assays.
CSF1R-IN-3 (30 and 100 nM) potently inhibits the migration of macrophages.
CSF1R-IN-3 (30 and 100 nM) could downregulate the messenger RNA (mRNA) expressions of Il10, Arg1, Chil3, Retnla, and Vegf and upregulate the expressions of Il12, Tnf, Il6, and Nos2.
CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity.
分子量 | 574.69 | |
分子式 | C30H38N8O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
1-Piperazineacetamide, N-[5-[(Z)-[6-[[[[5-(1,1-dimethylethyl)-3-isoxazolyl]amino]carbonyl]amino]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]-4-methyl- |
1. Qi Lv, et al. J Med Chem. 2021 Dec 9;64(23):17184-17208.
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