C-1100 Cobimetinib, Free Base, >99%

Solubility: DMSO.

CMT-101

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• Cobimetinib demonstrated a sustained tumor pharmacodynamic response due to longer residence times in tumor tissue than in plasma in mice. Following single doses, cobimetinib inhibited pERK in tumors with IC50 values of 780 nM in WM-266-4 and 520 nM in A375 xenograft mice.  Following multiple doses, cobimetinib inhibited pERK in tumors with an increased IC50 value of 3.9 μM in WM-266-4 xenograft mice.  Wong H., et al. "Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor." Clin. Cancer Res. 18: 3090-3099 (2012).
• 18 F-FDG-PET imaging reflected cobimetinib and vemurafenib action across a wide range of metastatic melanomas..  Baudy A.R., et al. "FDG-PET is a good biomarker of both early response and acquired resistance in BRAF V600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973." EJNMMI Res. 2: 22 (2012).
• The combination treatment of cobimetinib with vemurafenib resulted in a significant improvement in progression-free survival among patients with BRAF V600-mutated metastatic melanoma. Larkin J. et al. "Combined vemurafenib and cobimetinib in BRAF-mutated melanoma." N. Engl. J. Med. 371: 1867-1876 (2014).
• Related CAS numbers:  1369665-02-0 for the fumarate salt; 1035349-31-5 for the hydrochloride salt; and 934665-58-4 for a hydrochloride salt of unknown stoichiometry.
• Another CAS number previously assigned to Cobimetinib, Free Base, 1029872-29-4, has been deleted by CAS and is no  longer in use.
• Cobimetinib (as the fumarate salt) is the active ingredient in the drug product sold under the trade name Cotellic®.  This drug is currently approved in a least one country for treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, in combination with vemurafenib.  NOTE:  THE COBIMETINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT COTELLIC®, AND IS NOT FOR HUMAN USE.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This  product is offered for R&D use in accordance with (i) 35 USC  271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in  Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in  Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977  in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law  exemptions of Canadian patent law; (vi) Section 68B of the Patents Act  of 1953 in New Zealand together with the amendment of same by the  Statutes Amendment Bill of 2002; (vii) such related legislation and/or  case law as may be or become applicable in the aforementioned countries;  and (viii) such similar laws and rules as may apply in various other  countries.
• Not available in some countries; not available to some institutions; not available for some uses.