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Cat.No. 5800 - CHMFL-FLT3-122 | C26H29N7O2 | CAS No. 1839150-56-9
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
Literature (2)

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
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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
1eq. HCl 47.16 100
DMSO 47.16 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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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