| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | RU-301 | ||||||||||||
| CAS | 1110873-99-8 | ||||||||||||
| Formula | C21H19F3N4O4S | ||||||||||||
| Molar Mass | 480.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kimani SG, et al. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. [2]. Cai B, et al. Macrophage MerTK Promotes Liver Fibrosis in Nonalcoholic Steatohepatitis. Cell Metab. 2020 Feb 4;31(2):406-421.e7. |