RU-301

Research use only, not for human use.

RU-301 is a novel pan-tam inhibitor.

RU-301 is a novel pan-tam inhibitor.

Cell Viability AssayCell Line:H1299, MDA-MB-231 cells Concentration:10 μM (for H1299); 2.5, 5 μM (for MDA-MB-231)Incubation Time:30 min (pre-incubate)Result:Suppressed Gas6-inducible native phosphorylation of native Axl.Partially blocked Gas6-induced activation of Akt and Erk in H1299 or MDA-MB-231 at 5 μM.Inhibited the Gas6-induced phosphorylation of not only native Axl but also native Tyro3 and MerTK in H1299 at 10 μM.Cell Migration Assay Cell Line:H1299, MDA-MB-231 cells Concentration:10 μM Incubation Time:24 h Result:Strongly suppressed Gas6-inducible motility of H1299 lung cancer cell line.Cell Viability Assay Cell Line:H1299 cells Concentration:10 μM Incubation Time:14 days Result:Suppressed clonogenic growth of H1299 cells when cultured in the presence of Gas6.

Animal Model:NOD/SCIDγ mice (4-6 week; lung cancer xenograft model).Dosage:100, 300 mg/kg Administration:Intraperitoneal injection; single daily for 4 daysResult:Significantly decreased tumor volume while body weights were not significantly different.Showed no notable toxicity but displayed good bioavailability with a t1/2 life of ~7-8 hours.Animal Model:WT or Mertk?/? male mice (fed NASH diet for 12 weeks).Dosage:300 mg/kg Administration: Intraperitoneal injection; 3 times a week for 4 weeks Result:Reduced liver fibrosis as indicated by decreases in liver picrosirius red staining and collagen gene expression.

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Tyrosine Kinase

TAM Receptor

pan-TAM receptor

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1110873-99-8

480.46

C21H19F3N4O4S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (208.13 mM)

Cc1cc(CSc2ccccc2C(=O)NCCNc2ccc(C(F)(F)F)cc2[N+](=O)[O-])on1

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(-20℃)

With Ice Pack

≥ 2 years