TGX-221
Based on 18 publication(s) in Google Scholar
TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.45%
- CAS. Nr.: 663619-89-4
- Formel: C21H24N4O2
- Molecular Weight:364.44
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) TGX-221
More- Nat Commun. 2024 Dec 3;15(1):10499. [Abstract]
- Nat Commun. 2024 Aug 21;15(1):7181. [Abstract]
- Mol Cell. 2025 Mar 19:S1097-2765(25)00186-8. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2021 Dec 15;131(24):e140436. [Abstract]
- Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
- Cell Rep. 2025 Feb 5;44(2):115246. [Abstract]
- Cell Rep. 2024 Apr 23;43(5):114132. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Cell Biosci. 2022 Dec 30;12(1):210. [Abstract]
- EMBO Rep. 2020 Dec 3;21(12):e49756. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- J Biol Chem. 2020 May 22;295(21):7431-7441. [Abstract]
- Platelets. 2024 Dec;35(1):2288679. [Abstract]
- bioRxiv. 2026 May 12:2026.05.08.723799. [Abstract]
- bioRxiv. 2024 July 07.
- bioRxiv. 2023 Dec 26.
- Research Square Preprint. 2023 Oct 17.
Biologische Aktivität
|
p110β 8.5 nM (IC50) |
p110δ 211 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
10 nM
Compound: TGX-221
|
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay
|
[PMID: 22524426] |
| PC-3 | IC50 |
10 nM
Compound: TGX-221
|
Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
|
[PMID: 22524426] |
| PC-3 | IC50 |
3 nM
Compound: TGX-221
|
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
|
[PMID: 22524426] |
| PC-3 | IC50 |
10 nM
Compound: TGX-221
|
Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay
Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay
|
[PMID: 24387221] |
| RAW264.7 | IC50 |
>1000 nM
Compound: TGX-221
|
Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis
Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis
|
[PMID: 22524426] |
| Sf21 | IC50 |
30 nM
Compound: TGX-221
|
Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
|
[PMID: 24387221] |
| Sf21 | IC50 |
52 nM
Compound: TGX-221
|
Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay
Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay
|
[PMID: 27387421] |
| Sf21 | IC50 |
63 nM
Compound: TGX-221
|
Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration
Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration
|
[PMID: 32551006] |
| Sf9 | IC50 |
>10000 nM
Compound: TGX-221
|
Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
|
[PMID: 22524426] |
| Sf9 | IC50 |
851 nM
Compound: TGX-221
|
Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
|
[PMID: 22524426] |
| Sf9 | IC50 |
>10000 nM
Compound: TGX-221
|
Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
|
[PMID: 22524426] |
| Sf9 | IC50 |
10000 nM
Compound: TGX-221
|
Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
|
[PMID: 24387221] |
| Sf9 | IC50 |
851 nM
Compound: TGX-221
|
Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
|
[PMID: 24387221] |
| Sf9 | IC50 |
10 μM
Compound: TGX-221
|
Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay
|
[PMID: 24387221] |
| Sf9 | IC50 |
0.004 μM
Compound: 1a, TGX-221
|
Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
|
[PMID: 25890698] |
| Sf9 | IC50 |
0.14 μM
Compound: 1a, TGX-221
|
Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
|
[PMID: 25890698] |
| Sf9 | IC50 |
1 μM
Compound: 1a, TGX-221
|
Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay
|
[PMID: 25890698] |
TGX-221, BL05 and BL05-HA show selective cytotoxicity to LNCaP cells, which may be due to the deficiency of PTEN in this cell line and the accumulation of PIP3 in the cells[1].
TGX-221 (1 μM) does not affect the expression and phosphorylation of AMPK in C2C12 myoblasts[2].
TGX221 (0.1, 1, 10 μM) induces IL-6 release from ASM cells[2].
TGX-221 does not affect neurotensin-stimulated Akt phosphorylation when used alone, but it further suppresses neurotensin-stimulated phosphorylation of Akt when combined with gefitinib. TGX-221 abolishes the neurotensin-stimulated phosphorylation of Akt in Panc-1 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 663619-89-4
-
Appearance Solid
-
Molecular Weight 364.44
-
Formel C21H24N4O2
-
Color White to yellow
-
SMILES
O=C1N2C(C(C(NC3=CC=CC=C3)C)=CC(C)=C2)=NC(N4CCOCC4)=C1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (18)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Fast-diffusing receptor collisions with slow-diffusing peptide ligand assemble the ternary parathyroid hormone-GPCR-arrestin complex. [Abstract]2024 Dec 3;15(1):10499. PMID: 39627206 -
Nat Commun
A class I PI3K signalling network regulates primary cilia disassembly in normal physiology and disease. [Abstract]2024 Aug 21;15(1):7181. PMID: 39168978 -
Mol Cell
PI3Kβ functions as a protein kinase to promote cellular protein O-GlcNAcylation and acetyl-CoA production for tumor growth. [Abstract]2025 Mar 19:S1097-2765(25)00186-8. PMID: 40132583 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Clin Invest
WWP1 inactivation enhances efficacy of PI3K inhibitors while suppressing their toxicities in breast cancer models. [Abstract]2021 Dec 15;131(24):e140436. PMID: 34907909 -
Adv Sci (Weinh)
TRIM24 Cooperates with Ras Mutation to Drive Glioma Progression through snoRNA Recruitment of PHAX and DNA-PKcs. [Abstract]2024 Jun 3:e2400023. PMID: 38828688 -
Cell Rep
Meteorin-like alleviates hepatic steatosis by regulating hepatic triglyceride secretion and fatty acid oxidation. [Abstract]2025 Feb 5;44(2):115246. PMID: 39918960 -
Cell Rep
Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. [Abstract]2024 Apr 23;43(5):114132. PMID: 38656871 -
Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693 -
Cell Biosci
Inhibition of PI3 kinase isoform p110α suppresses neuroblastoma growth and induces the reduction of Anaplastic Lymphoma Kinase. [Abstract]2022 Dec 30;12(1):210. PMID: 36585695 -
EMBO Rep
2020 Dec 3;21(12):e49756. PMID: 33159421 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
J Biol Chem
The mTOR inhibitor manassantin B reveals a crucial role of mTORC2 signaling in Epstein-Barr virus reactivation. [Abstract]2020 May 22;295(21):7431-7441. PMID: 32312752 -
Platelets
2024 Dec;35(1):2288679. PMID: 38099316 -
bioRxiv
2026 May 12:2026.05.08.723799. PMID: 42182142 -
-
-
Lösungsmittel & Löslichkeit
DMSO : 12.5 mg/mL (34.30 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.43 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.43 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
The prostate cancer cell lines DU145 and LNCaP are maintained in RPMI-1640 medium, and PC3 cells are maintained in F-12K medium. LNCaP is a PSMA positive cell line, whereas DU145 and PC3 are PSMA negative. Both are supplemented with 10 % fetal bovine serum. Cells are plated in 96-well flat-bottomed plates at a concentration of 5,000 cells per well in 90 μL of growth medium. After 12 h, TGX-221, BL05, or BL05-HA loaded micelles in PBS are added at concentrations of 0, 0.1, 1, 5, 10, 50 or 100 μM. PBS and 10 μL of trichloroacetic acid (TCA) are added to negative and positive control wells, respectively. After 72 h, 10 μL of 55-μM resazurin blue is added to each well and incubated at 37°C for 4 h. After incubation, the resorufin product is measured with a fluorophotometer using an excitation wavelength of 560 nm and an emission wavelength of 590 nm. The IC50 is determined as the midpoint between positive and negative control groups for each plate using GraphPad Prism 5 software.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats are randomLy assigned to drug treatment groups consisting of the vehicle propylene glycol (0.25 mL/kg), LY294002 (2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one; a reversible non-specific PI3K inhibitor; 10 mg/kg), wortmannin (an irreversible non-specific PI3K inhibitor; 5 mg/kg), IC87114 (2-[(6-aminopurin- 9-yl)methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one; a PI3K p110δ antagonist; 2.5 mg/kg) and the selective PI3K p110β antagonist TGX221 (2.5 mg/kg). In the tail bleeding experiments, rats are randomLy assigned to drug treatment groups consisting of LY294002 (10 mg/kg), IC87114 (2.5 mg/kg), wortmannin (5 mg/kg), TGX221 (2.5 or 25 mg/kg), heparin (100 U/kg), aspirin (2× 200 mg/kg p.o.)± heparin (100 U/kg), and aspirin (2× 200 mg/kg p.o.) combined with heparin (100 U/kg) and TGX221 (2.5 mg/kg). All drugs, with the exception of aspirin, are administered as a slow (over ≈45-60 s) i.v. bolus of 0.25 mL/kg into the jugular vein. Aspirin (200 mg/kg suspended in 15% gum arabic in water) is administered twice orally (p.o.)-the first dose is given 24 h before the experiment and the second dose 1 h before the start of the experiment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (284 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Zhao Y, et al. Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells. Mol Pharm. 2012 Jun 4;9(6):1705-16. [Content Brief]
[2]. Sturgeon SA, et al. Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat. Eur J Pharmacol. 2008 Jun 10;587(1-3):209-15. [Content Brief]
[3]. Ge Q, et al. The phosphoinositide 3'-kinase p110δ modulates contractile protein production and IL-6 release in human airway smooth muscle. J Cell Physiol. 2012 Aug;227(8):3044-52. [Content Brief]
[4]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Content Brief]
[5]. Müller KM, et al. Role of protein kinase C and epidermal growth factor receptor signalling in growth stimulation by neurotensin in colon carcinoma cells. BMC Cancer. 2011 Oct 2;11:421. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7439 mL | 13.7197 mL | 27.4394 mL | 68.5984 mL |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL | 13.7197 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7439 mL | 6.8598 mL | |
| 15 mM | 0.1829 mL | 0.9146 mL | 1.8293 mL | 4.5732 mL | |
| 20 mM | 0.1372 mL | 0.6860 mL | 1.3720 mL | 3.4299 mL | |
| 25 mM | 0.1098 mL | 0.5488 mL | 1.0976 mL | 2.7439 mL | |
| 30 mM | 0.0915 mL | 0.4573 mL | 0.9146 mL | 2.2866 mL |