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AS-604850 

Cat. No.: HY-13531 Purity: 99.91%
Handling Instructions

AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively.

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

AS-604850 Chemical Structure

AS-604850 Chemical Structure

CAS No. : 648449-76-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively[1].

IC50 & Target[1]

PI3Kγ

0.25 μM (IC50)

PI3Kγ

0.18 μM (Ki)

PI3Kα

4.5 μM (IC50)

In Vitro

AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC50 of 10 μM in RAW264 mouse macrophages[1].
AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg+/+ or Pik3cg–/– mice[1].
AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg+/+ mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg+/+ mice[1].

Western Blot Analysis[1]

Cell Line: Primary monocytes from Pik3cg+/+ mice
Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time: 15 minutes
Result: Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg+/+ mice.
In Vivo

AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment[1].

Animal Model: Balb/C or C3H mice with human recombinant RANTES or thioglycollate[1]
Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kg
Administration: Oral administration; for 4.5 or 4.25 hours
Result: Reduced RANTES-induced peritoneal neutrophil recruitment with an ED50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment.
Molecular Weight

285.22

Formula

C₁₁H₅F₂NO₄S

CAS No.

648449-76-7

SMILES

O=C(NC/1=O)SC1=C\C2=CC=C(OC(F)(F)O3)C3=C2

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 : 250 mg/mL (876.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5061 mL 17.5303 mL 35.0607 mL
5 mM 0.7012 mL 3.5061 mL 7.0121 mL
10 mM 0.3506 mL 1.7530 mL 3.5061 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 (7.29 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

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

AS-604850AS604850AS 604850PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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AS-604850
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HY-13531
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