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SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer[1].

VEGFR2: 100 nM (IC₅₀); BRAF^WT: 331 nM (IC₅₀); BRaf^V600E: 187 nM (IC₅₀); CRAF: 257 nM (IC₅₀); Tie2: 23 nM (IC₅₀); CSF1R: 235 nM (IC₅₀)

[1] Sungpyo Hong, et al. "Targeting RAF isoforms and tumor microenvironments in RAS or BRAF mutant colorectal cancers with SJ-C1044 for anti-tumor activity." Current Issues in Molecular Biology 45.7 (2023): 5865-5878. DOI:10.3390/cimb45070371