CHMFL-FLT3-122

Name: CHMFL-FLT3-122
Brand: Tocris Bioscience
SKU: 5800

Catalog #: 5800 Datasheet / COA / SDS

Discontinued Product

5800 has been discontinued.

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CHMFL-FLT3-122 | CAS No. 1839150-56-9 | Flt-3 Inhibitors

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Description: Potent and selective FLT3 inhibitor

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

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Biological Activity

CHMFL-FLT3-122 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

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
Li et al.
J.Med.Chem., 2015;58:9625

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