Pexmetinib
Pexmetinib (ARRY-614) is a potent, orally active, dual Tie-2/p38 MAPK inhibitor with IC50 of 1, 26 and 35 nM for Tie-2, p38α and p38β, respectively; demonstrates in vitro mechanistic models (Angpt-1 or anisomycin-stimulated HUVEC) as well as functional readouts (LPS-induced TNF-alpha release from human PBMCs) with IC50 of 2282 nM and 172 nM for Tie2 and p38, respectively; abrogates cytokine mediated myelosuppresive effects in hematopoietic cells; inhibits leukemic cell proliferation and stimulates hematopoietic activity in MDS; inhibits LPS-induced TNF-alpha release) murine models .Blood Cancer Phase 1 Discontinued.
Product Specifications
CAS Number
945614-12-0
Product Name Alternative
ARRY-614 | ARRY614
Purity
>98% (HPLC)
Solubility
DMSO: 93 mg/mL (167.1 mM) ; Ethanol: 93 mg/mL (167.1 mM) ; Water: <1 mg/mL (< 1 mg/ml refers to the product slightly soluble or insoluble)
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
Molecular Formula
C31H33FN6O3
Molecular Weight
556.63
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1- (3- (tert-butyl) -1- (p-tolyl) -1H-pyrazol-5-yl) -3- (5-fluoro-2- ((1- (2-hydroxyethyl) -1H-indazol-5-yl) oxy) benzyl) urea
Available Sizes
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