CHMFL-FLT3-122

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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
Datasheet
Citations
Literature

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
InChI Key IZNAFSDUTMZGSF-LJQANCHMSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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 solvent 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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Product Datasheets

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References

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 leu 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, FLT3, Tocris Bioscience

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for CHMFL-FLT3-122

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