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XL019

Catalog No. T3072   CAS 945755-56-6

XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.

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XL019 Chemical Structure
XL019, CAS 945755-56-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 68.00
10 mg In stock $ 122.00
25 mg In stock $ 223.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
1 mL * 10 mM (in DMSO) In stock $ 75.00
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Purity: 99.23%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
Targets&IC50 JAK2:2.2 nM
Kinase Assay FRET-Based Z′-Lyte Assay Detecting Peptide Substrate Phosphorylation: The kinases ABL1, ABL1(E255K), ABL1 (G250E), ABL1(T315I), and ABL1(Y253F) are P3049, PV3864, PV3865, PV3866, and PV3863 are full-length human recombinant protein expressed in insect cells and histidine-tagged. Inhibition activities of inhibitors against Abl1 and its mutants are performed in 384-well plates using the FRET-based Z′-Lyte assay system. Briefly, the kinase substrate is diluted into 5 μL of kinase reaction buffer; and the kinase is added. Compounds (10 nL) with indicated concentrations are then delivered to the reaction by using Echo liquid handler, and the mixture is incubated for 30 min at room temperature. Then 5 μL of 2X ATP solution is added to initiate the reaction, and the mixture is further incubated for 2 h at room temperature. The resulting reactions contains 10 μM (for wild-type Abl1, and mutants Y253F, Q252H, M351T, and H396P) or 5 μM (for mutants E255K, G250E, T315I) of ATP, 2 μM of Tyr2 Peptide substrate in 50 mM HEPES (PH 7.5), 0.01% BRIJ-35, 10 mM MgCl2, 1 mM EGTA, 0.0247 μg/mL Abl1, and inhibitors as appropriate. Then, 5 μL of development reagent is added, and the mixture is incubated for 2 h at room temperature before 5 μL of stop solution is added. Fluorescence signal ratio of 445 nm (Coumarin)/520 nm (fluorescin) is examined on an EnVision Multilabel Reader. The data are analyzed using Graphpad Prism5. The data are the mean value of three experiments.
Molecular Weight 444.53
Formula C25H28N6O2
CAS No. 945755-56-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 13 mg/mL (29.2 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

TargetMolReferences and Literature

1. Forsyth T, et al. Bioorg Med Chem Lett, 2012, 22(24), 7653-7658. 2. Verstovsek S. Hematology Am Soc Hematol Educ Program, 2009, 636-642.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Aging Compound Library Bioactive Compound Library Anti-Liver Cancer Compound Library Inhibitor Library Anti-Prostate Cancer Compound Library Anti-Cardiovascular Disease Compound Library

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Keywords

XL019 945755-56-6 Angiogenesis Apoptosis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FLT JAK PDGFR Janus kinase antitumor,HEL.92.1.7 Inhibitor cells XL 019 XL-019 inhibit selective oral phosphorylation tumor inhibitor

 

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