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

Flumatinib (Synonyms: HHGV678)

Cat. No.: HY-13904 Purity: 99.94%
Handling Instructions

Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.

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

Flumatinib Chemical Structure

Flumatinib Chemical Structure

CAS No. : 895519-90-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 104 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 228 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].

IC50 & Target

IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit)[1].

In Vitro

Flumatinib (HH-GV-678) can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2 [1]. Flumatinib (HHGV678) effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) [2].

Clinical Trial
Molecular Weight

562.59

Formula

C₂₉H₂₉F₃N₈O

CAS No.

895519-90-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (177.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7775 mL 8.8875 mL 17.7749 mL
5 mM 0.3555 mL 1.7775 mL 3.5550 mL
10 mM 0.1777 mL 0.8887 mL 1.7775 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

FlumatinibHHGV678HHGV 678HHGV-678Bcr-Ablc-KitPDGFRSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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Product Name:
Flumatinib
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HY-13904
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