PZ0186
PF-477736
≥98% (HPLC)
동의어(들):
(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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모든 사진(2)
About This Item
실험식(Hill 표기법):
C22H25N7O2
CAS Number:
Molecular Weight:
419.48
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
양식
powder
색상
yellow
solubility
DMSO: ≥20 mg/mL
저장 온도
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
애플리케이션
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.
생화학적/생리학적 작용
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)
기타 정보
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.
법적 정보
Sold for research purposes under agreement from Pfizer Inc.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
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)
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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