CHMFL-FLT3-122

Cat. No. 5800

CHMFL-FLT3-122 C26H29N7O2 [1839150-56-9]

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Chemical Name: 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone

Biological Activity

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.

Technical Data

M.Wt:
471.55
Formula:
C26H29N7O2
Solubility:
Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
Storage:
Store at +4°C
CAS No:
1839150-56-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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 leukemia. J.Med.Chem. 58 9625. PMID: 26630553.

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Keywords: CHMFL-FLT3-122, supplier, Potent, selective, FLT, inhibitors, inhibits, AML, acute, myeloid, leukemia, cell, cycle, Tocris Bioscience, FLT3 Inhibitor products

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