RAF265 Inhibitor CAS No. 927880-90-8

Cat. No.	Name	Size	Price
KI0013	RAF265	5 mg	$272
	RAF265	10 mg	$512
	RAF265	50 mg	$1552
	RAF265	100 mg	$2672

Chemical Characteristic

Product Name	RAF265
Synonyms	CHIR-265
CAS No.	927880-90-8
Molecular Weight	518.41
Formula	C₂₄H₁₆F₆N₆O
Chemical Name	1-Methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazol-2-amine
Smiles	c1(nc2c(n1C)ccc(c2)Oc1cc(ncc1)c1ncc([nH]1)C(F)(F)F)Nc1ccc(cc1)C(F)(F)F
Chemical Structure

Biological activities

RAF265 is a selective and potent inhibitor of RAF and VEGFR2. The IC50s of RAF265 against VEGFR2 and RAF are 1.3 and 1.2 µM, respectively.^[1] RAF265 inhibits RAF downstream signaling only in BRAF mutant cells. In vitro, addition of RAF265 to RAD001 leads to decreased AKT, S6, and Eukaryotic translation initiation factor 4E binding protein 1 phosphorylation in HCT116 cells. In HT29 and MDAMB231 cells, RAF265 alone shows significant activity with IC20 values of 1 to 3 µM and IC50 values of 5 to 10 µM. In the presence of 1 nM RAD001, the IC50 for RAF265 is 5 µM in A549 cells and 10 µM in HCT116 cells.^[2] RAF265 inhibits 2-deoxy-2-[¹⁸F]fluoro-d-glucose (FDG) accumulation in the A375M(B-Raf(V600E)) human melanoma cell culture at 28 hours in a dose-dependent manner. In vivo, RAF265 treatment for 1 day also inhibits FDG accumulation in tumor xenografts.^[3] In HCT116 xenografts in vivo, RAF265 treatment (12 mg/kg) shows 71% to 72% tumor volume inhibition percentage (TVI%). Combination of RAF265 and RAD001 shows enhanced antitumor activity and tumor growth delay in vivo. In HCT116 and MDAMB231 xenografts, the combination of RAD001 and RAF265 also significantly enhances the activation of caspase-3.^[2]

Protocols

Stock solution of RAF265 is made in DMSO and diluted in PBS shortly before use.^[2]

References

[1] Luan X, et al. Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors. Bioorg Med Chem. 2011, 19(11): 3312-3319. [2] Mordant P, et al. Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination. Mol Cancer Ther. 2010, 9(2): 358-368. [3] Tseng JR, et al. Use of DNA microarray and small animal positron emission tomography in preclinical drug evaluation of RAF265, a novel B-Raf/VEGFR-2 inhibitor. Neoplasia. 2011, 13(3): 266-275

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com