Antitumor agent-19

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Antitumor agent-19 is an antitumor agent that targets tumor-associated macrophages (TAMs) and can be used as a potent TAMs modulator. Antitumor agent-19 can increase TNF-alpha levels in tumor cells with EC₅₀ values???of 17.18 μM and 18.87 μM in RAW 264.7 cells and BMDM cells, respectively.

For research use only. We do not sell to patients.

Antitumor agent-19 Chemical Structure

CAS No. : 2379727-90-7

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1 mg	Get quote 3 - 4 weeks 2 - 3 weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
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•Related Small Molecules:

•Related Proteins:

View All TNF Receptor Isoform Specific Products:

View All Isoforms

TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

tumor-associated macrophages (TAMs)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BMDM	EC₅₀	18.87 μM Compound: 23a	Increase in TNF-alpha production in mouse BMDM cells incubated for 24 hrs by ELISA Increase in TNF-alpha production in mouse BMDM cells incubated for 24 hrs by ELISA	[PMID: 31605873]
RAW264.7	EC₅₀	17.18 μM Compound: 23a	Increase in TNF-alpha production in mouse RAW264.7 cells incubated for 24 hrs by ELISA Increase in TNF-alpha production in mouse RAW264.7 cells incubated for 24 hrs by ELISA	[PMID: 31605873]

In Vitro

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)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[1]

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.

In Vivo

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-to eight-week-old C57BL/6 female mice with lewis lung cancer cells (LLC)^[1]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; every other day; for 30 days
Result:	Remarkably inhibited tumor growth of the LLC mouse model.

Molecular Weight

487.90

Formula

C₂₄H₂₁ClF₃N₅O

CAS No.

2379727-90-7

SMILES

O=C(NC1CCC(NC2=C3C(C4=CN(C)N=C4)=CC=C2)=C3C1)NC5=CC=C(Cl)C(C(F)(F)F)=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]