Home MAPK Raf inhibitor Belvarafenib For research use only.

Belvarafenib

Synonyms: HM95573, GDC5573, RG6185

Belvarafenib is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively.

Belvarafenib Chemical Structure

Belvarafenib Chemical Structure

CAS No. 1446113-23-0

Purity & Quality Control

Belvarafenib Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Biological Activity

Description Belvarafenib is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively.
Targets
CRAF [1]
(Cell-free assay)		 BRAF V600E [1]
(Cell-free assay)		 BRAF WT [1]
(Cell-free assay)
2 nM 7 nM 41 nM
In vitro
In vitro

Biochemically assayed for over 120 kinases, HM95573 shows the high selectivity toward BRAF mutant and CRAF kinases. The half maximal inhibition concentrations (IC50) of HM95573 against BRAFWT, BRAFV600E and CRAF kinases are 41nM, 7nM and 2nM, respectively. The strongly inhibited kinases subsequent to RAF kinases appear to be CSF1R (44nM), DDR1 (77nM) and DDR2 (182 nM). HM95573 potently inhibits the growth of mutant BRAF melanoma cell lines such as A375 (IC50: 57 nM) and SK-MEL-28 (69 nM) and of mutant NRAS melanoma cell lines such as SK-MEL-2 (53 nM) and SK-MEL-30 (24 nM). In addition, the phosphorylations of MEK and ERK downstream kinases associated with cell proliferation are effectively inhibited with treatment of HM95573 in mutant BRAF and mutant NRAS melanoma cells. HM95573 inhibits the downstream signaling in melanoma cells even in the presence of HGF which is known to mediate innate resistance to RAF inhibitors[1].
Cell Research Cell lines SUM-159 cells
Concentrations 5 μM
Incubation Time 48 h
Method

SUM-159 cells were treated with the pan-Raf inhibitor, belvarafenib, for 48 h
In Vivo
In vivo

HM95573 shows the excellent antitumor activity in mouse models xenografted with both of BRAF mutation cell lines (e.g. A375 and SK-MEL-28) and NRAS mutation cell lines (such as SK-MEL-2 and SK-MEL-30)[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04835805 Active not recruiting
Melanoma
Genentech Inc.
 May 13 2021 Phase 1
NCT03284502 Active not recruiting
Locally Advanced Solid Tumor|Metastatic Solid Tumor
Hanmi Pharmaceutical Company Limited
 May 22 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 478.93 Formula

C23H16ClFN6OS
CAS No. 1446113-23-0 SDF --
Smiles CC1=C(C2=C(C=C1)C(=NC=C2)NC3=C(C(=CC=C3)Cl)F)NC(=O)C4=CSC5=C4N=CN=C5N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (200.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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