1. MAPK/ERK Pathway
  2. p38 MAPK

Pexmetinib (Synonyms: ARRY-614)

Cat. No.: HY-16782 Purity: 98.30%
Handling Instructions

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

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

Pexmetinib Chemical Structure

Pexmetinib Chemical Structure

CAS No. : 945614-12-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 135 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 590 In-stock
Estimated Time of Arrival: December 31
100 mg USD 910 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

IC50 & Target

IC50: 1 nM (Tie-2), 35 nM (p38α), 26 nM (p38β)[1]

In Vitro

Pexmetinib is a Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively. Pexmetinib also shows IC50s of 4 nM (Abl), 10 nM (Arg), 28 nM (FGFR1), 47 nM (Flt1), 42 nM (Flt4), 41 nM (Fyn), 26 nM (Hck), 25 nM (Lyn), and 26 nM (MINK), respectively. Pexmetinib (0.5, 1 μM) blocks leukemic cell proliferation and stimulates hematopoietic activity in myelodysplastic syndromes[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (224.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7965 mL 8.9826 mL 17.9653 mL
5 mM 0.3593 mL 1.7965 mL 3.5931 mL
10 mM 0.1797 mL 0.8983 mL 1.7965 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cell lines and primary samples are incubated at indicated doses of of TIE2/p38 inhibitor Pexmetinib. Viability is assessed by addition of Cell Titer Blue and measured via Fluostar Omega Microplate reader[1].

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

References
Molecular Weight

556.63

Formula

C₃₁H₃₃FN₆O₃

CAS No.

945614-12-0

SMILES

O=C(NCC1=CC(F)=CC=C1OC2=CC3=C(N(CCO)N=C3)C=C2)NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Pexmetinib
Cat. No.:
HY-16782
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Pexmetinib

Cat. No.: HY-16782