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GDC-0623 - 97%, high purity , CAS No.1168091-68-6, Inhibitor of mitogen-activated protein kinase kinase 1

Moligand™
≥97%

CAS#: 1168091-68-6
Formula: C₁₆H₁₄FIN₄O₃
Molecular Weight: 456.21
PubChem CID: 42642654

Item Number

G413780

Grouped product items
SKU	Size	Availability	Price
G413780-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$147.90
G413780-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$666.90
G413780-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$969.90

MEK1 Selective Inhibitors

View related series

mitogen-activated protein kinase kinase 1 Inhibitor

Basic Description

Synonyms	GDC-0623\|1168091-68-6\|GDC 0623\|RG 7421\|GDC0623\|5-((2-FLUORO-4-IODOPHENYL)AMINO)-N-(2-HYDROXYETHOXY)IMIDAZO[1,5-A]PYRIDINE-6-CARBOXAMIDE\|G-868\|5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide\|HW67545I4Q\|RG-7421\|Imidazo[1,5
Specifications & Purity	Moligand™, ≥97%
Biochemical and Physiological Mechanisms	GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with K_i of 0.13 nM. Phase 1.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of mitogen-activated protein kinase kinase 1
Product Description	Information GDC-0623 (G-868) is a potent and ATP-uncompetitiveMEK1inhibitor withKiof 0.13 nM. Phase 1. Targets MEK1 0.13 nM In vitro In a panel of mutant cancer cell lines, GDC-0623 inhibits cellular proliferation with EC50 of 4 nM, 53 nM, 11 nM, 18 nM and 94 nM for A375 (BRAFV600E), HCT116 (KRASG13D), COLO 205 (V600E), HT-29 (V600E), and HCT116 (G13D) cells, respectively. In isogenic KRAS HCT116 and mutant KRAS SW620 colon cells, GDC-0623 upregulates BIM via its loss of phosphorylation at Ser69. GDC-0623 plus ABT-263 induces a synergistic cell apoptosis. 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. Cell Research(from reference) Cell lines：A375 (BRAFV600E), HCT116 (KRASG13D), COLO 205 (V600E), HT-29 (V600E), and HCT116 (G13D) cells Incubation Time：24 hours

ALogP

2.284

HBD Count

Rotatable Bond

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Discover Target: CYP2D6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

Discover Target: CYP2C19

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Discover Target: CYP2C9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 1 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 1 Activities

Discover Target: MAP2K1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide
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)
InChi Key	RFWVETIZUQEJEF-UHFFFAOYSA-N
Canonical SMILES	C1=CC(=C(C=C1I)F)NC2=C(C=CC3=CN=CN32)C(=O)NOCCO
Isomeric SMILES	C1=CC(=C(C=C1I)F)NC2=C(C=CC3=CN=CN32)C(=O)NOCCO
Alternate CAS	1168091-68-6
PubChem CID	42642654
MeSH Entry Terms	GDC-0623
Molecular Weight	456.21

Certificates

Certificate of Analysis(COA)

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3 results found

Lot Number	Certificate Type	Date	Item
E2322319	Certificate of Analysis	Apr 10, 2023	G413780
E2322375	Certificate of Analysis	Apr 10, 2023	G413780
E2322414	Certificate of Analysis	Apr 10, 2023	G413780

Solubility

Solubility (25°C) In vitro DMSO: 91 mg/mL warmed with 50ºC Water: bath (199.46 mM); Ethanol: 6 mg/mL warmed with 50ºC Water: bath (13.15 mM); Water: ˂1 mg/mL

DMSO(mg / mL) Max Solubility

DMSO(mM) Max Solubility

199.4695425

Water(mg / mL) Max Solubility

＜1

References

1. Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C et al.. (2013) Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.. Nature, 501 (7466): (232-6). [PMID:23934108]
2. Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P et al.. (2014) Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.. Bioorg Med Chem Lett, 24 (19): (4714-4723). [PMID:25193232]

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