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Potent and selective FLT3 inhibitor (IC50 = 40 nM). Exhibits >10-fold and 170-fold selectivity for FLT3 over BTK kinase and c-KIT kinase, respectively in vitro. Induces apoptosis by arresting cell cycle in G0/G1 phase in vitro. Suppresses tumor growth in an AML xenograft model. Modestly orally bioavailable.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 471.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.12 mL||10.6 mL||21.21 mL|
|5 mM||0.42 mL||2.12 mL||4.24 mL|
|10 mM||0.21 mL||1.06 mL||2.12 mL|
|50 mM||0.04 mL||0.21 mL||0.42 mL|
References are publications that support the biological activity of the product.
Li et al (2015) Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a potent and orally available FLT3 kinase inhibitor for FLT3-ITD positive acute myeloid leu J.Med.Chem. 58 9625 PMID: 26630553
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Keywords: CHMFL-FLT3-122, CHMFL-FLT3-122 supplier, Potent, selective, FLT, inhibitors, inhibits, AML, acute, myeloid, leukemia, cell, cycle, FLT3, Cell, Cycle, Inhibitors, Apoptosis, Inducers, 5800, Tocris Bioscience
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