2. PI3K/Akt/mTOR
  3. PI3K
  4. TGX-221

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 75 In-stock
Solution
10 mM * 1 mL in DMSO USD 75 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 69 In-stock
10 mg USD 117 In-stock
25 mg USD 245 In-stock
50 mg USD 393 In-stock
100 mg USD 590 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 16 publication(s) in Google Scholar

TGX-221 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

TGX-221 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

364.44

Formula

C21H24N4O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.74%

COA (252 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
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]

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

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
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TGX-221 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGX-221663619-89-4TGX221TGX 221PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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