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  3. TASP0415914

TASP0415914 

Cat. No.: HY-120438
Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 330 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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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)

Akt

294 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].

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

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].

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.
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)

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
10 mM 0.3092 mL 1.5462 mL 3.0924 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

TASP0415914TASP 0415914TASP-0415914PI3KAktPhosphoinositide 3-kinasePKBProtein kinase BPI3KγinflammatoryautoimmuneoralmetabolicstabilityInhibitorinhibitorinhibit

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TASP0415914
Cat. No.:
HY-120438
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