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Pexmetinib (ARRY-614) Sale

(Synonyms: ARRY-614) 目录号 : GC11857

A dual inhibitor of Tie2 and p38 MAPK

Pexmetinib (ARRY-614) Chemical Structure

Cas No.:945614-12-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥943.00
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1mg
¥350.00
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5mg
¥770.00
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10mg
¥1,330.00
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25mg
¥2,730.00
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50mg
¥4,130.00
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100mg
¥5,670.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

Cell lines and primary samples are incubated at indicated doses of of TIE2/p38 inhibitor Pexmetinib. Viability is assessed by addition of Cell Titer Blue and measured via Fluostar Omega Microplate reader[1].

References:

[1]. Bachegowda L, et al. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res. 2016 Aug 15;76(16):4841-4849.

产品描述

Pexmetinib (ARRY-614) is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. The in vitro IC50 values of ARR Y-614 for both Tie2 and p38 mitogen-activated protein kinase are 1000 ng/mL and 100 ng/mL, respectively [1, 2].

p38 is a group of mitogen-activated protein kinases. MAPKs are activated by the dual phosphorylation of Tyr and Thr residues in the Thr-Xaa-Tyr motif in subdomain VIII. Data indicated that p38 MAPK may mediate signaling to the nucleus [3].

ARRY-614 is active against MAPK and Tie2/Tek receptor tyrosine kinase in cells. In primary human bone marrow stromal cells, ARRY-614 inhibited basal cytokines with an IC50 value ranging from 50-100 nM [4].

In dose escalation or expansion cohorts, treatment with ARRY-614 either once daily or twice daily was applied to forty-five patients. ARRY-614 reduced the levels of circulating biomarkers and the p38 MAPK activation of bone marrow [1]. In ex vivo stimulated human whole blood, LPS-induced cytokines was inhibited by ARRY-614 with an IC50 value ranging from 50-120 nM. ARRY-614 inhibited the release of IL-6 from SEA- or LPS-challenged mice with an ED50 value less than 10 mg/kg. Combining ARRY-614 with lenalidomide inhibited both pro-inflammatory cytokines and tumor growth in vivo with higher potency, compared with either agent alone [4].

References:
[1].  Garcia-Manero G, Khoury HJ, Jabbour E, et al. A phase I study of oral ARRY-614, a p38 MAPK/Tie2 dual inhibitor, in patients with low or intermediate-1 risk myelodysplastic syndromes. Clinical Cancer Research, 2015, 21(5): 985-994.
[2].  Wollenberg LA, Corson DT, Nugent CA, et al. An exploratory, randomized, parallel-group, open-label, relative bioavailability study with an additional two-period crossover food-effect study exploring the pharmacokinetics of two novel formulations of pexmetinib (ARRY-614). Clinical pharmacology: advances and applications, 2015, 7: 87.
[3].  Raingeaud J, Whitmarsh AJ, Barrett T, et al. MKK3-and MKK6-regulated gene expression is mediated by the p38 mitogen-activated protein kinase signal transduction pathway. Molecular and cellular biology, 1996, 16(3): 1247-1255.
[4].  Winski S, Humphries M, Yeh T, et al. Activity of ARRY-614, an inhibitor of p38 map kinase and angiogenic targets, in hematologic malignancies. Cancer Research, 2009, 69(9 Supplement): 331-331.

Chemical Properties

Cas No. 945614-12-0 SDF
别名 ARRY-614
化学名 (Z)-N-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-N'-(5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)benzyl)carbamimidic acid
Canonical SMILES CC1=CC=C(N2C(N/C(O)=N/CC3=CC(F)=CC=C3OC4=CC=C5C(C=NN5CCO)=C4)=CC(C(C)(C)C)=N2)C=C1
分子式 C31H33FN6O3 分子量 556.63
溶解度 ≥ 107.6 mg/mL in DMSO, ≥ 113 mg/mL in EtOH 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 1.7965 mL 8.9826 mL 17.9653 mL
5 mM 0.3593 mL 1.7965 mL 3.5931 mL
10 mM 0.1797 mL 0.8983 mL 1.7965 mL
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