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Chemical Structure| 1895895-38-1 Chemical Structure| 1895895-38-1

Structure of CHZ868
CAS No.: 1895895-38-1

Chemical Structure| 1895895-38-1

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

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Product Details of CHZ868

CAS No. :1895895-38-1
Formula : C22H19F2N5O2
M.W : 423.42
SMILES Code : CC(NC1=NC=CC(OC2=CC=C3N(C)C(NC4=CC=C(F)C=C4F)=NC3=C2C)=C1)=O
MDL No. :MFCD30533612

Safety of CHZ868

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of CHZ868

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
TF1.8 cells 500 nM 5 or 15 min Inhibited IL-3-induced phosphorylation of JAK2, STAT5, and ERK Sci Adv. 2018 Nov 28;4(11):eaat3834
SET-2 cells 500 nM 48 h Inhibited cell proliferation Sci Adv. 2018 Nov 28;4(11):eaat3834
Ba/F3 cells 0.3 µM and 0.5 µM 48 h To investigate the effect of CHZ868 on JAK2 inhibitor-resistant cells. The results showed that the IC50 values of resistant cells to CHZ868 significantly increased, indicating that the cells had developed resistance to CHZ868 Clin Cancer Res. 2024 Feb 1;30(3):586-599.
Ba/F3 cells 0.5 μmol/L To study the resistance of Ba/F3 cells to CHZ868, results showed significantly increased IC50 Clin Cancer Res. 2024 Feb 1;30(3):586-599.
SET2 cells 0.3 μmol/L and 0.5 μmol/L To study the resistance mechanism of MPN cells to type II JAK2 inhibitors, results showed increased IC50 and reduced apoptosis in SET2 cells Clin Cancer Res. 2024 Feb 1;30(3):586-599.
CRLF2-rearranged B-ALL PDX cells 1 μM 48 h To evaluate the effect of CHZ868 on the proliferation and apoptosis of CRLF2-rearranged B-ALL PDX cells Cancer Cell. 2015 Jul 13;28(1):29-41
MHH-CALL4 cells 100 nM 72 h To evaluate the inhibitory effect of CHZ868 on the proliferation of MHH-CALL4 cells Cancer Cell. 2015 Jul 13;28(1):29-41
Ba/F3 JAK2 V617F cells 0.06 μM 48 h To evaluate the anti-proliferative effect of CHZ868 on JAK2 V617F mutant cells, results showed that CHZ868 was more potent in inhibiting JAK2 V617F cells compared to wild-type JAK2 cells. Cancer Cell. 2015 Jul 13;28(1):15-28
SET2 cells 59 nM 48 h To evaluate the anti-proliferative effect of CHZ868 on JAK2 V617F mutant cells, results showed that CHZ868 effectively inhibited the proliferation of SET2 cells. Cancer Cell. 2015 Jul 13;28(1):15-28

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID gamma (NSG) mice Subcutaneous xenograft model and systemic cell line-derived mouse model Oral gavage 15 mg/kg Daily or twice daily, treatment continued until tumor volume reached the upper limit To evaluate the inhibitory effect of combined JAK2/AXL or JAK2/MAPK inhibition on tumor growth, results showed that combination therapy significantly inhibited tumor growth Clin Cancer Res. 2024 Feb 1;30(3):586-599.
Mice CRLF2-rearranged B-ALL PDX model Oral 30 mg/kg/day Once daily for 25 days To evaluate the anti-tumor effect of CHZ868 in CRLF2-rearranged B-ALL PDX models Cancer Cell. 2015 Jul 13;28(1):29-41
Mice Jak2 V617F conditional knock-in mouse model Oral 30-40 mg/kg Once daily for 2-3 weeks To evaluate the efficacy of CHZ868 in a Jak2 V617F-driven polycythemia vera model, results showed that CHZ868 significantly reduced the proportion of mutant cells, improved splenomegaly and liver weight, and decreased hematocrit. Cancer Cell. 2015 Jul 13;28(1):15-28

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.81mL

2.36mL

1.18mL

23.62mL

4.72mL

2.36mL

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
Protocol 2
 

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