CEP-40783 (RXDX-106)

Catalog No.S8570 Batch:S857002

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Technical Data

Formula

C31H26F2N4O6
Molecular Weight 588.56 CAS No. 1437321-24-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (169.9 mM)
Ethanol 3 mg/mL (5.09 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description CEP-40783 (RXDX-106) 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)		 View More
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].
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 Assay:

[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 Study:

[2]
  • Animal Models

    SCID Beige mice

  • Dosages

    30 mg/kg

  • Administration

    p.o.

Selleck's CEP-40783 (RXDX-106) has been cited by 6 publications

Dissecting signaling regulators driving AXL-mediated bypass resistance and associated phenotypes by phosphosite perturbations [ bioRxiv, 2023, 2023.10.20.563266] PubMed: 37961516
Integrated Proteomics-Based Physical and Functional Mapping of AXL Kinase Signaling Pathways and Inhibitors Define Its Role in Cell Migration [ Mol Cancer Res, 2022, 20(4):542-555] PubMed: 35022314
Inhibition of Axl Promotes the Therapeutic Effect of Targeted Inhibition of the PI3K/Akt Pathway in NRAS Mutant Melanoma Cells [ J Oncol, 2022, 2022:2946929] PubMed: 35310910
Cell Type-specific Adaptive Signaling Responses to KRASG12C Inhibition [ Clin Cancer Res, 2021, 27(9):2533-2548] PubMed: 33619172
Attenuation of apoptotic cell detection triggers thymic regeneration after damage [ Cell Rep, 2021, 37(1):109789] PubMed: 34610317
Lysyl-tRNA synthetase-expressing colon spheroids induce M2 macrophage polarization to promote metastasis. [ J Clin Invest, 2018, 128(11):5034-5055] PubMed: 30188867

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.