| Identification | Back Directory | [Name]
GDC-0623 | [CAS]
1168091-68-6 | [Synonyms]
G-868
RG 7421
CS-1791
GDC-0623
MEK inhibitor 1
5-((2-FLUORO-4-IODOPHENYL)AMINO)-N-(2-HYDROXYETHOXY)IMIDAZO[1,5-A]PYRIDINE-6-CARBOXAMIDE
Imidazo[1,5-a]pyridine-6-carboxamide, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-
5-(2-Fluoro-4-iodophenylamino)imidazo[1,5-a]pyridine-6-carboxylic acid N-(2-hydroxyethoxy)amide
GDC-0623 (5-((2-Fluoro-4-Iodophenyl)amino)-N-(2-Hydroxyethoxy)imidazo[1,5-a]pyridine-6-Carboxamide)
5-(2-Fluoro-4-iodophenylamino)imidazo[1,5-a]pyridine-6-carboxylic acid N-(2-hydroxyethoxy)amide RG 7421 GDC-0623 | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C16H14FIN4O3 | [MDL Number]
MFCD25976760 | [MOL File]
1168091-68-6.mol | [Molecular Weight]
456.21 |
| Chemical Properties | Back Directory | [density ]
1.81±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥16.85 mg/mL in DMSO; ≥2.69 mg/mL in EtOH with ultrasonic | [form ]
solid | [pka]
14.17±0.10(Predicted) | [color ]
Light yellow to gray |
| Hazard Information | Back Directory | [Description]
GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP).1 It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively.1 GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.2 | [Definition]
ChEBI: GDC-0623 is a member of the class of imidazopyridines that is imidazo[1,5-a]pyridine substituted by (2-fluoro-4-iodophenyl)amino and (2-hydroxyethoxy)aminoacyl groups at positions 5 and 6. It is a potent ATP non-competitive inhibitor of MEK1 (Ki = 0.13nM) and also has efficacy against both mutant BRAF and mutant KRAS. It is in clinical development for treatment of patients with locally advanced or metastatic solid tumors. It has a role as an EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a substituted aniline, a member of monofluorobenzenes, an organoiodine compound, an imidazopyridine, a secondary amino compound, a hydroxamic acid ester and a primary alcohol. | [target]
MEK1 | [References]
[1] hatzivassiliou g, haling j r, chen h, et al. mechanism of mek inhibition determines efficacy in mutant kras-versus braf-driven cancers. nature, 2013, 501(7466): 232-236. |
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