Cat. No.: HY-15246

Tovorafenib

(Synonyms: TAK-580; MLN 2480; BIIB-024)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase. Tovorafenib can be used for the study of glioma.

For research use only. We do not sell to patients.

Purity: 99.17%
CAS No.: 1096708-71-2
Formula: C₁₇H₁₂Cl₂F₃N₇O₂S
Molecular Weight:506.29

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tovorafenib Chemical Structure

CAS No.: 1096708-71-2

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase. Tovorafenib can be used for the study of glioma^[1].

IC₅₀ & Target^[1]

RAF

All Raf Isoforms :

In Vitro

Tovorafenib (TAK-580, MLN 2480) has effect on reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tovorafenib (TAK-580, MLN 2480) inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo. TAK-580 (MLN 2480) is most potent in BRAF mutant melanoma models but also has single agent activity in some RAS mutant models. The combination of MLN2480 with TAK-733 inhibits the growth of a broader range of RAS mutant tumor models than single agent TAK-580 (MLN 2480), including primary human tumor xenograft models of melanoma and CRC^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1096708-71-2
Appearance Solid
Molecular Weight 506.29
Formula C₁₇H₁₂Cl₂F₃N₇O₂S
Color White to off-white
SMILES

NC1=NC=NC(C(N[C@@H](C2=NC=C(C(NC3=NC=C(Cl)C(C(F)(F)F)=C3)=O)S2)C)=O)=C1Cl
Synonyms

TAK-580; MLN 2480; BIIB-024
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

All WBCell Migration/Invasion AssayCell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

Nat Chem Biol

MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition. [Abstract]

2026 May 12:10.1038/s41589-026-02212-2. PMID: 42120500
Sci Signal

MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells. [Abstract]

2025 Sep 2;18(902):eadw3231. PMID: 40892895
Int J Mol Sci

The Rab18/Ras/ERK/FosB/MMP3 Signaling Pathway Mediates Cell Migration Regulation by 2'3'-cGAMP. [Abstract]

2025 Jun 16;26(12):5758. PMID: 40565221

Tovorafenib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jun 16;26(12):5758. [Abstract]

Tovorafenib (HY-15246) (1 μM; 12 h), inhibitor of RAF, significantly reduced FosB2 expression induced by 2'3'-cGAMP in MDA-MB-231 cells.

Tovorafenib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jun 16;26(12):5758. [Abstract]

Tovorafenib (HY-15246; RAFi) (1 μM; 24 h) significantly reduced the migration of MDA-MB-231 cells.

Tovorafenib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jun 16;26(12):5758. [Abstract]

MTT assays of MDA-MB-231 cells under the indicated conditions. Tovorafenib (HY-15246; RAFi) (1 μM) was co-administrated with 2.5 μg/mL 2'3'-cGAMP for 24 h.
Neoplasia

STAMBP promotes lung adenocarcinoma metastasis by regulating the EGFR/MAPK signaling pathway. [Abstract]

2021 Jun;23(6):607-623. PMID: 34102455
bioRxiv

2026 Jun 25.
University of Arizona

2025.
bioRxiv

BRAFV600 and ErbB inhibitors directly activate GCN2 in an off-target manner to limit cancer cell proliferation. [Abstract]

2024 Dec 20:2024.12.19.629301. PMID: 39763857
Technical University of Munich

24.01.2018.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (197.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9752 mL

9.8758 mL

19.7515 mL

5 mM

0.3950 mL

1.9752 mL

3.9503 mL

10 mM

0.1975 mL

0.9876 mL

1.9752 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.67 mg/mL (1.32 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.67 mg/mL (1.32 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.67 mg/mL (1.32 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Elizabeth Grace Carideo Cunniff, et al. Abstract C146: Combination treatment with the investigational RAF kinase inhibitor MLN2480 and the investigational MEK kinase inhibitor TAK-733 inhibits the growth of BRAF mutant and RAS mutant preclinical models of

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9752 mL	9.8758 mL	19.7515 mL	49.3788 mL
	5 mM	0.3950 mL	1.9752 mL	3.9503 mL	9.8758 mL
	10 mM	0.1975 mL	0.9876 mL	1.9752 mL	4.9379 mL
	15 mM	0.1317 mL	0.6584 mL	1.3168 mL	3.2919 mL
	20 mM	0.0988 mL	0.4938 mL	0.9876 mL	2.4689 mL
	25 mM	0.0790 mL	0.3950 mL	0.7901 mL	1.9752 mL
	30 mM	0.0658 mL	0.3292 mL	0.6584 mL	1.6460 mL
	40 mM	0.0494 mL	0.2469 mL	0.4938 mL	1.2345 mL
	50 mM	0.0395 mL	0.1975 mL	0.3950 mL	0.9876 mL
	60 mM	0.0329 mL	0.1646 mL	0.3292 mL	0.8230 mL
	80 mM	0.0247 mL	0.1234 mL	0.2469 mL	0.6172 mL
	100 mM	0.0198 mL	0.0988 mL	0.1975 mL	0.4938 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Tovorafenib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

FDA-Approved Anticancer Drug Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Publications Citing Use of MedChemExpress (MCE) Tovorafenib

All Raf Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tovorafenib Related Classifications

HY-15246 Related Classifications