1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

CHZ868 

Cat. No.: HY-18960 Purity: 98.33%
Handling Instructions

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

For research use only. We do not sell to patients.

CHZ868 Chemical Structure

CHZ868 Chemical Structure

CAS No. : 1895895-38-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 756 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

View All JAK Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

IC50 & Target[2]

JAK2

110 nM (IC50)

In Vitro

CHZ868 potently inhibits constitutive JAK2 and STAT5 phosphorylation in JAK2V617F SET2 cells. CHZ868 potently inhibits the proliferation of SET2 cells (GI50=59nM), and has 6-fold less growth inhibitory activity against CMK cells (GI50=378nM)[1]. At 100 nM CHZ868 has activity against 26 kinases, including JAK2 and TYK2. CHZ868 is thought to engage with the hinge region of JAK2 through two H-bonds, formed between the amino-pyridine of CHZ868 and the backbone-NH/CO of L932, while the pyridine is occupying the adenine pocket of the ATP binding site. CHZ868 potently suppresses the growth of CRLF2-rearranged human B-ALL cells, abrogates JAK2 signaling[2].

In Vivo

CHZ868 is characterized by high passive permeability, good metabolic stability, and low water solubility, as well as by moderate blood clearance and good oral bioavailability, making it suitable for in vivo use. CHZ868 improves survival in mice with human or murine B-ALL. CHZ868 and dexamethasone synergistically induces apoptosis in JAK2-dependent B-ALLs and further improves survival compared to CHZ868 alone[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.3617 mL 11.8086 mL 23.6172 mL
5 mM 0.4723 mL 2.3617 mL 4.7234 mL
10 mM 0.2362 mL 1.1809 mL 2.3617 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

CHZ868 is dissolved in DMSO to make 10 mM stock solution and diluted in culture media. Cells are treated with CHZ868 (0, 0.05, 0.1, 0.2 μM) or vehicle (DMSO). After 48 hr (Ba/F3 cells) or 72 hr (MHH-CALL4 and PDX cells), CellTiter-Glo Luminescent Cell Viability Assay is added (10 μL undiluted or 25 μL of a 1:2 dilution in each well) and plates are read[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: CHZ868 is reconstituted in 0.5% methylcellulose / 0.5% Tween-80 and administered at doses of 10 or 30 mg/kg/day by oral gavage. Pharmacokinetic/pharmacodynamic and efficacy studies in the mouse model of rhEpo-induced polycythemia are carried out essentially as reported. Detection of STAT5 phosphorylation in spleen lysates by Meso Scale Discovery is performed[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

423.42

Formula

C₂₂H₁₉F₂N₅O₂

CAS No.

1895895-38-1

SMILES

CC(NC1=CC(OC2=CC=C(N(C)C(NC3=CC=C(F)C=C3F)=N4)C4=C2C)=CC=N1)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 150 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.33%

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Product Name:
CHZ868
Cat. No.:
HY-18960
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