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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Fms (CSF1R)-CSF1R-IN-3
CSF1R-IN-3

Chemical Structure : CSF1R-IN-3

CAS No.: 2760584-90-3

CSF1R-IN-3 (Compound 21)

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
5 mg ¥2480 In stock
10 mg ¥3980 In stock
25 mg ¥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 574.69
分子式 C30H38N8O4
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

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-

参考文献

1. Qi Lv, et al. J Med Chem. 2021 Dec 9;64(23):17184-17208.

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