製品番号: HY-13775

XL019

5 Cited Publications

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.

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: 99.65%
CAS 番号: 945755-56-6
分子式: C₂₅H₂₈N₆O₂
分子量:444.53

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

XL019 構造式

CAS 番号: 945755-56-6

容量

価格（税別）

在庫状況

数量

Sample (0.1mg)

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(In Japan)

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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
- Cellular Effect
- 体内実験
- 臨床実験
化学情報
Publications (5)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

JAK2

2.2 nM (IC₅₀)

JAK3

214.2 nM (IC₅₀)

JAK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	7.34 μM Compound: XL019; 3	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 30243158]
MCF7	IC₅₀	27.2 μM Compound: XL019; 3	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30243158]
MDA-MB-231	IC₅₀	9.67 μM Compound: XL019; 3	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 30243158]
PC-3	IC₅₀	14.9 μM Compound: XL019; 3	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 30243158]

体内実験

XL019 (100-300 mg/kg; p.o.; twice daily for 14 days) inhibits HEL.92.1.7 xenograft tumor growth^[1].
XL019 (10 mg/kg) treatment shows that the?C_max, t_1/2?and V_d were?5.24 μM,?1.94 hours,?5.319 L/kg,?respectively^[1].

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

Animal Model:

Female nude mice (HEL.92.1.7 xenograft tumors)^[1]
Dosage:

100, 200, 300 mg/kg
Administration:

p.o.; twice daily for 14 days
Result:

Inhibition of HEL.92.1.7 xenograft tumor growth.

Animal Model:

Mouse^[1]
Dosage:

10 mg/kg
Administration:

p.o.(Pharmacokinetic Analysis)
Result:

The C_max, t_1/2 and V_d were 5.24 μM, 1.94 hours, and 5.319 L/kg, respectively.

臨床実験

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

化学情報

CAS 番号 945755-56-6
性状 Solid
分子量 444.53
分子式 C₂₅H₂₈N₆O₂
Color Light yellow to green yellow
SMILES

O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

All WB

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Ecotoxicol Environ Saf

Exposure to short-chain chlorinated paraffins induces astrocyte activation via JAK2/STAT3 signaling pathway. [Abstract]

2022 Dec 15:248:114268. PMID: 36375367

XL019 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 15:248:114268. [Abstract]

XL019 (10 μM) effectively attenuates the SCCP-mediated upregulation of iNOS and GFAP in C6 cells by Inhibiting JAK2.
Biochem Pharmacol

Dual inhibition of EGR1/STAT3 transcriptional hubs suppresses macrophage-driven liver fibrosis: A multi-omics-guided drug repurposing strategy. [Abstract]

2025 Oct:240:117120. PMID: 40623460

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (56.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.2496 mL

11.2478 mL

22.4957 mL

5 mM

0.4499 mL

2.2496 mL

4.4991 mL

10 mM

0.2250 mL

1.1248 mL

2.2496 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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

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 (273 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Portuguese - PT (418 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]. Forsyth T, et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2496 mL	11.2478 mL	22.4957 mL	56.2392 mL
	5 mM	0.4499 mL	2.2496 mL	4.4991 mL	11.2478 mL
	10 mM	0.2250 mL	1.1248 mL	2.2496 mL	5.6239 mL
	15 mM	0.1500 mL	0.7499 mL	1.4997 mL	3.7493 mL
	20 mM	0.1125 mL	0.5624 mL	1.1248 mL	2.8120 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2496 mL
	30 mM	0.0750 mL	0.3749 mL	0.7499 mL	1.8746 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4060 mL
	50 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1248 mL

Keywords

XL019

5 Cited Publications

100 mg お問い合わせ

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XL019

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 XL019

JAK 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 (5)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

XL019 関連分類

製品番号: HY-13775