PLX-4720

PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1 (Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Product Specifications

CAS Number

[918505-84-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/plx-4720.html

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(NC1=CC=C(C(C(C2=CNC3=NC=C(C=C23)Cl)=O)=C1F)F)(CCC)=O

Molecular Formula

C17H14ClF2N3O3S

Molecular Weight

413.83

Precautions

H302, H315, H319, H335

References & Citations

[1]Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105 (8), 3041-3046.|[2]Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71 (7), 2750-2760.|[3]Nucera C, et al. B-Raf (V600E) and thrombospondin-1 promote thyroid cancer progression. Proc Natl Acad Sci U S A, 2010, 107 (23), 10649-10654.|[4]Rizzolio S, et al. Neuropilin-1 upregulation elicits adaptive resistance to oncogene-targeted therapies. J Clin Invest. 2018 Aug 31;128 (9) :3976-3990.