Belvarafenib (HM95573)

Catalog No.S8853 Synonyms: GDC5573, RG6185

For research use only.

Belvarafenib (GDC5573, HM95573, RG6185) 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 (HM95573) Chemical Structure

CAS No. 1446113-23-0

Selleck's Belvarafenib (HM95573) has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description Belvarafenib (GDC5573, HM95573, RG6185) 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

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].

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].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 96 mg/mL
(200.44 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 478.93
Formula

C23H16ClFN6OS

CAS No. 1446113-23-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C2=C(C=C1)C(=NC=C2)NC3=C(C(=CC=C3)Cl)F)NC(=O)C4=CSC5=C4N=CN=C5N

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04835805 Recruiting Drug: Belvarafenib|Drug: Cobimetinib|Drug: Atezolizumab Melanoma Genentech Inc. May 13 2021 Phase 1
NCT03284502 Recruiting Drug: HM95573 cobimetinib|Drug: HM95573 cetuximab Locally Advanced Solid Tumor|Metastatic Solid Tumor Hanmi Pharmaceutical Company Limited May 22 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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