LY3009120

LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.

Product Specifications

CAS Number

[1454682-72-4]

Product Name Alternative

DP-4978

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Raf

Type

Reference compound

Related Pathways

Autophagy; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LY3009120.html

Concentration

10mM

Purity

98.66

Solubility

DMSO : ≥ 38 mg/mL

Smiles

O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C

Molecular Formula

C23H29FN6O

Molecular Weight

424.51

Precautions

H302, H315, H319, H335

References & Citations

[1]Vakana E, et al. LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer. Oncotarget. 2017 Feb 7;8 (6) :9251-9266|[2]Chen SH, et al. Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120. Cancer Discov. 2016 Mar;6 (3) :300-15|[3]Peng SB, et al. Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. Cancer Cell. 2015 Sep 14;28 (3) :384-98|[4]Henry JR, et al. Discovery of 1- (3,3-dimethylbutyl) -3- (2-fluoro-4-methyl-5- (7-methyl-2- (methylamino) pyrido[2,3-d]pyrimidin-6-yl) phenyl) urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumo