Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
AS041164 is a novel and potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM).
Targets |
PI3Kγ (IC50 = 70 nM); PI3Kα (IC50 = 240 nM); PI3Kβ (IC50 = 1.4 μM); PI3Kδ (IC50 = 1.7 μM)
|
---|---|
ln Vivo |
AS-041164 (10-100 mg/kg; oral administration; once) treatment results in the reduction of inflammatory swelling in the model of carrageenan-induced paw edema[1].
Treatment with AS-041164 (3-100 mg/kg p.o.) reduces RANTES-induced neutrophil recruitment in mice in a dose-dependent manner. As for AS-041164, the ED50 value is 27.35 mg/kg. AKT phosphorylation is decreased and chemotaxis caused by RANTES is blocked by AS-041164[1].
|
Animal Protocol |
Male Wistar rats (100-150 g) injected with carrageenan[1]
10 mg/kg, 30 mg/kg, 100 mg/kg Oral administration; once |
References |
Molecular Formula |
C11H7NO4S
|
---|---|
Molecular Weight |
249.24258
|
Exact Mass |
249.009
|
CAS # |
6318-41-8
|
Related CAS # |
6318-41-8
|
PubChem CID |
1269519
|
Appearance |
Light yellow to yellow solid
|
Density |
1.6±0.1 g/cm3
|
Index of Refraction |
1.731
|
LogP |
2.46
|
Hydrogen Bond Donor Count |
1
|
Hydrogen Bond Acceptor Count |
5
|
Rotatable Bond Count |
1
|
Heavy Atom Count |
17
|
Complexity |
395
|
Defined Atom Stereocenter Count |
0
|
SMILES |
O=C1NC(=O)/C(=C/C2C=CC3OCOC=3C=2)/S1
|
InChi Key |
SDGWAUUPHUBJNQ-RUDMXATFSA-N
|
InChi Code |
InChI=1S/C11H7NO4S/c13-10-9(17-11(14)12-10)4-6-1-2-7-8(3-6)16-5-15-7/h1-4H,5H2,(H,12,13,14)/b9-4+
|
Chemical Name |
(5E)-5-(1,3-benzodioxol-5-ylmethylidene)-1,3-thiazolidine-2,4-dione
|
Synonyms |
AS041164
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: ~125 mg/mL (~501.52 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.47 mg/mL (5.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0122 mL | 20.0610 mL | 40.1220 mL | |
5 mM | 0.8024 mL | 4.0122 mL | 8.0244 mL | |
10 mM | 0.4012 mL | 2.0061 mL | 4.0122 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.