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PZ0186

Sigma-Aldrich

PF-477736

≥98% (HPLC)

Synonyme(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

Formule empirique (notation de Hill):
C22H25N7O2
Numéro CAS:
952021-60-2
Poids moléculaire :
419.48
Numéro MDL:
MFCD16038847
Code UNSPSC :
12352200
ID de substance PubChem :
329823760
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

yellow

Solubilité

DMSO: ≥20 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

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

Clé InChI

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.

Actions biochimiques/physiologiques

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.

Autres remarques

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.

Informations légales

Sold for research purposes under agreement from Pfizer Inc.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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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)
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
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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