2. MAPK/ERK Pathway
  3. Raf p38 MAPK
  4. Exarafenib

Exarafenib  (Synonyms: RAF/KIN_2787)

Cat. No.: HY-147268 Purity: 99.68%
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Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity.

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

Exarafenib Chemical Structure

Exarafenib Chemical Structure

CAS No. : 2639957-39-2

Size Price Stock Quantity
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3200 In-stock
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Based on 1 publication(s) in Google Scholar

Exarafenib Related Antibodies

Top Publications Citing Use of Products

View All Raf Isoform Specific Products:

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BRaf c-Raf Raf

View All p38 MAPK Isoform Specific Products:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

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Description

Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity[1][2].

IC50 & Target[1]

RAF

 

p38 MAPK

 

In Vitro

Exarafenib (RAF/KIN_2787; 1-10000 nM; 24 h) inhibits RAF-dependent melanoma cell line growth. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines[1].

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

Exarafenib Related Antibodies

Cell Viability Assay[1]

Cell Line: Melanoma cell (A375 BRAFV600E, HMVII BRAFG469V; NRASQ61K, WM3629 BRAFD594G; NRASG12D, SKMEL2 NRASQ61R)
Concentration: 1-10000 nM
Incubation Time: 24 h
Result: Inhibited RAF-dependent melanoma cell line growth.
In Vivo

Exarafenib (RAF/KIN_2787; 3-30 mg/kg; Orally; twice daily; 29 days) is effective against BRAFmut & NRASmut human melanoma xenografts in vivo[1].

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

Animal Model: BALB/c nude mice xenograft models of BRAF and NRAS-mutant melanoma[1]
Dosage: 3, 5, 10, 20, 30 mg/kg
Administration: Orally; twice daily (BID); 29 days
Result: Was effective against BRAFmut & NRASmut human melanoma xenografts in vivo.
Molecular Weight

521.58

Formula

C26H34F3N5O3
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

CC1=CC=C(NC(N2C[C@@H](CC2)CC(F)(F)F)=O)C=C1C3=CC(N[C@H](C)CO)=NC(N4CCOCC4)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.73 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 1.9173 mL 9.5863 mL 19.1725 mL
5 mM 0.3835 mL 1.9173 mL 3.8345 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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: ≥ 2.5 mg/mL (4.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9173 mL 9.5863 mL 19.1725 mL 47.9313 mL
5 mM 0.3835 mL 1.9173 mL 3.8345 mL 9.5863 mL
10 mM 0.1917 mL 0.9586 mL 1.9173 mL 4.7931 mL
15 mM 0.1278 mL 0.6391 mL 1.2782 mL 3.1954 mL
20 mM 0.0959 mL 0.4793 mL 0.9586 mL 2.3966 mL
25 mM 0.0767 mL 0.3835 mL 0.7669 mL 1.9173 mL
30 mM 0.0639 mL 0.3195 mL 0.6391 mL 1.5977 mL
40 mM 0.0479 mL 0.2397 mL 0.4793 mL 1.1983 mL
50 mM 0.0383 mL 0.1917 mL 0.3835 mL 0.9586 mL
60 mM 0.0320 mL 0.1598 mL 0.3195 mL 0.7989 mL
80 mM 0.0240 mL 0.1198 mL 0.2397 mL 0.5991 mL
100 mM 0.0192 mL 0.0959 mL 0.1917 mL 0.4793 mL
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Exarafenib 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:

Exarafenib2639957-39-2RAF/KIN_2787Rafp38 MAPKRaf kinasesorallyBRAFmelanomaanticancerA375HMVIIWM3629SKMEL2Inhibitorinhibitorinhibit

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