4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]-
TGX-221
CAS: 663619-89-4
Molecular Formula: C21H24N4O2
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- - Names and Identifiers
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- - Physico-chemical Properties
| Molecular Formula | C21H24N4O2 |
| Molar Mass | 364.44 |
| Density | 1.25±0.1 g/cm3(Predicted) |
| Melting Point | 198-201oC |
| Boling Point | 557.3±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO, not in water |
| Appearance | Pale yellow solid. |
| Color | Off-White to Pale Yellow |
| pKa | 3.90±0.50(Predicted) |
| Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
| Use | TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit.TGX221 selectively inhibits renal cell carcinoma cells with both VHL and SETD2 mutations and links multiple pathways. TGX221 blocks xenograft tumor growth of prostate cancer in nude mice. TGX221 is a selective inhibitor for ccRCC with both VHL and SETD2 mutations. TGX221 also targeted cancer cells with CDKN2A and PTEN mutations. TGX221 also exhibited significant selectivity in inhibiting cell motility and tumourigenesis of ccRCC cells with VHL and SETD2 mutations. TGX221 is a novel inhibitor with high selectivity for ccRCC with VHL and SETD2 mutations. |
| Target | p110α : ic50 5μM p110β : ic50 5nM p110γ : ic50 >10μM p110δ : ic50 0.1μM |
| In vitro study | Using Recombinant p85/p110, an in vitro PI3K experiment was performed to determine the activity of TGX-221 acting on different subtypes, TGX-221 acting efficiently and highly selectively on p110β, on PI3K p110β and PI3K p110δ, the IC50 was 8.5 and 211 nM, respectively. Furthermore, TGX-221 acts on J774.2 macrophages to locally reduce insulin-induced phosphorylation of PKB at the Ser473 site. TGX-221 inhibits platelet-ECC interactions, platelet aggregation, and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. Recent studies have shown that treatment of PC3 cells with 0.2, 2, and 20 μm TGX-221 inhibits proliferation and significantly reduces the activity of the p110β PI3K subtype. |
| In vivo study | As an antithrombotic agent, the mouse model was treated with 1+1(49±13.9%) and 3+3(88±10.6%) doses in TGX-221, and the comprehensive blood flow was increased after 30 minutes. In addition, treatment with 3+3 (mean 1560) and 1+1 (1305) doses increased tail bleeding time (BT) and mean renal BT TGX-221. |
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- - Reference
| Reference Show more | 1: Feng C, Sun Y, Ding G, Wu Z, Jiang H, Wang L, Ding Q, Wen H. PI3Kβ inhibitor TGX221 selectively inhibits renal cell carcinoma cells with both VHL and SETD2 mutations and links multiple pathways. Sci Rep. 2015 Apr 8;5:9465. doi: 10.1038/srep09465. PubMed PMID: 25853938. 2: Chen R, Zhao Y, Huang Y, Yang Q, Zeng X, Jiang W, Liu J, Thrasher JB, Forrest ML, Li B. Nanomicellar TGX221 blocks xenograft tumor growth of prostate cancer in nude mice. Prostate. 2015 May;75(6):593-602. doi: 10.1002/pros.22941. Epub 2015 Jan 25. PubMed PMID: 25620467; PubMed Central PMCID: PMC4376584. 3: Ukhanov K, Corey EA, Ache BW. Phosphoinositide 3-kinase dependent inhibition as a broad basis for opponent coding in Mammalian olfactory receptor neurons. PLoS One. 2013 Apr 9;8(4):e61553. doi: 10.1371/journal.pone.0061553. Print 2013. PubMed PMID: 23585911; PubMed Central PMCID: PMC3621990. 4: Moir LM, Trian T, Ge Q, Shepherd PR, Burgess JK, Oliver BG, Black JL. Phosphatidylinositol 3-kinase isoform-specific effects in airway mesenchymal cell function. J Pharmacol Exp Ther. 2011 May;337(2):557-66. doi: 10.1124/jpet.110.173583. Epub 2011 Feb 24. PubMed PMID: 21349933. |
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.744 ml | 13.719 ml | 27.439 ml |
| 5 mM | 0.549 ml | 2.744 ml | 5.488 ml |
| 10 mM | 0.274 ml | 1.372 ml | 2.744 ml |
| 5 mM | 0.055 ml | 0.274 ml | 0.549 ml |
Last Update：2024-01-02 23:10:35
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- - Cell Experiment
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.(Only for Reference) Cell lines: PC3 cells
Last Update：2023-08-16 21:32:38
4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE, 7-METHYL-2-(4-MORPHOLINYL)-9-[1-(PHENYLAMINO)ETHYL]- - Reference Information
| biological activity | TGX-221 is a p110β-specific inhibitor. in cell-free test, IC50 is 5 nM, and the selectivity to p110β is 1000 times that to p110α. |
| target | TargetValue p110β (cell-free say) 5 nM p110δ (cell-free say) 0.1 μM |
| Target | Value |
| p110β (Cell-free assay) | 5 nM |
| p110δ (Cell-free assay) | <0.1 μM |
| in vitro study | using recombinant p85/p110, in vitro PI3K experiment was carried out to determine the activity of TGX-221 acting on different subtypes, TGX-221 effective and highly selective p110β, when acting on PI3K p110β and PI3K p110δ, IC50 is 8.5 and 211 nM respectively. Moreover, TGX-221 acts on J774.2 macrophages to locally reduce insulin-induced phosphorylation of PKB at Ser473 site. TGX-221 acts on cardiopulmonary bypass (ECC) model, inhibiting platelet-ECC interaction, platelet aggregation, and platelet-granulocyte binding. The latest research shows that PC3 cells were treated with 0.2, 2, and 20 μM TGX-221, which inhibited proliferation and significantly reduced the activity of p110β PI3K subtype. |
| in vivo study | as an antithrombotic agent, the mouse model was TGX-221 treated at doses of 1+1(49±13.9%) and 3+3(88±10.6%), and after 30 minutes, the comprehensive blood flow was increased. In addition, TGX-221 were treated with 3+3 (mean 1560) and 1+1 (1305) doses to improve tail bleeding time (BT) and average renal BT. |
Last Update：2024-04-09 19:05:03
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Spot supply
Product Name: TGX-221 Visit Supplier Webpage Request for quotationCAS: 663619-89-4
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: TGX-221 Visit Supplier Webpage Request for quotationCAS: 663619-89-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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