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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Bcr-Abl-PF-114
PF-114

Chemical Structure : PF-114

CAS No.: 1416241-23-0

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PF-114 (Vamotinib, PF114)

货号: 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).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 532.57
分子式 C29H27F3N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

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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