GDC-0623

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H14FIN4O3
Molecular Weight	456.2102
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OCCONC(=O)C1=C(NC2=CC=C(I)C=C2F)N3C=NC=C3C=C1

InChI

InChIKey=RFWVETIZUQEJEF-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Molecular Formula	C16H14FIN4O3
Molecular Weight	456.2102
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23934108
Curator's Comment: The description was created based on several sources, including https://clinicaltrials.gov/ct2/show/record/NCT01106599

DC-0623 is an orally active, selective and ATP-uncompetitive MEK inhibitor with potential antineoplastic activity. 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. In a panel of mutant cancer cell lines, GDC-0623 inhibits cellular proliferation with EC50 values in the low nanomolar range. In vivo, GDC-0623 (40 mg/kg, p.o.) causes potent tumor growth inhibition (TGI) in mouse MiaPaCa-2 (120%), A375 (102%) and HCT116 (115%) xenografts. GDC-0623 had been in phase I clinical trials by Genentech, Inc. for the treatment of Advanced or Metastatic Solid Tumors. However, the clinical development of GDC-0623 was discontinued.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dual specificity mitogen-activated protein kinase kinase 1 20 Target ID: CHEMBL3587 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23934108	Inhibitor 8504		0.13 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Locally advanced or metastatic solid tumors 1 Sources: https://clinicaltrials.gov/ct2/show/record/NCT01106599	Primary		Phase I 438	Unknown Approved Use Unknown

T_1/2

Value	Dose	Co-administered	Analyte	Population
5 h EXPERIMENT https://mct.aacrjournals.org/content/12/11_Supplement/B75	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:		GDC-0623 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY34536	https://www.001chemical.com/chem/search?q=DY34536
1PlusChem LLC	1P008TX1	https://www.1pchem.com/search?query=1P008TX1
AChemBlock	L13965	http://www.achemblock.com/catalogsearch/result/?q=L13965
AOBIOUS INC	AOB87143	http://aobious.com/aobious/search?search_query=AOB87143
ApexBio Technology	B1135	https://www.apexbt.com/catalogsearch/result/?q=B1135
AstaTech	42236	http://astatechinc.com/CPSResult.php?CRNO=42236
BLD Pharm	BD333077	http://www.bldpharm.com/search/Search.html?keyword=BD333077
Cayman Chemical	19479	http://www.caymanchem.com/app/template/Product.vm/catalog/19479
Chem Scene	CS-2281	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-2281
ChemShuttle	140499	https://www.chemshuttle.com/catalogsearch/result/?q=140499
Debye Scientific	DA-33609	https://www.debyesci.com/index.php?id=product&ext[cno]=DA-33609
eMolecules	50282669	https://orderbb.emolecules.com/search/#?query=50282669
eNovation Chemicals	D501909	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D501909&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A2060	http://www.excenen.com/searchresultlist.php?id=EX-A2060
KeyOrganics	AS-55986	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-55986
mcule	MCULE-7096700372	https://mcule.com/MCULE-7096700372/
MedChem Express	HY-15610	https://www.medchemexpress.com/search.html?q=HY-15610&ft=&fa=&fp=
Molcore	MC34536	http://www.molcore.com/CatMC34536.html
Molnova	M17163	https://www.molnova.com/en/serch-list.html?keywords=M17163
MolPort	MolPort-039-193-834	https://www.molport.com/shop/molecule-link/MolPort-039-193-834
MuseChem	I000603	https://www.musechem.com/product/I000603.html
Selleck Chemicals	S7553	http://www.selleckchem.com/search.html?searchDTO.searchParam=S7553
ShangHai Biochempartner	BCP28689	http://www.biochempartner.com/search_BCP28689
TargetMol	T6843	https://www.targetmol.com/search?keyword=T6843

PubMed

Title	Date	PubMed
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.	2013-09-12	23934108

Patents

Sample Use Guides

In Vivo Use Guide

40 mg/kg, p.o. (mouse)

Route of Administration: Oral

In Vitro Use Guide

HCT116 and A375 cell lines were used for activity evaluation. Cells were treated with DC-0623 (1nM-1mkM) for 24-hour. Viability following compound treatment was assessed via ATP content using the CellTiter-Glo Luminescent Assay (Promega, Madison, WI).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:58:19 GMT 2025` Edited by `admin` on `Mon Mar 31 20:58:19 GMT 2025`
Record UNII	HW67545I4Q
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

GDC 0623 [WHO-DD]

Preferred Name

English

GDC-0623

Common Name

English

Code System Code Type Description

PUBCHEM

42642654