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GDC-0623

GDC-0623 Structure
GDC-0623
  • CAS No.1168091-68-6
  • Chemical Name:GDC-0623
  • 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)
  • color Light yellow to gray
  • FDA UNII HW67545I4Q
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338

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.
  • Uses GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
  • 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.
  • in vivo

    GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models[1].

  • target MEK1
  • IC 50 MEK1: 0.13 nM (Ki, +ATP)
  • 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.
GDC-0623 Preparation Products And Raw materials
Raw materials
Preparation Products
GDC-0623 Suppliers
Global(84)Suppliers
  • Supplier：
    Career Henan Chemica Co
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    InvivoChem
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    TargetMol Chemicals Inc.
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    Aladdin Scientific
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  • Supplier： NCE Biomedical Co.,Ltd.
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GDC-0623 Spectrum
1168091-68-6, GDC-0623Related Search:
  • 合成有机化合物配体
  • 抑制剂
  • 细胞生物学试剂
  • C16H14FIN4O3
  • 化合物GDC-0623,10 MM DMSO 溶液
  • 化合物GDC-0623
  • MEK1抑制剂
  • 5-((2-氟-4-碘苯基)氨基)-N-(2-羟基乙氧基)咪唑并[1,5-A]吡啶-6-甲酰胺
  • MEK1抑制剂(GDC-0623)
  • 1168091-68-6
  • GDC-0623, 10 mM in DMSO
  • Mitogen-activated protein kinase kinase,Apoptosis,inhibit,MEK,Inhibitor,MAP2K,MAPKK,MEK inhibitor1,GDC-0623,RG7421,GDC 0623,MEK inhibitor-1,RG-7421
  • GDC-0623 (G-868)
  • Imidazo[1,5-a]pyridine-6-carboxamide, 5-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-
  • CS-1791
  • 5-((2-FLUORO-4-IODOPHENYL)AMINO)-N-(2-HYDROXYETHOXY)IMIDAZO[1,5-A]PYRIDINE-6-CARBOXAMIDE
  • G-868
  • MEK inhibitor 1
  • GDC-0623
  • 5-(2-Fluoro-4-iodophenylamino)imidazo[1,5-a]pyridine-6-carboxylic acid N-(2-hydroxyethoxy)amide RG 7421 GDC-0623
  • 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

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