SJ-C1044

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].

Product Specifications

CAS Number

[2121503-76-0]

UNSPSC

12352005

Target

C-Fms; ERK; MEK; Raf; Ras; Tie; VEGFR

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sj-c1044.html

Smiles

FC(C(NC(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)=O)=C2)=CC=C2NC3=NC=CC=C3C4=NC=NC5=C4N=CN5

Molecular Formula

C25H14F7N7O

Molecular Weight

561.41

References & Citations

[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.