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Pimasertib (SAR245509, AS703026, MSC1936369B)

This product is for research use only, not for human use. We do not sell to patients.

Pimasertib (SAR245509, AS703026, MSC1936369B)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
500mg$790Check With Us
1g$1250Check With Us
5g$3160Check With Us

Cat #: V0455 CAS #: 1236699-92-5 Purity ≥ 98%

Description: Pimasertib (formerly SAR-245509, AS-703026, MSC-1936369B) is a selective, orally bioavailable and non-ATP competitive (allosteric) inhibitor of MEK1/2 with potential anticancer activity.

References: Kim K, et al. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol, 2010, 149(4), 537-549.

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Product Promise

Promise
Molecular Weight (MW)431.20
Molecular FormulaC15H15FIN3O3
CAS No.1236699-92-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 86 mg/mL (199.4 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo0.5% CMC+0.25% Tween 80: 30 mg/mL
SMILES CodeO=C(NC[C@H](O)CO)C1=CC=NC=C1NC2=CC=C(I)C=C2F
SynonymsMSC 1936369B, SAR 245509; AS-703026; SAR245509; SAR-245509; AS703026; AS 703026
ProtocolIn VitroPimasertib (5, 0.5, and 0.1 μM) specifically blocks ERK1/2 activation in MM cells, cultured alone or with BMSCs. Pimasertib inhibits the growth of MM cell lines in a dose-dependent manner, with IC50s ranging from 0.005 to 2 μM. The IC50s of Pimasertib against INA-6, U266, H929 cells are 10 nM, 5 nM, 200 nM respectively. Pimasertib induces apoptosis and modulates the cell cycle profile. Pimasertib targets MM cells in the BM microenvironment.
In VivoPimasertib (15, 30 mg/kg) significantly inhibits the growth of tumor in the human H929 MM xenograft model in CB17 SCID mice.
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
1mM2.3191 mL11.5955 mL23.1911 mL46.3822 mL
5mM0.4638 mL2.3191 mL4.6382 mL9.2764 mL
10mM0.2319 mL1.1596 mL2.3191 mL4.6382 mL
20mM0.1160 mL0.5798 mL1.1596 mL2.3191 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.