PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies.
PFK158 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Acute myeloid leukemia cells
0.9 μM
96 hours
Evaluate the inhibitory effect of PFK158 combined with meclizine on AML cells, showing synergistic inhibition
J Hepatol. 2020 Apr;72(4):746-760.
HuH7 cells
2 or 5 μM
24 and 48 hrs
Evaluate the inhibitory effect of PFK158 combined with meclizine on the growth of liver cancer cells, showing synergistic inhibition
J Hepatol. 2020 Apr;72(4):746-760.
HepG2 cells
2 or 5 μM
24 and 48 hrs
Evaluate the inhibitory effect of PFK158 combined with meclizine on the growth of liver cancer cells, showing synergistic inhibition
J Hepatol. 2020 Apr;72(4):746-760.
DMS53 cells
0, 2.5, 5, 10 μM
24 hours
Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2
Oncogene. 2022 Aug;41(33):4003-4017.
H1876 cells
0, 2.5, 5, 10 μM
24 hours
Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2
Oncogene. 2022 Aug;41(33):4003-4017.
H1882 cells
0, 2.5, 5, 10 μM
24 hours
Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2
Oncogene. 2022 Aug;41(33):4003-4017.
H1048 cells
0, 2.5, 5, 10 μM
24 hours
Inhibition of glycolysis, proliferation, spheroid formation, and the expression of cancer stem cell markers CD133, Aldh1, CD44, Sox2, and ABCG2
Oncogene. 2022 Aug;41(33):4003-4017.
Patient-derived ascites cells
3-5µM
24 hours
To evaluate the effect of PFK158 on cell viability, results showed that PFK158 treatment reduced cell viability and restored primary cilia formation
J Exp Clin Cancer Res. 2021 Jun 3;40(1):182.
OVCAR5
10µM
24 hours
To evaluate the effect of PFK158 on primary cilia formation, results showed that PFK158 treatment significantly restored primary cilia formation
J Exp Clin Cancer Res. 2021 Jun 3;40(1):182.
OVCAR8
10µM
24 hours
To evaluate the effect of PFK158 on primary cilia formation, results showed that PFK158 treatment significantly restored primary cilia formation
J Exp Clin Cancer Res. 2021 Jun 3;40(1):182.
EMMeso
0-30μM
24 and 48 hours
PFK158 treatment inhibited MPM cell viability with IC50 values ranging from 3 to 12μM
Cell Death Dis. 2019 Sep 27;10(10):725.
NCI-H28
0-30μM
24 and 48 hours
PFK158 treatment inhibited MPM cell viability with IC50 values ranging from 3 to 12μM
Cell Death Dis. 2019 Sep 27;10(10):725.
OVCAR8 cells
5 µM
48 hours
To evaluate the effect of PFK158 on PARPi resistance, results showed that PFK158 inhibited PFKFB3 activity and enhanced PARPi sensitivity.
Cell Commun Signal. 2025 Jan 25;23(1):48.
SKOV3 cells
5 µM
48 hours
To evaluate the effect of PFK158 on PARPi resistance, results showed that PFK158 inhibited PFKFB3 activity and enhanced PARPi sensitivity.
Cell Commun Signal. 2025 Jan 25;23(1):48.
ARK-2
0-20 μM
24-72 hours
Inhibited cell proliferation, reduced glucose uptake, ATP production, and lactate dehydrogenase activity
Oncogene. 2021 Feb;40(8):1409-1424.
HEC-1B
0-20 μM
24-72 hours
Inhibited cell proliferation, reduced glucose uptake, ATP production, and lactate dehydrogenase activity
Oncogene. 2021 Feb;40(8):1409-1424.
HeyA8MDR
5μM
30 minutes
To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake
Int J Cancer. 2019 Jan 1;144(1):178-189.
HeyA8
5μM
30 minutes
To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake
Int J Cancer. 2019 Jan 1;144(1):178-189.
C13
5μM
30 minutes
To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake
Int J Cancer. 2019 Jan 1;144(1):178-189.
OV2008
5μM
30 minutes
To evaluate the effect of PFK158 on glucose uptake, results showed that PFK158 treatment significantly decreased glucose uptake
Int J Cancer. 2019 Jan 1;144(1):178-189.
EMMeso
5 µM
24 hours
PFK158 treatment significantly increased p27 levels in EMMeso cells.
Br J Cancer. 2022 Oct;127(7):1352-1364.
NCI-H2052
2.5 µM
24 hours
PFK158 significantly decreased SOX2 and CD133 transcript levels in H2052 cells.
Br J Cancer. 2022 Oct;127(7):1352-1364.
NCI-H28
2.5 µM
24 hours
PFK158 significantly decreased SOX2, CD133 and CD44 transcript levels in H28 cells.
Br J Cancer. 2022 Oct;127(7):1352-1364.
DMS79
2.5 μM
72 hours
To evaluate the effect of PFK158 on ATP production, glucose uptake, and lactate secretion in MYC-low SCLC cell lines. Results showed that PFK158 had minimal effect on ATP production, glucose uptake, and lactate.
Cancer Metab. 2021 Sep 23;9(1):33.
H446
2.5 μM
72 hours
To evaluate the effect of PFK158 on ATP production, glucose uptake, and lactate secretion in MYC-high SCLC cell lines. Results showed that PFK158 significantly attenuated glucose uptake, ATP production, and lactate.
Cancer Metab. 2021 Sep 23;9(1):33.
PFK158 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
SCID-NSG mice
H1048 CSC xenograft model
Intraperitoneally (ip)
25 mg/kg
Twice a week for 3 weeks
PFK158 treatment and PFKFB3 knockdown significantly reduced tumor growth and weight with reduced expression of cancer stem cell markers, ABCG2, and YAP/TAZ
Oncogene. 2022 Aug;41(33):4003-4017.
NOG mice
Human hepatocarcinoma cell line xenotransplantation model
Oral
25 mg/kg
Once daily for two weeks
Evaluate the inhibitory effect of PFK158 combined with meclizine on liver cancer growth, showing significant reduction in tumor burden
J Hepatol. 2020 Apr;72(4):746-760.
Female athymic nude mice
EMMeso xenograft model
Subcutaneous injection
30 mg/kg
Twice a week for 2 weeks
PFK158 alone or in combination with carboplatin significantly inhibited tumor growth
Cell Death Dis. 2019 Sep 27;10(10):725.
BALB/c nude mice
SKOV3 xenograft models
Intraperitoneally
35 mg/kg
Twice weekly for 28 days
To evaluate the in vivo efficacy of PFK158 combined with PARPi, results showed that the combination significantly inhibited tumor growth and increased DNA damage.
Cell Commun Signal. 2025 Jan 25;23(1):48.
Nude mice
HEC-1B and ARK-2 xenograft models
Intraperitoneal injection
35 mg/kg
Twice weekly for 14 days
Significantly inhibited tumor growth, reduced tumor volume and weight, and enhanced chemosensitivity
Oncogene. 2021 Feb;40(8):1409-1424.
Female athymic nude mice
Highly metastatic PTX-resistant ovarian mouse model
Intraperitoneal injection
25 mg/kg
PFK158 every 3rd day, CBPt every 3rd day, PTX every 5th day, for 28 days
To evaluate the effect of PFK158 alone or in combination with CBPt/PTX on tumor growth and ascites, results showed that the combination treatment significantly reduced tumor weight and ascites
Int J Cancer. 2019 Jan 1;144(1):178-189.
Female athymic nude mice
MPM xenograft model
30 mg/kg
Twice a week for 2 weeks
PFK158 significantly reduced tumour burden, tumour weight and tumour volume in TIC-mediated MPM xenografts.
Br J Cancer. 2022 Oct;127(7):1352-1364.
Mice
Apoe−/− mice
Intraperitoneal injection
2 mg/kg
3 times per week for 5 weeks
To evaluate the effect of PFK158 on plaque stability, results showed that PFK158 improved plaque stability.
Br J Pharmacol. 2022 Nov;179(21):4974-4991.
Nude mice
H446 xenograft model
Intraperitoneal injection
25 mg/kg
Every 2 days for a total of six treatments
To evaluate the effect of PFK158 on tumor growth in MYC-high SCLC xenograft models. Results showed that PFK158 significantly delayed tumor growth.
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