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表单
powder
颜色
yellow
溶解性
H2O: ≥8 mg/mL
创始人
GlaxoSmithKline
储存温度
2-8°C
SMILES字符串
O.[Na+].O=C1[N-]C(=O)C(\S1)=C\c2ccc3nccc(-c4ccncc4)c3c2
InChI
1S/C18H11N3O2S.Na.H2O/c22-17-16(24-18(23)21-17)10-11-1-2-15-14(9-11)13(5-8-20-15)12-3-6-19-7-4-12;;/h1-10H,(H,21,22,23);;1H2/q;+1;/p-1/b16-10-;;
InChI key
KKSRFFGUIONCPS-FLPKAINGSA-M
生化/生理作用
GSK 1059615 is a PI3 Kinase inhbitor
GSK 1059615 is a phosphatidylinositol-3-kinases (PI3K) inhibitor. GSK 1059615 inhibits proliferation of breast cancer BT474 cells via four different mechanisms that include retinoblastoma 1 (RB1)-mediated cell cycle arrest, elevated forkhead box protein O1 (FOXO) signaling, deduced MYC and transferrin receptor (TFRC) signaling and decreased cellular metabolism. Additionally, GSK 1059615 can suppress cell proliferation by decreasing mitogen-activated protein kinase (MAPK) signaling and imparts sensitivity to phosphoinositide 3-kinase (PI3K) inhibitor in cells resistant to the protein kinase B or AKT inhibitor.[1] GSK 1059615 functions as a druggable target to reduce radiation-induced apoptosis in NCCIT cells.[2] GSK 1059615 has entered clinical trial in patients with solid tumors or lymphoma and refractory malignancies.[3][4]
GSK 1059615 is a potent inhibitor of PI3 Kinase. (IC50 = 2 nM)
特点和优势
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
免责声明
Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Crystal D Zellefrow et al.
Radiation research, 178(3), 150-159 (2012-07-04)
Currently, there is a serious absence of pharmaceutically attractive small molecules that mitigate the lethal effects of an accidental or intentional public exposure to toxic doses of ionizing radiation. Moreover, cellular systems that emulate the radiobiologically relevant cell populations and
Pixu Liu et al.
Nature reviews. Drug discovery, 8(8), 627-644 (2009-08-01)
The phosphoinositide 3-kinase (PI3K) pathway is a key signal transduction system that links oncogenes and multiple receptor classes to many essential cellular functions, and is perhaps the most commonly activated signalling pathway in human cancer. This pathway therefore presents both
Causal Network? Modeling identifies common and unique mechanisms for sensitivity to the PI3K inhibitor GSK1059615 and the AKT inhibitor GSK690693
Macoritto M P
Molecular Cancer Therapeutics, 8(12 Suppl), 15-19 (2009)
Steven D Knight et al.
ACS medicinal chemistry letters, 1(1), 39-43 (2010-04-08)
Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancers. The mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, is also
商品
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
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