Cobimetinib (GDC-0973, RG7420)

Catalog No.S8041 Synonyms: XL518

Cobimetinib (GDC-0973, RG7420) Chemical Structure

Molecular Weight(MW): 531.31

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.

Size Price Stock Quantity  
USD 197 In stock
USD 597 In stock
USD 997 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 19 Publications

Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.
Targets
MEK1 [1]
(Cell-free assay)
4.2 nM
In vitro

Cobimetinib shows strong activity on cell growth inhibtion in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In combination with GDC-0941, GDC-0973 results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. [1] Coadministration of GDC-0973 and vemurafenib significantly increases decreased levels of GLUT-1 on the cellular membrane across all BRAFV600E lines. [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells M1zpcGZ2dmO2aX;uJIF{e2G7 NFr4c4wyKGh? M4\Eb2lvcGmkaYTpc44hd2ZiTVXLMY1m\GmjdHXkJGVTUyCWMkCyM3kzODRicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKE2GQT3NRk0zOzGWIHPlcIx{KGGodHXyJFEhcHJiYomgbY1ufW6xYnzveJRqdmgxvJygTWM2OD1yLkKgcm0> Mlz2NlQ6ODB2OE[=
human COLO205 cells MXXGeY5kfGmxbjDhd5NigQ>? M2\sU2lvcGmkaYTpc44hd2ZiQj3yZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFPPUG8zODViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGVTUzFxRWLLNkBxcG:|cHjvdplt[XSrb36sJGlEPTB;MT64JI5O NYnrfFR1OjJ|MUWzN|I>
human COLO205 cells NGL0cIdRem:uaX\ldoF1cW:wIHHzd4F6 M1nicWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU|IxPSClZXzsd{BmgHC{ZYPzbY5oKEJvcnHmJHY3ODCHIH31eIFvfCxiSVO1NF05KG6P NIDVWlQzOjNzNUOzNi=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pERK / ERK / MCL-1 / p-MCL1 / BIM / cleaved PARP; 

PubMed: 27765849     


RKO cells were treated with increasing doses of cobimetinib for 48 h and protein expression, including BIM isoforms [extra long (EL), long (L) and short (S)] and PARP cleavage (CL), were analyzed by immunboblotting. 

p-c-RAF / c-RAF / p-MEK / MEK; 

PubMed: 26384788     


Effect of cobimetinib on MAPK cascade pathway. Changes in activation status of RAF, MEK and ERK were evaluated in three NB cell lines after treatment with cobimetinib (1 μM) or DMSO for four hours. Cell lysates were made with lysis buffer containing prote䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣痖�෋

27765849 26384788
Growth inhibition assay
Cell viability ; 

PubMed: 28098866     


MEL-XY3 cells were treated with different concentrations of GDC-0973 (0–10 µM) for 72 h and viability was determined using MTT assay. 

28098866
In vivo In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of GDC-0973 and GDC-0941 show improved efficacy. [1] In mice bearing drug-resistant A375 xenografts, combination of GDC-0973 and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. [2]

Protocol

Animal Research:

[1]
+ Expand
  • Animal Models: Molm-13, Molm-16, MX-1, DLD-1, HCT-116, LoVo, FaDu, 537MEL, A2058, A2058-X1, A375, A375.X1, A427, A549, Calu-6, EBC-1, NCI-H441, NCI-H2122, NCI-H460, NCI-H520.X1, SKOV-3, KP4-X1.1, MiaPaCa-2, 22Rv1, DU-145.X1,S, NCI-H69 xenograft tumors in mice
  • Formulation: --
  • Dosages: 10 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.21 mM)
Ethanol 47 mg/mL warmed (88.46 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 531.31
Formula

C21H21F3IN3O2
CAS No. 934660-93-2
Storage powder
in solvent
Synonyms XL518

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04005690 Recruiting Drug: Cobimetinib|Drug: Olaparib Resectable Pancreatic Ductal Adenocarcinoma|Stage 0 Pancreatic Cancer AJCC v8|Stage I Pancreatic Cancer AJCC v8|Stage IA Pancreatic Cancer AJCC v8|Stage IB Pancreatic Cancer AJCC v8|Stage II Pancreatic Cancer AJCC v8|Stage IIA Pancreatic Cancer AJCC v8|Stage IIB Pancreatic Cancer AJCC v8|Stage III Pancreatic Cancer AJCC v8 OHSU Knight Cancer Institute|National Cancer Institute (NCI) August 1 2019 Phase 2
NCT04007848 Recruiting Drug: Cobimetinib|Drug: Placebo oral tablet Disease or R Group Histiocytoses Assistance Publique - Hôpitaux de Paris July 25 2019 Phase 3
NCT03695380 Recruiting Drug: Cobimetinib|Drug: Niraparib|Drug: Atezolizumab OVARIAN CANCER Hoffmann-La Roche January 9 2019 Phase 1
NCT03273153 Active not recruiting Drug: Cobimetinib|Drug: Atezolizumab|Drug: Pembrolizumab Advanced BRAFV600 Wild-type Melanoma Hoffmann-La Roche December 11 2017 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    How to reconstitute the inhibitor for in vivo studies?

  • Answer:

    S8041 can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly and it is ok for both oral gavage and injection.

selleck catalog

MEK Signaling Pathway Map

Related MEK Products

  • BI-847325 New

    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

  • GDC-0623 New

    GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

  • Ravoxertinib (GDC-0994) New

    GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.

  • Trametinib (GSK1120212)

    Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.

    Features:More potent than PD0325901 or AZD6244.

  • PD0325901

    PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.

  • Selumetinib (AZD6244)

    Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.

    Features:First MEK inhibitor being tested in Phase II clinical trials.

  • U0126-EtOH

    U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059.

    Features:A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

  • PD98059

    PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.

    Features:Does not inhibit c-Raf phosphorylated MEK1.

  • PD184352 (CI-1040)

    PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.

    Features:First MEK inhibitor to begin clinical development.

  • Binimetinib (MEK162, ARRY-162, ARRY-438162)

    Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.

Tags: buy Cobimetinib (GDC-0973, RG7420) | Cobimetinib (GDC-0973, RG7420) supplier | purchase Cobimetinib (GDC-0973, RG7420) | Cobimetinib (GDC-0973, RG7420) cost | Cobimetinib (GDC-0973, RG7420) manufacturer | order Cobimetinib (GDC-0973, RG7420) | Cobimetinib (GDC-0973, RG7420) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID