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Cobimetinib

Chemical Structure : Cobimetinib

CAS No.: 934660-93-2

Cobimetinib (GDC-0973;XL-518;GDC 0973;XL 518;GDC0973;XL518)

Catalog No.: PC-43369Not For Human Use, Lab Use Only.

Cobimetinib (GDC-0973, XL-518) is a potent, selective MEK inhibitor with IC50 of 4.2 nM for MEK1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Cobimetinib (GDC-0973, XL-518) is a potent, selective MEK inhibitor with IC50 of 4.2 nM for MEK1.
Cobimetinib (GDC-0973, XL-518) shows excellent selectivity against mTOR, DNA-dependent protein kinase (DNA-PK), and a panel of more than 228 kinases.
Cobimetinib (GDC-0973, XL-518) shows strong cellular potency in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines, triggers robust apoptosis and tumor growth inhibition in vivo combined with PI3K inhibitor GDC-0941.

Physicochemical Properties

M.Wt 531.31
Formula C21H21F3IN3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Methanone, [3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl][3-hydroxy-3-[(2S)-2-piperidinyl]-1-azetidinyl]-

References

1. Hoeflich KP, et al. Cancer Res. 2012 Jan 1;72(1):210-9.

2. Wong H, et al. Clin Cancer Res. 2012 Jun 1;18(11):3090-9.

3. Rice KD, et al. ACS Med Chem Lett. 2012 Apr 9;3(5):416-21.

4. Ribas A, et al. Lancet Oncol. 2014 Aug;15(9):954-65.

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