RXDX-106 (CEP-40783)

Catalog No.S8570

For research use only.

RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.

RXDX-106 (CEP-40783) Chemical Structure

CAS No. 1437321-24-8

Selleck's RXDX-106 (CEP-40783) has been cited by 4 Publications

Purity & Quality Control

Choose Selective Axl Inhibitors

Biological Activity

Description RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively.
Targets
Axl [2]
(Cell-free assay)
c-Met [2]
(Cell-free assay)
Tyro3 [2]
(Cell-free assay)
MER [2]
(Cell-free assay)
Tyro3 [2]
(Cell-free assay)
Click to View More Targets
7 nM 12 nM 19 nM 29 nM 29 nM
In vitro

RXDX-106 inhibits TAM and c-MET phosphorylation in vitro. This inhibition of TAM and c-MET activation in vitro is accompanied by a decrease in downstream MAPK and PI3K signaling and cell viability[1]. It completely inhibits cellular proliferation and viability at sub-nanomolar concentrations in TAM-expressing cells[2].

Assay
Methods Test Index PMID
Western blot p-MerTK / MerTK / p-ERK / ERK / p-AKT / AKT 29285287
In vivo RXDX-106 could inhibit tumors harboring activating TAM gene fusions and affect the TAM-expressing tumor microenvironment to result in a global anti-cancer environment[1].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: 3T3 cells
  • Concentrations: 0.25, 1, 2.5, 10, 25, 100, 250 nM
  • Incubation Time: 30 min
  • Method:

    3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or RXDX-106 for 30 minutes, and receptor phosphorylation is monitored. 

Animal Research:

[2]

  • Animal Models: SCID Beige mice
  • Dosages: 30 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 588.56
Formula

C31H26F2N4O6

CAS No. 1437321-24-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N1C=C(C(=O)N(C1=O)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C5C=C(C(=CC5=NC=C4)OC)OC)F

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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