Home
Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassay Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
Polymers & Contract Manufacturing
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Products
Small Molecule Inhibitors and Antagonist
Bioactive Compounds and Agonist
Primary Antibodies
Catalog Peptides
Amino Acids Derivatives
Reagents
Fluorescent dyes
Intermediates
PCR
Proteasomes and Enzymes
Enzyme substrate
Nucleotides
Promotions
Customer Support
About Us
Site Map
Contact Us
Small Molecule Inhibitors and Antagonist
Anti-virus
Cell Cycle
DMPK/Tox
Endocrinology
Epigenetics
GPCR/G-protein
Mitogen-activated Protein Kinases (MAPK)
PI3K/Akt/mTOR
Proteases/Proteasome
Protein Tyrosine Kinases (PTK)
Stem Cells
TGF-Beta/Smad
Transporter
Others
Cat. No. Name Size Price Add Cart
KI3014GDC-0973 (XL-518)5 mg$676
GDC-0973 (XL-518)10 mg$1196
GDC-0973 (XL-518)20 mg$1716
GDC-0973 (XL-518)50 mg$2496
GDC-0973 (XL-518)100 mg$3640
GDC-0973 (XL-518)200 mg$4940
GDC-0973 (XL-518)1 g$14300

Chemical Characteristic

Product NameGDC-0973 (XL-518)
SynonymsGDC 0973,XL 518
CAS No.934660-93-2
Molecular Weight 531.31
FormulaC21H21F3IN3O2
Chemical Name[3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone
SmilesC(=O)(N1CC(C1)(C1NCCCC1)O)c1c(c(c(cc1)F)F)Nc1c(cc(cc1)I)F
Chemical Structure

Biological activities

GDC-0973 is a potent, selective, orally active inhibitor of MEK1/2. GDC-0973 inhibits MEK1 with an IC50 of 4.2 nM. In Colo205 cells (BRAF V600E mutant), GDC-0973 inhibits ERK1/2 phosphorylation and proliferation with IC50s of 1.8 and 8 nM, respectively.[1]In vitro, GDC-0973 exerts antiproliferative effects in multiple tumor cell lines harboring KRAS or BRAF mutations.[2] GDC-0973 causes potent inhibition of pERK in 2 models of B-RAF mutant melanoma, WM-266-4 and A375 xenograft mice.[3]

Protocols

In vivo, GDC-0973 is dissolved in 0.9% normal saline. [1]

References

[1] Choo EF, et al. Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions. Drug Metab Dispos. 2012, 40(5): 919-927.
[2] Fr?min C, et al. From basic research to clinical development of MEK1/2 inhibitors for cancer therapy. J Hematol Oncol. 2010, 3: 8.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
About
KareBayTM Biochem
Sitemap
Blog
Custom Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Biochemical Products
Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR
Contact Us
KareBayTM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852
Telephone
: 732-823-1545

Fax
: 732-823-1349
product@karebaybio.com
service@karebaybio.com
support@karebaybio.com
Follow Us
Follow Karebay on LinkedinFollow IMAGING on Twitter Google+ Facebook