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Chemical Structure : Flumbatinib
CAS No.: 895519-90-1
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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|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 562.601 | |
| Formula | C29H29F3N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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