Pemrametostat (GSK3326595)

製品コードS8664 バッチS866401

印刷

化学情報

Chemical Structure Synonyms EPZ015938 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H32N6O3
分子量 452.55 CAS No. 1616392-22-3
Solubility (25°C)* 体外 DMSO 90 mg/mL (198.87 mM)
Ethanol 90 mg/mL (198.87 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
in vitro

Both GSK3326595 and Santacruzamate A treatments rescue the ZEB2-mediated E-cadherin promoter suppression in SW480-ZEB2 cells, confirming that the ZEB2-mediated repression of E-cadherin in CRC cells is facilitated by PRMT5 and HDAC2.[2]
in vivo

GSK3326595 reduces liver metastasis of CRC cells and completely inhibits the distant metastasis of SW620 cells in nude mice.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SW480 cells
濃度 100, 250, 500 nM
反応時間 48 h
実験の流れ

SW480+Vector and SW480+ZEB2 cells express plasmid pGL3-E-cadherin promoter-Luc. InPRMT5 (GSK3326595) and inHDAC2 (Santacruzamate A) were added to the cell medium, and luciferase activity was assayed, 48 h later, luciferase activity was assayed and normalized to Renilla. (E) SW620 cells express plasmid pGL3-E-cadherin promoter-Luc. InPRMT5 (GSK3326595) and inHDAC2 (Santacruzamate A) were added to the medium, and luciferase activity was assayed, 48 h later, luciferase activity was assayed and normalized to Renilla.

(Data sourced from selleck products)
動物実験 動物モデル Female BALB/c nude mice injected with SW620
投薬量 100 mg/kg
投与方法 i.v.

(Data sourced from selleck products)

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52] PubMed: 38413740
Metabolic rewiring induced by ranolazine improves melanoma responses to targeted therapy and immunotherapy [ Nat Metab, 2023, 10.1038/s42255-023-00861-4] PubMed: 37563469
Metabolic rewiring induced by ranolazine improves melanoma responses to targeted therapy and immunotherapy [ Nat Metab, 2023, 5(9):1544-1562] PubMed: 37563469
MST2 methylation by PRMT5 inhibits Hippo signaling and promotes pancreatic cancer progression [ EMBO J, 2023, e114558.] PubMed: 37905571
PRMT5 reduces immunotherapy efficacy in triple-negative breast cancer by methylating KEAP1 and inhibiting ferroptosis [ J Immunother Cancer, 2023, 11(6)e006890] PubMed: 37380368
PRMT5 triggers glucocorticoid-induced cell migration in triple-negative breast cancer [ Life Sci Alliance, 2023, 6(10)e202302009] PubMed: 37536978
PRMT5/FGFR3/AKT Signaling Axis Facilitates Lung Cancer Cell Metastasis [ Technology in Cancer Research & Treatment, 2023, 10.1177/15330338231161139] PubMed: None
PRMT5/FGFR3/AKT Signaling Axis Facilitates Lung Cancer Cell Metastasis [ Technol Cancer Res Treat, 2023, 22:15330338231161139] PubMed: 36927233
Ribosome subunit attrition and activation of the p53-MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition [ bioRxiv, 2023, 2023.07.26.550648] PubMed: 37546802
Ribosome subunit attrition and activation of the p53-MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition [ bioRxiv, 2023, 2023.07.26.550648] PubMed: 37546802

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。