Pexmetinib

SKU: orb1223552

Description

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.

Key Properties

• CAS Number: 945614-12-0
• MW: 556.63
• Purity: >98% (HPLC)
• Formula: C₃₁H₃₃FN₆O₃
• 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
• Target: Angiopoietin Receptor
• 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 )

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ARRY-614 | ARRY614

Quick Database Links

Gene Symbol

Angiopoietin Receptor