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

Belvarafenib  (Synonyms: HM95573; GDC-5573; RG6185)

Cat. No.: HY-109080 Purity: 99.71%
COA Handling Instructions

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Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

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

Belvarafenib Chemical Structure

Belvarafenib Chemical Structure

CAS No. : 1446113-23-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 126 In-stock
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10 mM * 1 mL in DMSO USD 126 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Belvarafenib:

Belvarafenib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Belvarafenib

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively[1].

IC50 & Target[1]

BRafV600E

7 nM (IC50)

CRAF

5 nM (IC50)

B-Raf

56 nM (IC50)

In Vitro

Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively[1].

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

Belvarafenib Related Antibodies
Clinical Trial
Molecular Weight

478.93

Formula

C23H16ClFN6OS
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C(C(C1=NC=N2)=CSC1=C2N)NC(C3=C4C(NC(C=CC=C5Cl)=C5F)=NC=C3)=C(C=C4)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (26.10 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 2.0880 mL 10.4399 mL 20.8799 mL
5 mM 0.4176 mL 2.0880 mL 4.1760 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • 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: ≥ 1.25 mg/mL (2.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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, 1 year; -20°C, 6 months (stored under nitrogen)

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: 99.71%

COA (249 KB) HNMR (139 KB) RP-HPLC (173 KB) LCMS (111 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0880 mL 10.4399 mL 20.8799 mL 52.1997 mL
5 mM 0.4176 mL 2.0880 mL 4.1760 mL 10.4399 mL
10 mM 0.2088 mL 1.0440 mL 2.0880 mL 5.2200 mL
15 mM 0.1392 mL 0.6960 mL 1.3920 mL 3.4800 mL
20 mM 0.1044 mL 0.5220 mL 1.0440 mL 2.6100 mL
25 mM 0.0835 mL 0.4176 mL 0.8352 mL 2.0880 mL
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Belvarafenib 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:

Belvarafenib1446113-23-0HM95573 GDC-5573 RG6185HM 95573HM-95573GDC5573GDC 5573GDC-5573RG6185RG 6185RG-6185RafRaf kinasesInhibitorinhibitorinhibit

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