A dual inhibitor of Tie2 and p38 MAPK
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Pexmetinib

Item No. 26187

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[[5-fluoro-2-[[1-(2-hydroxyethyl)-1H-indazol-5-yl]oxy]phenyl]methyl]-urea
CAS Number
945614-12-0
Synonyms
  • ARRY 614
Molecular Formula
C31H33FN6O3
Formula Weight
556.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
λmax
310 nm
SMILES
FC1=CC(CNC(NC2=CC(C(C)(C)C)=NN2C3=CC=C(C)C=C3)=O)=C(OC4=CC=C(N(CCO)N=C5)C5=C4)C=C1
InChi Code
InChI=1S/C31H33FN6O3/c1-20-5-8-24(9-6-20)38-29(17-28(36-38)31(2,3)4)35-30(40)33-18-22-15-23(32)7-12-27(22)41-25-10-11-26-21(16-25)19-34-37(26)13-14-39/h5-12,15-17,19,39H,13-14,18H2,1-4H3,(H2,33,35,40)
InChi Key
LNMRSSIMGCDUTP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).1 It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bachegowda, L., Morrone, K., Winski, S.L., et al. Pexmetinib: A novel dual inhibitor of Tie-2 and p38 MAPK with efficacy in preclinical models of myelodysplastic syndromes and acute myeloid leukemia. Cancer Res. 76(16), 4841-4849 (2016).