TGX-221

製品コードS1169 バッチS116901

印刷

化学情報

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

C21H24N4O2
分子量 364.44 CAS No. 663619-89-4
Solubility (25°C)* 体外 DMSO 12 mg/mL (32.92 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 TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
in vitro The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. This compound shows slow potent to p110δ with IC50 of 211 nM. Furthermore, it partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. [1] This chemical inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. [2] A recent study shows that after treatment with this compound (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. [3]
in vivo As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with this compound at doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Lipid kinase activity
IC50 values are measured using a standard lipid kinase activity with PI as a substrate. (i)100 μM cold ATP is used instead of 10 μM, (ii) the DMSO concentration is 1%, and (iii) [γ-33P]ATP is used instead of [γ-32P]ATP. The TLC plates are quantified using a phosphorimager screen. The reported IC50 values are determined by non-linear regression analysis on the basis of at least three independent experiments repeated across multiple preparations of recombinant protein.
細胞アッセイ 細胞株 PC3 cells
濃度 ~20 μM
反応時間 24-72 hours
実験の流れ For measurement of proliferation, cells are seeded in triplicate in 96-well culture plates and incubated overnight to allow cell attachment. The cells are incubated with TGX-221 for 24, 48, and 72 hours. At designated time intervals, cells are quantified by a crystal violet staining-based colorimetric assay. Briefly, cells are fixed by addition of 100 μl of 2.5% glutaraldehyde solution and incubated at room temperature for 30 minutes. Plates are washed three times by submersion in PBS solution. Plates are air-dried and stained by addition of 100 μL of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 minutes at room temperature, excess dye is removed by extensive washing with deionized water, and plates are air-dried prior to bound dye solubilization in 100 μL of 10% acetic acid. The optical density of dye extracts is measured directly in plates using a microplate reader at 570 nm.
動物実験 動物モデル FeCl3-induced arterial thrombosis in mice
投薬量 0.3 + 0.3, 1 + 1, 3 + 3 mg/kg + mg/kg/hour
投与方法 Administered via i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17362206/
  • https://pubmed.ncbi.nlm.nih.gov/18327411/
  • https://pubmed.ncbi.nlm.nih.gov/21286711/
  • https://pubmed.ncbi.nlm.nih.gov/21396684/
  • https://pubmed.ncbi.nlm.nih.gov/15834429/

カスタマーフィードバック

Data from [Mol Med, 2012, 18, 336-45]

Data from [Mol Med, 2012, 18, 336-45]

Data from [Mol Med, 2012, 18, 336-45]

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：

hnRNPL phase separation activates PIK3CB transcription and promotes glycolysis in ovarian cancer [ Nat Commun, 2025, 16(1):4828] PubMed: 40413189
PI3K-dependent GAB1/Erk phosphorylation renders head and neck squamous cell carcinoma sensitive to PI3Kα inhibitors [ Cell Death Dis, 2025, 16(1):457] PubMed: 40533463
Role and Therapeutic Potential of miR-301b-3p in Regulating the PI3K-AKT Pathway via PIK3CB in Eosinophilic Chronic Rhinosinusitis [ J Inflamm Res, 2025, 18:10235-10251] PubMed: 40756418
Development of Acquired Resistance in Alpelisib-treated Gastric Cancer Cells With PIK3CA Mutations and Overcoming Strategies [ Anticancer Res, 2025, 45(5):1877-1896] PubMed: 40295072
Integration of 3D bioprinting and multi-algorithm machine learning identified glioma susceptibilities and microenvironment characteristics [ Cell Discov, 2024, 10(1):39] PubMed: 38594259
Microglia degrade Alzheimer's amyloid-beta deposits extracellularly via digestive exophagy [ Cell Rep, 2024, 43(12):115052] PubMed: 39644493
WWP1 inhibition suppresses the proliferation of pancreatic cancer cells by regulating the PI3K-AKT pathway [ J Gastroenterol, 2024, 10.1007/s00535-024-02192-x] PubMed: 39656237
Machine learning-based identification of lower grade glioma stemness subtypes discriminates patient prognosis and drug response [ Comput Struct Biotechnol J, 2023, 21:3827-3840] PubMed: 37560125
Machine learning-based identification of lower grade glioma stemness subtypes discriminates patient prognosis and drug response [ Comput Struct Biotechnol J, 2023, 21:3827-3840] PubMed: 37560125
Pan-PI3K inhibition with copanlisib overcomes Treg- and M2-TAM-mediated immune suppression and promotes anti-tumor immune responses [ Clin Exp Med, 2023, 10.1007/s10238-023-01227-6] PubMed: 37935952

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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