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Flumatinib (HHGV678) (Synonyms: HH-GV-678)

Catalog No.GC32867

플루마티닙(HHGV678)(HHGV678)은 Bcr-Abl의 경구용 선택적 억제제입니다. 플루마티닙(HHGV678)은 c-Abl, PDGFRβ을 억제합니다. IC50이 각각 1.2nM, 307.6nM 및 665.5nM인 c-Kit.

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Flumatinib (HHGV678) Chemical Structure

Cas No.: 895519-90-1

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$79.00
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5mg
US$65.00
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10mg
US$82.00
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50mg
US$175.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

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].

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].

[1]. Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9. [2]. Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10. [3]. Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40.

Chemical Properties

Cas No. 895519-90-1 SDF
Synonyms HH-GV-678
Canonical 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
Formula C29H29F3N8O M.Wt 562.59
Solubility DMSO : ≥ 32 mg/mL (56.88 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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 3.555 mL
10 mM 0.1777 mL 0.8887 mL 1.7775 mL
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리뷰

Review for Flumatinib (HHGV678)

Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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