2. MAPK/ERK Pathway
  3. Raf
  4. Tovorafenib

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

Cat. No.: HY-15246 Purity: 99.89%
COA Handling Instructions

Molarity Calculator

Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.

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

Tovorafenib Chemical Structure

Tovorafenib Chemical Structure

CAS No. : 1096708-71-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
1 mg USD 61 In-stock
5 mg USD 130 In-stock
10 mg USD 230 In-stock
50 mg USD 744 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Tovorafenib Related Antibodies

Top Publications Citing Use of Products

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BRaf c-Raf Raf

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.

IC50 & Target[1]

RAF

 

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.

Tovorafenib Related Antibodies
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
Molecular Weight

506.29

Formula

C17H12Cl2F3N7O2S
CAS No.
Appearance

Solid

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
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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9752 mL 9.8758 mL 19.7515 mL
5 mM 0.3950 mL 1.9752 mL 3.9503 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.89%

COA (258 KB) HNMR (240 KB) LCMS (123 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Tovorafenib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tovorafenib1096708-71-2TAK-580 MLN 2480 BIIB-024TAK580TAK 580MLN2480MLN 2480MLN-2480BIIB024BIIB 024BIIB-024RafRaf kinasesInhibitorinhibitorinhibit

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