All AbMole products are for research use only, cannot be used for human consumption.
Cobimetinib (GDC-0973, RG7420) is an effective, selective, oral MEK1 inhibitor with an IC50 of 4.2 nM against MEK1. In addition, Cobimetinib is an inhibitor of Akt.
Int J Mol Sci. 2018 Jan 18;19(1) pii: E289.
BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy
Cobimetinib purchased from AbMole
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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. |
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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%. |
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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 |
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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%. |
| 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 |
| Molecular Weight | 531.31 |
| Formula | C21H21F3IN3O2 |
| CAS Number | 934660-93-2 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MEK Products |
|---|
| AS703026
Pimasertib (AS-703026) is a novel selective MEK1/2 inhibitor, and induces pleiotropic anti-myeloma activity in vitro and in vivo. |
| AZD6244
AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. |
| AZD8330
AZD8330 (ARRY-424704) is a novel, selective, highly efficacious, uncompetitive MEK inhibitor with an IC50 of 7 nM. |
| CI-1040
CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. |
| ARRY-162 (Binimetinib)
ARRY-162 (MEK-162; Binimetinib) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively. |
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