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Chemical Structure| 945755-56-6 Chemical Structure| 945755-56-6

Structure of XL019
CAS No.: 945755-56-6

Chemical Structure| 945755-56-6

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XL019 is a selective and potent JAK2 inhibitor with IC50 value of 2.2 nM, with less potency to JAK1, JAK3, FLT3 and PDGFRβ with IC50 values of 134.3 nM, 214.2 nM, 139.7 nM and 125.4 nM, respectively.

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Product Details of XL019

CAS No. :945755-56-6
Formula : C25H28N6O2
M.W : 444.53
SMILES Code : O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2
MDL No. :MFCD24386874
InChI Key :ISOCDPQFIXDIMS-QHCPKHFHSA-N
Pubchem ID :57990869

Safety of XL019

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of XL019

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • JAK1

    JAK1, IC50:134.3 nM

  • JAK3

    JAK3, IC50:214.2 nM

  • JAK2

    JAK2, IC50:2.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
PANC1 cells 2.5 µM 24 h XL019, as a JAK2 inhibitor, further enhanced the cytotoxic effect of DHA/DDP PMC8280115
Hep3B cells 10 nM 48 h To study the effect of XL019 on the invasion ability of Hep3B cells, results showed that XL019 inhibited CEP55 overexpression-induced cell invasion. PMC6115913
PANC1 cells 2.5 µM 24 h Inhibition of NF-κB, JAK2, and ERK pathways further enhanced the cytotoxicity of DHA/DDP PMC8280115
hMSC-TERT cells 3 µM 10 days XL019 significantly reduced ALP activity in hMSC-TERT cells, indicating inhibition of osteoblast differentiation. PMC7866227

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00522574 Myeloproliferative Disorders|M... More >>yelofibrosis|Polycythemia Vera|Thrombocythemia, Essential Less << PHASE1 TERMINATED - UCSF - Division of Hematology/... More >>Oncology, San Francisco, California, 94143, United States|H. Lee Moffitt Cancer Center & Research Institute, Tampa, Florida, 33612, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Mt. Sinai School of Medicine, New York, New York, 10029, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States Less <<
NCT00595829 Polycythemia Vera PHASE1 TERMINATED 2025-02-09 UCLA School of Medicine, Cente... More >>r for Health Sciences, Los Angeles, California, 90095, United States|UCSF - Division of Hematology/Oncology, San Francisco, California, 94143, United States|H. Lee Moffitt Cancer Center & Research Institute, Tampa, Florida, 33612, United States|University of Michigan Health System, Ann Arbor, Michigan, 48109, United States|Weill Cornell Medical College, New York, New York, 10065, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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