GDC-0623
- Product Name
- GDC-0623
- CAS No.
- 1168091-68-6
- Chemical Name
- GDC-0623
- Synonyms
- G-868;CS-1791;RG 7421;GDC-0623;MEK inhibitor 1;GDC-0623 (G-868);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)
- CBNumber
- CB72655407
- Molecular Formula
- C16H14FIN4O3
- Formula Weight
- 456.21
- MOL File
- 1168091-68-6.mol
GDC-0623 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 19479
- Product name
- GDC-0623
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $41
- Updated
- 2024/03/01
- Product number
- 19479
- Product name
- GDC-0623
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 19479
- Product name
- GDC-0623
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $201
- Updated
- 2024/03/01
- Product number
- 19479
- Product name
- GDC-0623
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $302
- Updated
- 2024/03/01
- Product number
- 474102
- Product name
- GDC 0623
- Packaging
- 100mg
- Price
- $2272
- Updated
- 2021/12/16
GDC-0623 Chemical Properties,Usage,Production
Description
GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP). 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. 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.
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.