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.

Product information

CAS Number: 2379727-90-7

Molecular Weight: 487.90

Formula: C24H21ClF3N5O

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

Smiles: CN1C=C(C=N1)C1=CC=CC2NC3CCC(CC=3C=21)NC(=O)NC1C=C(C(Cl)=CC=1)C(F)(F)F

InChiKey: RTILPKXOEYEQSE-UHFFFAOYSA-N

InChi: InChI=1S/C24H21ClF3N5O/c1-33-12-13(11-29-33)16-3-2-4-21-22(16)17-9-14(6-8-20(17)32-21)30-23(34)31-15-5-7-19(25)18(10-15)24(26,27)28/h2-5,7,10-12,14,32H,6,8-9H2,1H3,(H2,30,31,34)

Technical Data

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

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).

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.

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.

Products are for research use only. Not for human use.