| Identification | Back Directory | [Name]
SJ-C1044 | [CAS]
2121503-76-0 | [Synonyms]
SJ-C1044
Benzamide, N-[2-fluoro-5-[[3-(9H-purin-6-yl)-2-pyridinyl]amino]phenyl]-3,5-bis(trifluoromethyl)- | [Molecular Formula]
C25H14F7N7O | [MOL File]
2121503-76-0.mol | [Molecular Weight]
561.41 |
| Chemical Properties | Back Directory | [Boiling point ]
610.422±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.576±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [pka]
8.419±0.10(predicted) |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
VEGFR2: 100 nM (IC50); BRAFWT: 331 nM (IC50); BRafV600E: 187 nM (IC50); CRAF: 257 nM (IC50); Tie2: 23 nM (IC50); CSF1R: 235 nM (IC50) | [References]
[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 |
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