Antitumor agent-19

Research use only, not for human use.

Antitumor agent-19 is an antitumor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator (EC50s: 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells).

Antitumor agent-19 is an antitumor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator (EC50s: 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells).(In Vitro):In RAW 264.7 cells, Antitumor agent-19 (10 μM, 20 μM, or 50 μM) effectively and dose-dependently induces the expression of M1-phenotype macrophage markers including IL-1β, TNF-α, iNOS and IL-12α. Antitumor agent-19 dose-dependently repolarizes tumor-associated macrophages from M1 (anti-tumor) and M2 (pro-tumor).(In Vivo):In C57BL/6 female mice with lewis lung cancer cells, Antitumor agent-19 (5 mg/kg; i.p.) remarkably inhibits tumor growth. The synergy of Antitumor agent-19 with anti-PD-1 antibody shows more superior antineoplastic effects in vivo.

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). RT-PCR Cell Line:RAW 264.7 cells Concentration:10 μM, 20 μM, or 50 μM Incubation Time:1 hour Result:Induced the expression of M1-phenotype macrophage markers (IL-1β, TNF-α, iNOS and IL-12α) in a dose-dependent manner.

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. Animal Model:Six-to eight-week-old C57BL/6 female mice with lewis lung cancer cells (LLC)Dosage:5 mg/kg Administration:Intraperitoneal injection; every other day; for 30 days Result:Remarkably inhibited tumor growth of the LLC mouse model.

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Others

Other Targets

Endogenous Metabolite

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2379727-90-7

487.91

C24H21ClF3N5O

>98% (HPLC)

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Cn1cc(cn1)-c1cccc2[nH]c3CCC(Cc3c12)NC(=O)Nc1ccc(Cl)c(c1)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years