PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes and shows ~100-fold selectivity for Chk1 than Chk2.
PF-477736 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HRP UWB+B1 cells
50 nM
24 hours
PF-477736 inhibited rucaparib-induced CHK1S296 phosphorylation and reduced RAD51 foci formation, indicating inhibition of HRR function.
Br J Cancer. 2024 Sep;131(5):905-917.
HRP V-C8.B2 cells
50 nM
24 hours
PF-477736 significantly potentiated rucaparib cytotoxicity, indicating sensitisation of HRP cells to PARPi via HRR inhibition.
Br J Cancer. 2024 Sep;131(5):905-917.
SKOV3 CR
20 µM
3 days
To investigate the combined effect of PF-477736 with cisplatin on cell viability.
Cancer Lett. 2018 Aug 1;428:104-116.
SMS-SAN cells
1 µM
3 days
Increased the expression of two pro-apoptotic proteins, BAX and PUMA, providing a mechanism for the effect of the CHK1 inhibitor
Int J Mol Sci. 2019 Jul 29;20(15):3700.
CHP134 cells
1 µM
3 days
Increased the expression of two pro-apoptotic proteins, BAX and PUMA, providing a mechanism for the effect of the CHK1 inhibitor
Int J Mol Sci. 2019 Jul 29;20(15):3700.
NB-39-nu cells
1 µM
3 days
Induced DNA double-strand breaks and activated the ATM-p53-p21 axis of the DDR pathway, which rendered the cells relatively insensitive to the antiproliferative effects of the CHK1 inhibitor
Int J Mol Sci. 2019 Jul 29;20(15):3700.
SK-N-BE cells
1 µM
3 days
Induced DNA double-strand breaks and activated the ATM-p53-p21 axis of the DDR pathway, which rendered the cells relatively insensitive to the antiproliferative effects of the CHK1 inhibitor
Int J Mol Sci. 2019 Jul 29;20(15):3700.
PF-477736 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
SKOV3 CR xenograft tumors
Oral and Intraperitoneal injection
60 mg/kg
2 weeks
To assess the antitumor effects of PF-477736 in combination with cisplatin.
搜索
