Discontinued Product

CHMFL-FLT3-122 (Cat. No. 5800) has been withdrawn from sale for commercial reasons.
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

Biological Activity for CHMFL-FLT3-122

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 for CHMFL-FLT3-122

M. Wt 471.55
Formula C26H29N7O2
Storage Store at +4°C
CAS Number 1839150-56-9
PubChem ID 121513893
Smiles NC1=C2C(N([C@@H]3CCCN(C(CN(C)C)=O)C3)N=C2C4=CC=C(OC5=CC=CC=C5)C=C4)=NC=N1

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.

Product Datasheets for CHMFL-FLT3-122

References for CHMFL-FLT3-122

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

Citations for CHMFL-FLT3-122

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Currently there are no citations for CHMFL-FLT3-122.

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