Flumatinib (HH-GV678) | BCR-ABL inhibitor

Chemical Structure : Flumbatinib

CAS No.: 895519-90-1

Flumbatinib (HH-GV678, HH-GV-678)

Catalog No.: PC-38393Not For Human Use, Lab Use Only.

Flumatinib (HH-GV678) is a potent BCR-ABL/PDGFR/KIT inhibitor, potently inhibits ABL, PDGFR-β and KIT kinase with IC50 of 1.2, 307.6 and 665.5 nM, respectively.

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Biological Activity

Flumatinib (HH-GV678) is a potent BCR-ABL/PDGFR/KIT inhibitor, potently inhibits ABL, PDGFR-β and KIT kinase with IC50 of 1.2, 307.6 and 665.5 nM, respectively.
Flumatinib (HH-GV678) displays only weak inhibition of VEGFR2/3, SRC, FLT3, RET, EGFR, and HER2.
Flumatinib (HH-GV678) is a more potent inhibitor of BCR-ABL1 tyrosine kinase than imatinib (IC50=100.9 nM).
Flumatinib (HH-GV678) exhibited a selective inhibition pattern toward imatinib-resistant KIT mutants associated with GISTs, effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P).
Flumatinib (HH-GV678) had superior efficacy compared with imatinib or sunitinib against 32D cells with the secondary mutation Y823D.

Physicochemical Properties

M.Wt	562.601
Formula	C29H29F3N8O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(4-Methyl-piperazin-1-ylmethyl)-N-[6-methyl-5-(4-pyridin-3-yl-pyrimidin-2-ylamino)-pyridin-3-yl]-3-trifluoromethyl-benzamide

References

1. Luo H, et al. Leukemia. 2010 Oct;24(10):1807-9.

2. Kuang Y, et al. Cancer Chemother Pharmacol. 2020 Sep;86(3):339-346.

3. Zhang L, et al. Clin Cancer Res. 2021 Jan 1;27(1):70-77.

4. Zhao J, et al. Cancer Sci. 2014 Jan;105(1):117-25.

Flumbatinib (HH-GV678, HH-GV-678)

Biological Activity

Physicochemical Properties

References

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