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 a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit 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
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Based on 1 publication(s) in Google Scholar

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Description

Flumatinib (HHGV678) is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.

IC50 & Target

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

In Vitro

HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib (HHGV678) can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib (HHGV678) 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].

In Vivo

The purpose of this study was to identify the metabolites of flumatinib in CML patients, with the aim of determining the main metabolic pathways of Flumatinib (HHGV678) in humans after oral administration. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry revealed 34 metabolites; 7 primary metabolites were confirmed by comparison with synthetic reference standards. The results show that the parent drug Flumatinib (HHGV678) was the main form recovered in human plasma, urine, and feces. The main metabolites of Flumatinib (HHGV678) in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis [3].

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 : ≥ 32 mg/mL (56.88 mM)

*"≥" means soluble, but saturation unknown.

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.
References
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Flumatinib
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HY-13904
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