2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl c-Kit PDGFR
  4. Flumatinib mesylate

Flumatinib mesylate  (Synonyms: HHGV678 mesylate)

Cat. No.: HY-13905 Purity: 99.87%
SDS COA Handling Instructions

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Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model.

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Flumatinib mesylate Chemical Structure

Flumatinib mesylate Chemical Structure

CAS No. : 895519-91-2

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Based on 1 publication(s) in Google Scholar

Other Forms of Flumatinib mesylate:

Flumatinib mesylate Related Antibodies

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1 Publications Citing Use of MCE Flumatinib mesylate

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Description

Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model[1][2].

IC50 & Target

PDGFRβ

307.6 nM (IC50)

c-Abl

1.2 nM (IC50)

In Vitro

Flumatinib mesylate (HH-GV-678) (0-1000 μM; 4, 7 and 10 days) blocks cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation in K562 leukemia cells[1].
Flumatinib mesylate (HH-GV-678) (0-10 μM; 72 hours) remarkably decreases the number of cells in chronic myelogenous leukemia cell lines[1].

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

Flumatinib mesylate Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Chronic myelogenous leukemia cell line
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: The proliferation inhibitory activity was 32-to 58-fold more potent than that of imatinib and 2-to 5-fold more potent than that of nilotinib.

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 0, 1, 3, 10, 30, 100, 300 and 1000 μM
Incubation Time: 4, 7 and 10 days
Result: Suppressed cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation.
In Vivo

Flumatinib mesylate (HH-GV-678) (18-75 mg/kg; p.o.; Twice daily, for 14 days.) inhibits tumor growth in nude mice[1].

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

Animal Model: Nude mice (subcutaneously injecting K562 cells)[1]
Dosage: 18.75, 37.5, 75 mg/kg
Administration: Oral administration; Twice daily, for 14 days.
Result: Inhibited the growth of K562 xenografts in a dose-dependent manner and induced regression in all tumors at a daily dose of 75 mg/kg for nine days.
Clinical Trial
Molecular Weight

658.69

Formula

C30H33F3N8O4S
CAS No.
Appearance

Solid

Color

Light brown to yellow

SMILES

O=C(NC1=CC(NC2=NC=CC(C3=CC=CN=C3)=N2)=C(C)N=C1)C4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4.CS(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (75.91 mM; Need ultrasonic)

DMSO : 50 mg/mL (75.91 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 1.5182 mL 7.5908 mL 15.1816 mL
5 mM 0.3036 mL 1.5182 mL 3.0363 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

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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: ≥ 2.08 mg/mL (3.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (75.91 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.87%

SDS (393 KB)

COA (249 KB) LCMS (265 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 1.5182 mL 7.5908 mL 15.1816 mL 37.9541 mL
5 mM 0.3036 mL 1.5182 mL 3.0363 mL 7.5908 mL
10 mM 0.1518 mL 0.7591 mL 1.5182 mL 3.7954 mL
15 mM 0.1012 mL 0.5061 mL 1.0121 mL 2.5303 mL
20 mM 0.0759 mL 0.3795 mL 0.7591 mL 1.8977 mL
25 mM 0.0607 mL 0.3036 mL 0.6073 mL 1.5182 mL
30 mM 0.0506 mL 0.2530 mL 0.5061 mL 1.2651 mL
40 mM 0.0380 mL 0.1898 mL 0.3795 mL 0.9489 mL
50 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7591 mL
60 mM 0.0253 mL 0.1265 mL 0.2530 mL 0.6326 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Flumatinib mesylate 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:

Flumatinib895519-91-2HHGV678HHGV 678HHGV-678Bcr-Ablc-KitPDGFRSCFRCD117Platelet-derived growth factor receptorc-AblPDGFRβInhibitorinhibitorinhibit

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