Pexmetinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pexmetinib (ARRY-614) 是一种有效的口服活性 Tie-2/p38 MAPK 双重抑制剂，对 Tie-2、p38α 和 p38β 的 IC50 分别为 1、26 和 35 nM。

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.

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.

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ARRY-614 | ARRY614

Tyrosine Kinase

Angiopoietin Receptor

p38MAPK

Cancer

Blood cancer

945614-12-0

556.63

C31H33FN6O3

>98% (HPLC)

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 )

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

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

(-20℃)

With Ice Pack

≥ 2 years