RU-301

• CAT Number: I018159
• CAS Number: 1110873-99-8
• Molecular Formula: C21H19F3N4O4S
• Molecular Weight: 480.46
• Purity: ≥95%
• Synonyms: 2-[(3-methyl-1,2-oxazol-5-yl)methylsulfanyl]-N-[2-[2-nitro-4-(trifluoromethyl)anilino]ethyl]benzamide
• InChI: InChI=1S/C21H19F3N4O4S/c1-13-10-15(32-27-13)12-33-19-5-3-2-4-16(19)20(29)26-9-8-25-17-7-6-14(21(22,23)24)11-18(17)28(30)31/h2-7,10-11,25H,8-9,12H2,1H3,(H,26,29)
• InChIKey: BPHPWPNHNGXNPR-UHFFFAOYSA-N
• SMILES: CC1=NOC(=C1)CSC2=CC=CC=C2C(=O)NCCNC3=C(C=C(C=C3)C(F)(F)F)[N+](=O)[O-]

RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis[1][2].
RU-301 (10 μM; 30 min) inhibits native TAMs activation in H1299 cells[1].
RU-301 (10 μM; 24 h) inhibits migration of H1299 and MDA-MB-231 cells[1].
RU-301 (10 μM; 14 days) inhibits growth of H1299 clonogenic cells under Gas6[1].
RU-301 (100, 300 mg/kg; i.p.; single daily for 4 days) inhibits tumor growth in lung cancer xenograft model[1].
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice[2].

Reference

[1]. Kimani SG, et al. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908.
 [Content Brief]

[2]. Cai B, et al. Macrophage MerTK Promotes Liver Fibrosis in Nonalcoholic Steatohepatitis. Cell Metab. 2020 Feb 4;31(2):406-421.e7.
 [Content Brief]