rac-CCT 250863

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Cat.No. 4546 - rac-CCT 250863 | C24H25F3N4O2S | CAS No. 1364269-06-6
Description: Potent Nek2 inhibitor
Chemical Name: 4-[2-Amino-5-[4-[(dimethylamino)methyl]-2-thienyl]-3-pyridinyl]-2-[[(2Z)-4,4,4-trifluoro-1-methyl-2-buten-1-yl]oxy]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent Nek2 inhibitor (IC50 = 73 nM). Exhibits selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A.

Technical Data

M. Wt 490.54
Formula C24H25F3N4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1364269-06-6
PubChem ID 57386035
InChI Key LLEOOSLUHRQCHZ-SREVYHEPSA-N
Smiles CN(C)CC1=CSC(C2=CN=C(N)C(C3=CC(OC(/C=C\C(F)(F)F)C)=C(C(N)=O)C=C3)=C2)=C1

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 49.05 100
DMSO 49.05 100
ethanol 9.81 20

Preparing Stock Solutions

The following data is based on the product molecular weight 490.54. 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 2.04 mL 10.19 mL 20.39 mL
5 mM 0.41 mL 2.04 mL 4.08 mL
10 mM 0.2 mL 1.02 mL 2.04 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Innocenti et al (2012) Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. J.Med.Chem. 55 3228 PMID: 2404346


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View all Nek2 Kinase Inhibitors

Keywords: rac-CCT250863 potent NEK2 inhibitors inhibits selective never-in-mitosis-gene-a-related kinases Nek2 Kinase

Citations for rac-CCT 250863

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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
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Pathways for rac-CCT 250863

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