1. PI3K/Akt/mTOR
  2. PI3K

TGX-221 

Cat. No.: HY-10114 Purity: 99.78%
Handling Instructions

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

For research use only. We do not sell to patients.
TGX-221 Chemical Structure

TGX-221 Chemical Structure

CAS No. : 663619-89-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 420 In-stock
100 mg USD 660 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

IC50 & Target[5]

p110β

8.5 nM (IC50)

p110δ

211 nM (IC50)

In Vitro

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].

In Vivo

TGX-221 (TGX221, 2.5 mg/kg i.v.) abolishes cyclic flow reductions in a Folts-like carotid artery stenosis preparation of thrombosis, without changing bleeding time, heart rate, blood pressure or carotid vascular conductance[4].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.7439 mL 13.7197 mL 27.4394 mL
5 mM 0.5488 mL 2.7439 mL 5.4879 mL
10 mM 0.2744 mL 1.3720 mL 2.7439 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

TGX-221 is formulated in vehicle propylene glycol.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

364.44

Formula

C₂₁H₂₄N₄O₂

CAS No.

663619-89-4

SMILES

O=C1N2C(C(C(NC3=CC=CC=C3)C)=CC(C)=C2)=NC(N4CCOCC4)=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.78%

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TGX-221
Cat. No.:
HY-10114
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