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
CHZ868 动物实验
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.
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