PZ0186
PF-477736
≥98% (HPLC)
别名:
(2R)-2-Amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-acetamide, PF-00477736
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选择尺寸
关于此项目
经验公式（希尔记法）:
C22H25N7O2
化学文摘社编号:
分子量:
419.48
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
PF-477736, ≥98% (HPLC)
InChI key
NDEXUOWTGYUVGA-LJQANCHMSA-N
SMILES string
Cn1cc(cn1)-c2[nH]c3cc(NC(=O)[C@H](N)C4CCCCC4)cc5C(=O)NN=Cc2c35
InChI
1S/C22H25N7O2/c1-29-11-13(9-25-29)20-16-10-24-28-21(30)15-7-14(8-17(27-20)18(15)16)26-22(31)19(23)12-5-3-2-4-6-12/h7-12,19,27H,2-6,23H2,1H3,(H,26,31)(H,28,30)/t19-/m1/s1
assay
≥98% (HPLC)
form
powder
color
yellow
solubility
DMSO: ≥20 mg/mL
storage temp.
2-8°C
Quality Level
Application
PF-477736 has been used as a checkpoint protein 1 (CHK1) inhibitor to study the effect of CHK1 in cell cycle regulation in primary breast and lung primary epithelial cells.
Biochem/physiol Actions
PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin.
PF-477736 may be effectively used to resensitize platinum resistant ovarian cancer cells. PF-477736 alone or in combination with other chemotherapeutic agents may be used to treat triple-negative breast cancer.
Potent and selective ATP-competitive inhibitor of Checkpoint kinase 1 (Chk1)
Other Notes
PF-477736 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PF-477736 probe summary on the Chemical Probes Portal website.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Marijn T M van Jaarsveld et al.
Oncogenesis, 9(3), 35-35 (2020-03-15)
Cancer is a life-threatening disease that affects one in three people. Although most cases are sporadic, cancer risk can be increased by genetic factors. It remains unknown why certain genes predispose for specific forms of cancer only, such as checkpoint
Abstract NTOC-095: THE SYNERGISTIC EFFECTS OF CARBOPLATIN AND PF--477736, A SMALL MOLECULE CHECKPOINT KINASE 1 INHIBITOR ON A PLATINUM RESISTANT OVARIAN CANCER CELL LINE
Lee J, et al.
Clinical Cancer Research, 9(3), 1-7 (2017)
Cell-type-specific role of CHK2 in mediating DNA damage-induced G2 cell cycle arrest
van Jaarsveld MTM, et al.
Oncogenesis, 9(3), 1-7 (2020)
Chk1 inhibition as a novel therapeutic strategy for treating triple-negative breast and ovarian cancers
Bryant C, et al.
BMC Cancer, 14(1), 570-570 (2014)
Stéphanie Arnould et al.
Oncotarget, 8(56), 95206-95222 (2017-12-10)
Reduction in nucleotide pools through the inhibition of mitochondrial enzyme dihydroorotate dehydrogenase (DHODH) has been demonstrated to effectively reduce cancer cell proliferation and tumour growth. The current study sought to investigate whether this antiproliferative effect could be enhanced by combining
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