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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
Biological Activity
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases.
Targets
| MEK1 | ||||
| 4.2 nM |
| In vitro (25°C) | DMSO | 88 mg/mL (165.62 mM) | |
| Water | Insoluble | ||
| Ethanol | Warmed: 41 mg/mL (77.17 mM) | ||
| In vivo | 5% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.86 mL | 94.32 mL | 188.64 mL |
| 0.5 mM | 3.77 mL | 18.86 mL | 37.73 mL |
| 1 mM | 1.89 mL | 9.43 mL | 18.86 mL |
| 5 mM | 0.38 mL | 1.89 mL | 3.77 mL |
*The above data is based on the productmolecular weight 530.1 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11441 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 934660-93-2 |
| Formula | C21H21F3IN3O2 |
| M. Wt | 530.1 |
| Purity | >98% |
| Synonyms | XL518, XL 518, XL-518, RG7420 |
| SMILES | C1CCN[[email protected]@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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