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GDC-0623

CAT: 0013-GTR19161401-02Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161401-02Size:500 mg
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Description
GDC-0623, also known as G-868, is an orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) . (In Vitro) :GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF (V600E) . GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases. (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.
CAS Number
1168091-68-6
Product Name Alternative
GDC0623 | GDC-0632 | GDC 0632 | G868 | G 868 | G-868
Purity
>98% (HPLC)
Solubility
DMSO : ≥ 30 mg/mL. 65.76 mM
Smiles
OCCONC (=O) C1=C (NC2=C (F) C=C (I) C=C2) N2C=NC=C2C=C1
Molecular Formula
C16H14FIN4O3
Molecular Weight
456.21
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
5- ((2-fluoro-4-iodophenyl) amino) -N- (2-hydroxyethoxy) imidazo[1,5-a]pyridine-6-carboxamide

Chemical Information

Gdc-0623

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 antineoplastic agent, an apoptosis inducer and an EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor. It is a primary alcohol, an organoiodine compound, an imidazopyridine, a substituted aniline, a secondary amino compound, a hydroxamic acid ester and a member of monofluorobenzenes.

CAS Number1168091-68-6
PubChem CID42642654
IUPAC Name5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide
Molecular FormulaC16H14FIN4O3
Molecular Weight456.21
XLogP3.7
Topological Polar Surface Area87.9
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count6
Rotatable Bond Count6
Heavy Atom Count25
Formal Charge0
Complexity461
SMILES
C1=CC(=C(C=C1I)F)NC2=C(C=CC3=CN=CN32)C(=O)NOCCO
InChI
InChI=1S/C16H14FIN4O3/c17-13-7-10(18)1-4-14(13)20-15-12(16(24)21-25-6-5-23)3-2-11-8-19-9-22(11)15/h1-4,7-9,20,23H,5-6H2,(H,21,24)
InChIKey
RFWVETIZUQEJEF-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Gdc-0623
CAS: 1168091-68-6
CID: 42642654
Formula: C16H14FIN4O3
MW: 456.21
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight456.21
XLogP33.7
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count6
Rotatable Bond Count6
Exact Mass456.00947
Monoisotopic Mass456.00947
Topological Polar Surface Area87.9 Ų
Heavy Atom Count25
Formal Charge0
Complexity461
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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