1. MAPK/ERK Pathway
  2. MEK
  3. Pimasertib

Pimasertib (Synonyms: AS703026; MSC1936369B)

Cat. No.: HY-12042 Purity: 99.70%
Handling Instructions

Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.

For research use only. We do not sell to patients.

Pimasertib Chemical Structure

Pimasertib Chemical Structure

CAS No. : 1236699-92-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 65 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 280 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All MEK Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.

IC50 & Target

MEK1

 

MEK2

 

In Vitro

Pimasertib (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[1]. Pimasertib (10 μmol/L) inhibits ERK pathway, proliferation, and transformation in cetuximab-resistant D-MUT cells[2]. Pimasertib in combination with PLX4032 significantly induces apoptosis of RPMI-7951 cells, whereas each drug used alone does not. Pimasertib synergizes with small interfering RNA-mediated downregulation of BRAF to produce results similar to those of combined treatment with PLX4032 and Pimasertib[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pimasertib (15, 30 mg/kg) significantly inhibits the growth of tumor in the human H929 MM xenograft model in CB17 SCID mice[1]. Pimasertib (10 mg/kg, p.o.) inhibits tumor growth of cetuximab-resistant tumor attributed by K-ras mutation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

431.20

Formula

C₁₅H₁₅FIN₃O₃

CAS No.

1236699-92-5

SMILES

FC1=C(C=CC(I)=C1)NC2=CN=CC=C2C(NC[[email protected]@H](CO)O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (231.91 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3191 mL 11.5955 mL 23.1911 mL
5 mM 0.4638 mL 2.3191 mL 4.6382 mL
10 mM 0.2319 mL 1.1596 mL 2.3191 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

The inhibitory effects of study compounds on MM cell growth and survival are assessed by both [3H]thymidine incorporation and by measuring MTT dye absorbance. Cells (104/well for MM cell line, in triplicates and 2-5×105/well for patient MM cells) are cultured in 96-well plates for 3 days (MM cell lines) or 5-days (patient MM cells). For the [3H]thymidine incorporation assay, cells are pulsed with 0.5 μCi (0.0185 MBq)/well [3H]thymidine for 6 h (cell lines), harvested onto glass fiber filters, and counted in a β-scintillation counter. Due to low DNA synthesis of patient MM cells, they are pulsed with 2 μCi/well [3H]thymidine and measured during the last 36 h of culture.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

CB17 severe combined immunodeficiency (SCID) mice are subcutaneously inoculated with H929 (4×106) cells in 100 μL RPMI-1640 medium. Mice developed palpable tumors (appr 130 mm3) approximately 3 weeks after cell injection and are randomized to receive orally twice daily either Pimasertib (15 or 30 mg/kg) or control vehicle alone. Tumor size is measured every other day in 2 dimensions using calipers, and tumor volume is calculated. Animals are euthanized when their tumors reach 2 cm3 in volume, when they are moribund or show paralysis or major compromise in their quality of life occurs. Tumor formation changes in mice treated with control vehicle vs. Pimasertib are plotted using the GraphPad Prism version 4.03 for Windows. Tumors are subjected to immunoblotting and immunochemistry analyses using specific monoclonal (m)Abs. Images are examined with a Leica DM LB research microscope, captured using Leica IM50 Image Manager, and processed using Adobe Photoshop Software version 7.0.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.70%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

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: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PimasertibAS703026 MSC1936369BAS 703026AS-703026MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Pimasertib
Cat. No.:
HY-12042
Quantity:
MCE Japan Authorized Agent: