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MedKoo product information:

 

  Cobimetinib (GDC-0973)

   

Description of cobimetinib:  cobimetinib, also known as GDC-0973 and XL-518, is an orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor GDC-0973 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (last updated 8/1/2014)

  

MedKoo Cat#:  203185

Name:  Cobimetinib

CAS#:  934660-93-2

Synonym:   XL518; XL 518; XL-518; GDC-0973; GDC 0973; GDC0973; cobimetinib.

IUPAC/Chemical name: 

(S)-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)phenyl)(3-hydroxy-3-(piperidin-2-yl)cyclobutyl)methanone.

Chemical structure

Theoretical analysis

MedKoo Cat#:  203185
Name:  Cobimetinib
CAS#:  934660-93-2

Chemical Formula: C22H22F3IN2O2

Exact Mass: 530.06781

Molecular Weight: 530.32196

Elemental Analysis: C, 49.83; H, 4.18; F, 10.75; I, 23.93; N, 5.28; O, 6.03

 

Availability and price:

Cobimetinib (GDC-0973), purity > 98%, is available through custom synthesis. Current shipping out time is about 70 days after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee:  $30.00 (USA); $45.00 (Canada); $70.00 (international).

10mg / Not Available

25mg / Not Available

50mg / Not Available

100mg / Not Available

200mg / Not Available

500mg / Not Available

1.0g / Ask price

2.0g / Ask price

5.0g / Ask price

Please ask price and availability of other quantity.

  

 

Technical data

Product data sheet

View product data sheet

Appearance:

white solid powder

Purity:

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

View current batch of CoA

QC data:

View NMR, View HPLC, View MS

Safety Data Sheet (MSDS):

View Material Safety Data Sheet (MSDS)

Shipping condition:

Shipped under ambient temperature as non-hazardous chemical.  This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage condition:

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:

Soluble in DMSO, not in water

Shelf life:

>2 years if stored properly

Drug formulation:

This drug may be formulated in DMSO

Stock solution storage:

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Note: The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

 

Protocols from literature

In vitro protocol::

XXX

In vivo protocol:

XXX

Clinical study:

XXX

Review papers:

XXX 

 

Information about this agent

GDC-0973 is a potent and highly selective inhibitor of MEK (Figure 1A), with a biochemical IC50 of 4.2 nM against MEK1. In biochemical assays, GDC-0973 demonstrated >100-fold selectivity for MEK when tested against a panel of >100 serine-threonine and tyrosine kinases. GDC-0973 shows strong cellular potency in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines

 

Current developer:   Genentech

 

References

1: Choo EF, Ng CM, Berry L, Belvin M, Lewin-Koh N, Merchant M, Salphati L. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. doi: 10.1007/s00280-012-1988-6. Epub 2012 Oct 7. PubMed PMID: 23053270.

2: Baudy AR, Dogan T, Flores-Mercado JE, Hoeflich KP, Su F, van Bruggen N, Williams SP. FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973. EJNMMI Res. 2012 May 31;2(1):22. doi: 10.1186/2191-219X-2-22. PubMed PMID: 22651703; PubMed Central PMCID: PMC3405466.

3: Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L, Engst S, Joshi AA, Kennedy AR, Kim AI, Koltun ES, Lougheed JC, Manalo JC, Martini JF, Nuss JM, Peto CJ, Tsang TH, Yu P, Johnston S. Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med Chem Lett. 2012 Apr 9;3(5):416-21. doi: 10.1021/ml300049d. eCollection 2012 May 10. PubMed PMID: 24900486; PubMed Central PMCID: PMC4025802.

4: Wong H, Vernillet L, Peterson A, Ware JA, Lee L, Martini JF, Yu P, Li C, Del Rosario G, Choo EF, Hoeflich KP, Shi Y, Aftab BT, Aoyama R, Lam ST, Belvin M, Prescott J. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. doi: 10.1158/1078-0432.CCR-12-0445. Epub 2012 Apr 10. PubMed PMID: 22496205.

5: Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH. Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions. Drug Metab Dispos. 2012 May;40(5):919-27. doi: 10.1124/dmd.111.043778. Epub 2012 Feb 7. PubMed PMID: 22315332.

6: Hoeflich KP, Merchant M, Orr C, Chan J, Den Otter D, Berry L, Kasman I, Koeppen H, Rice K, Yang NY, Engst S, Johnston S, Friedman LS, Belvin M. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9. doi: 10.1158/0008-5472.CAN-11-1515. Epub 2011 Nov 14. PubMed PMID: 22084396.

 

 

 

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