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
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)
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 |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23934108Curator's Comment: The description was created based on several sources, including
https://clinicaltrials.gov/ct2/show/record/NCT01106599
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 |
---|---|---|---|
Target ID: CHEMBL3587 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23934108 |
0.13 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23934108
40 mg/kg, p.o. (mouse)
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23934108
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
Edited
Sat Dec 16 01:41:52 GMT 2023
by
admin
on
Sat Dec 16 01:41:52 GMT 2023
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Record UNII |
HW67545I4Q
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Record Status |
Validated (UNII)
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Record Version |
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