製品番号: HY-16782

Pexmetinib

(別名: ARRY-614)

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC₅₀s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.81%
CAS 番号: 945614-12-0
分子式: C₃₁H₃₃FN₆O₃
分子量:556.63

保管条件:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pexmetinib 構造式

CAS 番号: 945614-12-0

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 臨床実験
化学情報
Publications (2)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC50: 1 nM (Tie-2), 35 nM (p38α), 26 nM (p38β)^[1]

Tie アイソフォーム固有の製品をすべて表示 :

Tie1
Tie2

p38 MAPK アイソフォーム固有の製品をすべて表示 :

体外実験

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 945614-12-0
性状 Solid
分子量 556.63
分子式 C₃₁H₃₃FN₆O₃
Color White to off-white
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
別名

ARRY-614
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Cancer Res

SMAD4 and KRAS Status Shape Cancer Cell-Stromal Crosstalk and Therapeutic Response in Pancreatic Cancer. [Abstract]

2025 Apr 15;85(8):1368-1389. PMID: 39841099
Mol Hum Reprod

Angiopoietin 2 stimulates trophoblast invasion via a mechanism associated with JNK signaling. [Abstract]

2021 Feb 27;27(3):gaab014. PMID: 33629098

溶剤 & 溶解度

体外:

DMSO : ≥ 125 mg/mL (224.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7965 mL	8.9826 mL	17.9653 mL	44.9131 mL
	5 mM	0.3593 mL	1.7965 mL	3.5931 mL	8.9826 mL
	10 mM	0.1797 mL	0.8983 mL	1.7965 mL	4.4913 mL
	15 mM	0.1198 mL	0.5988 mL	1.1977 mL	2.9942 mL
	20 mM	0.0898 mL	0.4491 mL	0.8983 mL	2.2457 mL
	25 mM	0.0719 mL	0.3593 mL	0.7186 mL	1.7965 mL
	30 mM	0.0599 mL	0.2994 mL	0.5988 mL	1.4971 mL
	40 mM	0.0449 mL	0.2246 mL	0.4491 mL	1.1228 mL
	50 mM	0.0359 mL	0.1797 mL	0.3593 mL	0.8983 mL
	60 mM	0.0299 mL	0.1497 mL	0.2994 mL	0.7486 mL
	80 mM	0.0225 mL	0.1123 mL	0.2246 mL	0.5614 mL
	100 mM	0.0180 mL	0.0898 mL	0.1797 mL	0.4491 mL

Keywords

Pexmetinib

2 Cited Publications

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Pexmetinib

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MedChemExpress（MCE）の使用を引用している文献 Pexmetinib

Tie アイソフォーム固有の製品をすべて表示

p38 MAPK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Pexmetinib 関連分類

HY-16782 関連分類