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GDC-0973

Cat. No. M3626
GDC-0973 Structure
Synonym:

XL518, RG7420, Cobimetinib

Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 200 In stock
50mg USD 590 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GDC-0973 is a potent and selective mitogen-activated protein (MAP)/extracellular signal-regulated kinase (ERK) kinase (MEK) inhibitor. GDC-0973 is known as mitogen activated protein kinase kinase (MAPKK). GDC-0973 is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors.

Product Citations
Customer Product Validations & Biological Datas
Source Int J Mol Sci (2018). Figure 5. GDC-0973 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 0.5 μM
Incubation Time 16 h
Results In contrast, the condition containing Cobi alone showed significantly reduced lytic capacity of the CAR-T cells, and this lytic capacity was even further reduced in the additional presence of Vem.
Source Int J Mol Sci (2018). Figure 4. GDC-0973 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 0.5 μM
Incubation Time 16 h
Results The presence of Vem alone, Tram alone,Cobi alone, Vem + Cobi, and Dabra + Tram, but not of Dabra alone seemed to reduce these quantities to approximately 50%.
Source Int J Mol Sci (2018). Figure 3. GDC-0973 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 0.5 μM
Incubation Time 16 h
Results Both MEKi significantly reduced IFN -secretion but the effect of Cobi alone was significantly stronger
Source Int J Mol Sci (2018). Figure 2. GDC-0973 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 0.5 μM
Incubation Time 16 h
Results Incubation with the MEK inhibitors Tram and Cobi alone, but also the combination of Vem + Cobi reduced the CD25 upregulation approximately to 50%.
Protocol
Cell Experiment
Cell lines Human 888MEL (BRAFV600E) mutant melanoma cell lines
Preparation method Plating cells in quadruplicate at a density of 3,000 per well in 384-well plates in normal growth medium and allowing to adhere overnight. Adding compounds in 10 concentrations based on a 3-fold dilution series. Using the CellTiter-Glo Luminescent Cell Viability Assay to measure cell viability 72 h later.
Concentrations ~10 μM
Incubation time 4 days
Animal Experiment
Animal models Human A375.X1 BRAFV600E mutant melanoma xenograft
Formulation
Dosages 5 mg/kg/day
Administration orally daily (QD) for 2 1 consecutive days
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 531.31
Formula C21H21F3IN3O2
CAS Number 934660-93-2
Purity >98%
Solubility DMSO
Storage at -20°C
References

Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.
Wong H, et al. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. PMID: 22496205.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GDC-0973, XL518, RG7420, Cobimetinib supplier, MEK, inhibitors

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