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Cobimetinib hemifumarate is a potent and selective MEK1 inhibitor with an IC50 value of 4.2 nM for MEK1.

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $37 | - | In Stock | |
| 5 mg | Preferential | - | In Stock |
| Description | Cobimetinib hemifumarate is a potent and selective MEK1 inhibitor with an IC50 value of 4.2 nM for MEK1. |
| Targets&IC50 | MEK1:4.2 nM |
| In vitro | The EC50 values of Cobimetinib hemifumarate(GDC-0973) on 888MEL and A2058 cells were 0.2 μM and 10 μM, respectively. Melanoma cells were treated with MEK and PI3K inhibitors with EC50 concentration for 24 hours (888mel: 0.05μ m GDC-0973, 2.5 μM GDC-0941;; A2058:2.5 μM GDC-0973、2.5 μM GDC-0941)[1]。 Mitochondrial oxidative phosphorylation can limit cell death induced by Cobimetinib hemifumarate(100 nM) in melanoma with constitutive MAPK activation in A375 cells [4]. |
| Synonyms | XL-518 hemifumarate, XL518 hemifumarate, XL 518 hemifumarate, GDC-0973 hemifumarate, GDC0973 hemifumarate, GDC 0973 hemifumarate |
| Molecular Weight | 1178.71 |
| Formula | C46H46F6I2N6O8 |
| Cas No. | 1369665-02-0 |
| Smiles | OC(=O)\C=C\C(O)=O.OC1(CN(C1)C(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F)[C@@H]1CCCCN1.OC1(CN(C1)C(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F)[C@@H]1CCCCN1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 50.00 mg/mL (42.42 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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