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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Angiopoietin Receptor-Pexmetinib
Pexmetinib

Chemical Structure : Pexmetinib

CAS No.: 945614-12-0

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Pexmetinib (ARRY-614, ARRY614)

货号: PC-35149Not For Human Use, Lab Use Only.

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.

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10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
Pexmetinib (ARRY-614) 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.
Pexmetinib (ARRY-614) abrogates cytokine mediated myelosuppresive effects in hematopoietic cells.
Pexmetinib (ARRY-614) inhibits leukemic cell proliferation and stimulates hematopoietic activity in MDS.
Pexmetinib (ARRY-614) inhibits LPS-induced TNF-alpha release) murine models .

物理化学性质&存储条件

分子量 556.63
分子式 C31H33FN6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Bachegowda L, et al. Cancer Res. 2016 Aug 15;76(16):4841-4849.

2. Garcia-Manero G, et al. Clin Cancer Res. 2015 Mar 1;21(5):985-94.

3. Wollenberg LA, et al. Clin Pharmacol. 2015 Sep 30;7:87-95.

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