Home MAPK Raf inhibitor Tovorafenib (MLN2480)

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Tovorafenib (MLN2480) Raf Kinase Inhibitor

Cat.No.S7121

Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Tovorafenib (MLN2480) Raf inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 506.29

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Quality Control

Batch: Purity: 99.94%
99.94

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (197.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 506.29 Formula

C17H12Cl2F3N7O2S

 Storage (From the date of receipt)
CAS No. 1096708-71-2 Download SDF Storage of Stock Solutions

Synonyms BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101 SMILES CC(C1=NC=C(S1)C(=O)NC2=NC=C(C(=C2)C(F)(F)F)Cl)NC(=O)C3=C(C(=NC=N3)N)Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Raf
In vitro

Tovorafenib (MLN2480) inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo.

It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of this compound are found to vary across models and genetic contexts.

In vitro analysis of the drug combination of MLN2480 and TAK-733 (an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity. In addition, western blot analysis demonstrates the effect of it in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition. It only modestly inhibits PRAK.
In vivo

In vivo, Tovorafenib (MLN2480) shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.

This compound (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of it (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/26671150/
  • [5] https://pubmed.ncbi.nlm.nih.gov/28002790/

Applications

Methods Biomarkers Images PMID
Western blot p-ERK / ERK
S7121-WB1
28082416

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-31)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07206849 NOT_YET_RECRUITING
High Grade Glioma (HGG) of the Brain With BRAF Aberration; High Grade Glioma (III or IV); Diffuse Intrinsic Pontine Glioma; High Grade Glioma; WHO Grade 3 Glioma; WHO Grade 4 Glioma; Metastatic Brain Tumor
Nationwide Children's Hospital
 2026-11 PHASE2
NCT07441707 ACTIVE_NOT_RECRUITING
Low-grade Glioma
Ipsen
 2026-03-10 PHASE1
NCT06965114 RECRUITING
Hairy Cell Leukemia; Recurrent Hairy Cell Leukemia; Refractory Hairy Cell Leukemia
National Cancer Institute (NCI)
 2026-05-29 PHASE1; PHASE2
NCT05828069 RECRUITING
Recurrent Langerhans Cell Histiocytosis; Refractory Langerhans Cell Histiocytosis
National Cancer Institute (NCI)
 2024-03-28 PHASE2
NCT05566795 ACTIVE_NOT_RECRUITING
Low-grade Glioma; Rapidly Accelerated Fibrosarcoma (RAF) Altered Glioma; Pediatric Low-grade Glioma
Day One Biopharmaceuticals, Inc.
 2023-02-27 PHASE3
NCT04775485 RECRUITING
Low-grade Glioma; Advanced Solid Tumor
Day One Biopharmaceuticals, Inc.
 2021-04-22 PHASE2

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