Cobimetinib (GDC-0973, XL518) | MEK1/2 inhibitor, YAP-TEAD inhibitor

Chemical Structure : Cobimetinib

CAS No.: 934660-93-2

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

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

Cobimetinib (GDC-0973, XL518) is a potent, selective MEK1/2 inhibitor with IC50 of 4.2 nM for MEK1, also is a potent inhibitor of YAP-TEAD complex, binds to TEAD lipid pocket and disrupts TEAD palmitoylation.

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5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$198	In stock
50 mg	$298	In stock
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Biological Activity

Cobimetinib (GDC-0973, XL518) is a potent, selective MEK1/2 inhibitor with IC50 of 4.2 nM for MEK1, also is a potent inhibitor of YAP-TEAD complex, binds to TEAD lipid pocket and disrupts TEAD palmitoylation.

Cobimetinib (GDC-0973, XL518) shows excellent selectivity against mTOR, DNA-dependent protein kinase (DNA-PK), and a panel of more than 228 kinases.

Cobimetinib (GDC-0973, XL518) 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.

Cobimetinib could overcome resistance to mitogen-activated protein kinase kinase 1/2 inhibitors.

Cobimetinib suppressed tumor growth and tumorigenesis associated with hyperactivated YAP-TEAD activities in mouse model of lung cancer.

Cobimetinib bolstered the efficacy of sorafenib and lenvatinib in inhibiting both hepatocellular carcinoma tumor growth and tumorigenesis.

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.

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

Biological Activity

Physicochemical Properties

References

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