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Chemical Structure : PF-114
CAS No.: 1416241-23-0
Catalog No.: PC-20215Not For Human Use, Lab Use Only.
Vamotinib (PF-114) is a potent, selective and orally available inhibitor of native (IC50=0.49 nM) and mutated BCR/ABL (IC50=0.7-4 nM, ABL (T315I) IC50=0.78 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $278 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | $898 | In stock | |
| 100 mg | $1380 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Vamotinib (PF-114) is a potent, selective and orally available inhibitor of native (IC50=0.49 nM) and mutated BCR/ABL (IC50=0.7-4 nM, ABL (T315I) IC50=0.78 nM).
PF-114 potently inhibits ABL2, DDR1, DDR2, FMS, FRK, LCK, LYN and PDGFR kinases, but did not inhibit c-SRC, CSK, or c-KIT.
PF-114 is a potent TKI with a more restricted selectivity profile as compared to ponatinib or dasatinib.
PF-114 inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I and abolishes factor-independent growth of Ba/F3 cells mediated by BCR/ABL and its resistance mutants.
PF-114 potently inhibits Ph+ patient derived cell lines, abolishes tumor growth in a K562 nude-mouse xenograft model.
PF-114 suppresses growth of Ph+ PD-LTC with non mutational resistance as well as T315I mutation.
PF-114 prolongs the survival of mice with both BCR/ABL- and BCR/ABL-T315I-driven CMLlike disease.
| M.Wt | 532.57 | |
| Formula | C29H27F3N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-Methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1,2,4-triazolo[4,3-a]pyridin-3-yl)ethynyl]benzamide |
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1. A A Mian, et al. Leukemia. 2015 May;29(5):1104-14.
2. Ivanova ES, et al. Int J Oncol. 2019 Jul;55(1):289-297.
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