2. PI3K/Akt/mTOR
  3. PI3K Akt
  4. TASP0415914

TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research.

For research use only. We do not sell to patients.

TASP0415914 Chemical Structure

TASP0415914 Chemical Structure

CAS No. : 1292300-75-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 In-stock
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Solid
5 mg USD 250 In-stock
10 mg USD 400 In-stock
25 mg USD 670 In-stock
50 mg USD 950 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

TASP0415914 Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research[1].

IC50 & Target[1]

PI3Kγ

29 nM (IC50)

In Vitro

TASP0415914 (compound 8j) shows high metabolic stability in rat/human liver microsomes. TASP0415914 has no CYP inhibition up to 10 μM for CYP1A2, 2C9, 2C19, 2D6 and 3A4[1].

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

TASP0415914 Related Antibodies
In Vivo

TASP0415914 (compound 8j; 10-100 mg/kg; orally administration; twice daily; for 14 days) treatment suppressed the progression of the disease in a dose-dependent manner in a mouse collagen-induced arthritis (CIA) model[1].

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

Animal Model: Collagen-primed DBA/1 mice[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: Orally administration; twice daily; for 14 days
Result: Suppressed the progression of the disease in a dose-dependent manner.
Molecular Weight

323.37

Formula

C13H17N5O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(NC1=NC(C)=C(C2=NC(N3CC(O)CCC3)=NO2)S1)=O
Shipping

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

DMSO : 125 mg/mL (386.55 mM; Need ultrasonic; 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 3.0924 mL 15.4622 mL 30.9243 mL
5 mM 0.6185 mL 3.0924 mL 6.1849 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 2.08 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0924 mL 15.4622 mL 30.9243 mL 77.3108 mL
5 mM 0.6185 mL 3.0924 mL 6.1849 mL 15.4622 mL
10 mM 0.3092 mL 1.5462 mL 3.0924 mL 7.7311 mL
15 mM 0.2062 mL 1.0308 mL 2.0616 mL 5.1541 mL
20 mM 0.1546 mL 0.7731 mL 1.5462 mL 3.8655 mL
25 mM 0.1237 mL 0.6185 mL 1.2370 mL 3.0924 mL
30 mM 0.1031 mL 0.5154 mL 1.0308 mL 2.5770 mL
40 mM 0.0773 mL 0.3866 mL 0.7731 mL 1.9328 mL
50 mM 0.0618 mL 0.3092 mL 0.6185 mL 1.5462 mL
60 mM 0.0515 mL 0.2577 mL 0.5154 mL 1.2885 mL
80 mM 0.0387 mL 0.1933 mL 0.3866 mL 0.9664 mL
100 mM 0.0309 mL 0.1546 mL 0.3092 mL 0.7731 mL
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TASP0415914 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:

TASP04159141292300-75-4TASP 0415914TASP-0415914PI3KAktPhosphoinositide 3-kinasePKBProtein kinase BPI3KγinflammatoryautoimmuneoralmetabolicstabilityInhibitorinhibitorinhibit

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