SML0083

GSK1059615 ナトリウム塩 水和物

• 別名: (5Z)-5-[[4-(4-ピリジニル)-6-キノリニル]メチレン]-2,4-チアゾリジンジオン ナトリウム塩 水和物
• 実験式（ヒル表記法）: C₁₈H₁₀N₃O₂S·Na · xH₂O
• CAS番号: 1356195-42-0
• 分子量: 355.35 (anhydrous basis)
• UNSPSCコード: 12352203
• PubChem Substance ID: 329825144
• NACRES: NA.44

特性

• フォーム: powder
• 色: yellow
• 溶解性: H₂O: ≥8 mg/mL
• オーガナイザー: GlaxoSmithKline
• 保管温度: 2-8°C
• SMILES記法: 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

詳細

生物化学的／生理学的作用

GSK 1059615はPI3キナーゼインヒビターです。

GSK 1059615は、PI3キナーゼの強力なインヒビターです。(IC₅₀ = 2 nM)

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]

特徴および利点

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.

免責事項

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.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable