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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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:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
yellow
solubility
DMSO: ≥20 mg/mL
storage temp.
2-8°C
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
InChI key
NDEXUOWTGYUVGA-LJQANCHMSA-N
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-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.
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.
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
flash_point_f
Not applicable
flash_point_c
Not applicable