PZ0186
PF-477736
≥98% (HPLC)
Synonym(s):
(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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About This Item
Empirical Formula (Hill Notation):
C22H25N7O2
CAS Number:
Molecular Weight:
419.48
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
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.
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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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)
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)
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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| PZ0186-25MG | 04061832449241 |
| PZ0186-5MG | 04061832449258 |