Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
CAS Number: 2379727-90-7
Molecular Weight: 487.90
Chemical Name: 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[5-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]urea
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
Antitumor agent-19 (Compound 23a; 10-50 µM; 1 hour; RAW 264.7 cells) treatment effectively induces the expression of M1-phenotype macrophage markers (IL-1β, TNF-α, iNOS and IL-12α) in a dose-dependent manner. Antitumor agent-19 is found to dose-dependently repolarize TAMs from M1 (anti-tumor) and M2 (pro-tumor).
Antitumor agent-19 (Compound 23a; 5 mg/kg; intraperitoneal injection; every other day; for 30 days; C57BL/6 female mice) is capable of remarkably inhibiting tumor growth of the LLC mouse model. Moreover, the synergy of Antitumor agent-19 with anti-PD-1 antibody has more superior antineoplastic effects than the exclusive use of either in vivo.
- Pei H, et al. iscovery of potent ureido tetrahydrocarbazole derivatives for cancer treatments through targeting tumor-associated macrophages. Eur J Med Chem. 2019 Sep 28;183:111741.
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