GDC-0973 (Cobimetinib)

Catalog No. A11441

GDC-0973 (Cobimetinib,RG7420)是一种有效且高度选择性的MEK1抑制剂，IC50为4.2 nM，对MEK1的选择性选择性是对MEK2的100倍以上，并且当针对一组超过100个丝氨酸的抑制剂进行测试时，没有显示出明显的抑制作用。

Product Citations

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

Technical details

Catalog Num	A11441
M. Wt	530.1
Formula	C21H21F3IN3O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	934660-93-2
Synonyms	XL518, XL 518, XL-518, RG7420
SMILES	C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O

Biological Activity

Targets

MEK1
4.2 nM

Solubility *

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.

Preparing Stock Solutions

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.