XL019
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.65%
- CAS No.: 945755-56-6
- Formule: C25H28N6O2
- Masse moléculaire:444.53
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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Immunology/Inflammation Compound Library
HY-L007
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JAK/STAT Compound Library
HY-L008
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Kinase Inhibitor Library
HY-L009
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Protein Tyrosine Kinase Compound Library
HY-L016
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Stem Cell Signaling Compound Library
HY-L017
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Anti-Cancer Compound Library
HY-L025
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Clinical Compound Library
HY-L026
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Anti-Aging Compound Library
HY-L034
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Drug Repurposing Compound Library
HY-L035
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Differentiation Inducing Compound Library
HY-L038
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Reprogramming Compound Library
HY-L039
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Orally Active Compound Library
HY-L061
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Blood Cancer Compound Library
HY-L079
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Anti-Obesity Compound Library
HY-L087
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Targeted Diversity Library
HY-L099
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Anti-Liver Cancer Compound Library
HY-L101
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Anti-Prostate Cancer Compound Library
HY-L124
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Cancer Stem Cells Compound Library
HY-L135
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Heterocyclic Compound Library
HY-L138
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Pain-Related Compound Library
HY-L139
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Autoimmune Disease Compound Library
HY-L156
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Rheumatic Arthritis Compound Library
HY-L210
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) XL019
More
Customer Validation & Images
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WB
Activité biologique
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JAK2 2.2 nM (IC50) |
JAK3 214.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
7.34 μM
Compound: XL019; 3
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Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 30243158] |
| MCF7 | IC50 |
27.2 μM
Compound: XL019; 3
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 30243158] |
| MDA-MB-231 | IC50 |
9.67 μM
Compound: XL019; 3
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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
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[PMID: 30243158] |
| PC-3 | IC50 |
14.9 μM
Compound: XL019; 3
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Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
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[PMID: 30243158] |
XL019 (10 mg/kg) treatment shows that the?Cmax, t1/2?and Vd 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.
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Animal Model:Female nude mice (HEL.92.1.7 xenograft tumors)[1]
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Dosage:100, 200, 300 mg/kg
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Administration:p.o.; twice daily for 14 days
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Result:Inhibition of HEL.92.1.7 xenograft tumor growth.
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Animal Model:Mouse[1]
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Dosage:10 mg/kg
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Administration:p.o.(Pharmacokinetic Analysis)
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Result:The Cmax, t1/2 and Vd were 5.24 μM, 1.94 hours, and 5.319 L/kg, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 945755-56-6
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Appearance Solid
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Masse moléculaire 444.53
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Formule C25H28N6O2
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Color Light yellow to green yellow
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SMILES
O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Science
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.
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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
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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.
| 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 |
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