Cabotegravir (GSK1265744)

製品コードS7766 バッチS776601

印刷

化学情報

Chemical Structure Synonyms GSK744, S/GSK1265744 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H17F2N3O5
分子量 405.35 CAS No. 1051375-10-0
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 38 mg/mL (93.74 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 Cabotegravir (GSK744, GSK1265744, S/GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.
in vitro Cabotegravir (GSK1265744) inhibits HIV replication with EC50 of 0.22 nM and 0.34-1.3 nM against HIV-1 Ba-L and NL432, respectively. It produces cytotoxicity with CC50 of 6.4, 5.0, 9.2, and 13 μM in proliferating IM-9, U-937, MT-4, and Molt-4 cell lines, respectively. [1]
in vivo Cabotegravir (GSK1265744) (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges. [2]

プロトコル(参考用のみ)

キナーゼアッセイ In vitro strand transfer assay
The inhibitory concentrations of Cabotegravir (GSK1265744) are measured in a strand transfer assay using recombinant HIV IN. A complex of integrase and biotinylated donor DNA–streptavidin-coated SPA beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA–4 mg/mL streptavidin-coated SPA beads in 25 mM sodium MOPS pH 7.2, 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37°C. These beads are spun down and preincubated with diluted INSTIs for 60 minutes at 37°C. Next, [3H]-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction is incubated at 37°C for 25 to 45 minutes, which allowed for a linear increase in strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
細胞アッセイ 細胞株 Human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4)
濃度 ~20 μM
反応時間 --
実験の流れ

In vitro growth inhibition (cytotoxicity) studies are conducted with Cabotegravir (GSK1265744) in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as stimulated and unstimulated human PBMCs. As a surrogate of cell growth, ATP levels are quantified using CellTiter-Glo luciferase reagent.
動物実験 動物モデル Rhesus macaques
投薬量 50 mg/kg
投与方法 --

参考

  • https://pubmed.ncbi.nlm.nih.gov/25367908/
  • https://pubmed.ncbi.nlm.nih.gov/25589630/

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：

Interactive effects of morphine and the HIV integrase inhibitor, cabotegravir, in male and female mice [ Biomed Pharmacother, 2025, 184:117925] PubMed: 39999644
An effective two-stage NMBzA-induced rat esophageal tumor model revealing that the FAT-Hippo-YAP1 axis drives the progression of ESCC [ Cancer Lett, 2024, 588:216813] PubMed: 38499266
Ultra-long-acting in-situ forming implants with cabotegravir protect female macaques against rectal SHIV infection [ Nat Commun, 2023, 14(1):708] PubMed: 36759645
Dose-Ranging Plasma and Genital Tissue Pharmacokinetics and Biodegradation of Ultra-Long-Acting Cabotegravir In Situ Forming Implant [ Pharmaceutics, 2023, 15(5)1487] PubMed: 37242729
Dose-Ranging Plasma and Genital Tissue Pharmacokinetics and Biodegradation of Ultra-Long-Acting Cabotegravir In Situ Forming Implant [ Pharmaceutics, 2023, 15(5)1487] PubMed: 37242729
Long-Acting Technologies for Prevention of HIV and Unplanned Pregnancy [ ProQuest, 2023, 30314559] PubMed: none
Virus-Mimicking Polymer Nanoparticles Targeting CD169+ Macrophages as Long-Acting Nanocarriers for Combination Antiretrovirals [ ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c17415] PubMed: 34995059
Impact of combinations of clinically observed HIV integrase mutations on phenotypic resistance to integrase strand transfer inhibitors (INSTIs): a molecular study [ J Antimicrob Chemother, 2022, dkab498] PubMed: 35061879
Female Genital Fibroblasts Diminish the In Vitro Efficacy of PrEP against HIV [ Viruses, 2022, 14(8)1723] PubMed: 36016345
Drug Interactions in Lenacapavir-Based Long-Acting Antiviral Combinations [ Viruses, 2022, 14(6)1202] PubMed: 35746673

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。

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