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CEP-40783

Cat. No. M8928
CEP-40783 Structure
Synonym:

RXDX-106

Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 250 In stock
25mg USD 500 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CEP-40783 (RXDX-106) is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively. CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. In 3/5 (60%) of the tumor models, CEP-40783 shows in vivo efficacy, including tumor regressions, significantly superior to that achieved with an optimal regimen of paclitaxel. In 4/4 (100%) of the erlotinib-insensitive tumor models, CEP-40783 demonstrates significant efficacy (66 to 118% TGI) compared to the control group at the 30 mg/kg dose.

Protocol
Cell Experiment
Cell lines 3T3 cells
Preparation method 3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or CEP-40783 for 30 minutes, and receptor phosphorylation is monitored.
Concentrations 0.25, 1, 2.5, 10, 25, 100, 250 nM
Incubation time 30 min
Animal Experiment
Animal models SCID Beige mice
Formulation
Dosages 30 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 588.56
Formula C31H26F2N4O6
CAS Number 1437321-24-8
Purity >98%
Solubility DMSO 8 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CEP-40783, RXDX-106 supplier, c-Met, inhibitors

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