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经验公式(希尔记法):
C13H11N3O2
化学文摘社编号:
分子量:
241.25
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
InChI
1S/C13H11N3O2/c1-18-9-2-3-12-10(5-9)11(13(17)16-12)4-8-6-14-7-15-8/h2-7H,1H3,(H,14,15)(H,16,17)/b11-4-
SMILES string
COc1ccc2NC(=O)C(=C/c3cnc[nH]3)\c2c1
InChI key
QNUKRWAIZMBVCU-WCIBSUBMSA-N
assay
≥98% (HPLC)
form
crystalline
color
brown
solubility
DMSO: ~17 mg/mL, H2O: insoluble
Gene Information
human ... CDK2(1017), PDGFRB(5159), SRC(6714)
Application
Identified through a high-throughput screening with Cdk2. IC50=22 nM.
SU 9516 may be used to study cyclin-dependent kinase-2-dependent cell signaling.
Biochem/physiol Actions
3-substituted indoline cyclin-dependent kinase-2 (Cdk2) inhibitor. Induces apoptosis in colon carcinoma cells.
The apoptosis induced by SU 9516 in colon carcinoma cells involves dephosphorylation of pRb and cell cycle arrest in G1 or G2/M phase. In human leukemia cells, SU 9516 induces release of cytochrome c, Bax translocation and causes mitochondrial injury. It is being explored as an anti-cancer drug.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
新产品
此项目有
Ning Gao et al.
Molecular pharmacology, 70(2), 645-655 (2006-05-05)
Mechanisms of lethality of the three-substituted indolinone and putatively selective cyclin-dependent kinase (CDK)2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) were examined in human leukemia cells. Exposure of U937 and other leukemia cells to SU9516 concentrations > or =5 microM rapidly (i.e., within 4
Yufu Zhu et al.
Journal of cellular and molecular medicine, 21(11), 2685-2694 (2017-05-05)
SH3GL2 (Src homology 3 (SH3) domain GRB2-like 2) is mainly expressed in the central nervous system and regarded as a tumour suppressor in human glioma. However, the molecular mechanism of the SH3GL2 protein involved in malignant behaviours of human glioma
Tim Hunt
Cell cycle (Georgetown, Tex.), 7(24), 3789-3790 (2008-12-11)
Ever since it emerged that cyclin-dependent protein kinases catalyzed cell cycle transitions and with cancer seen as "a disease of the cell cycle," people have pursued the aim of testing kinase inhibitors as anti-cancer drugs. Quite early on, Laurent Meijer
Hengliang Shi et al.
Journal of cellular and molecular medicine, 18(10), 2061-2070 (2014-08-16)
Immunotherapy mediated by recombinant antibodies is an effective therapeutic strategy for a variety of cancers. In a previous study, we demonstrated that the fibroblast growth factor 1 (FGF-1)-specific recombinant antibody scFv1C9 arrests the cell cycle at the G0/G1 transition by
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