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Cobimetinib hemifumarate

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Cobimetinib hemifumarate
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Cat #: V4524 CAS #: 1369665-02-0 Purity ≥ 98%

Description: Cobimetinib hemifumarate (formerly also known as RG7420; XL518; GDC0973), the hemifumarate salt of cobimetinib, is an oral, highly potent and selective MEK1 inhibitor with potential antineoplastic activity.

References: Hoeflich KP, et al. 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.

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Molecular Weight (MW)647.38
Molecular FormulaC₂₅H₂₅F₃IN₃O₆
CAS No.1369665-02-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 100 mg/mLr
Water: <1 mg/mLr
Ethanol: 47 mg/mL
Solubility In Vivo5% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
SMILES CodeO=C(/C=C/C(O)=O)O.O=C(N1CC(O)(C1)[C@H]2NCCCC2)C3=CC=C(C(F)=C3NC4=CC=C(C=C4F)I)F.O=C(N5CC(O)(C5)[C@H]6NCCCC6)C7=CC=C(C(F)=C7NC8=CC=C(C=C8F)I)F
SynonymsXL518 hemifumarate, GDC-0973, RG7420 fumarate; XL518; XL 518; XL-518 fumarate; GDC0973 fumarate; GDC 0973; GDC-0973; RG-7420; RG 7420 fumarate
ProtocolIn VitroThe EC50 values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC50 concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941).
In VivoIn the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.5447 mL7.7234 mL15.4469 mL30.8938 mL
5mM0.3089 mL1.5447 mL3.0894 mL6.1788 mL
10mM0.1545 mL0.7723 mL1.5447 mL3.0894 mL
20mM0.0772 mL0.3862 mL0.7723 mL1.5447 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.