2. PI3K/Akt/mTOR
  3. PI3K
  4. AS-252424

AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.

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

AS-252424 Chemical Structure

AS-252424 Chemical Structure

CAS No. : 900515-16-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 4 publication(s) in Google Scholar

AS-252424 Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.

IC50 & Target[1]

PI3Kγ

30 nM (IC50)

PI3Kα

935 nM (IC50)

PI3Kδ

20 μM (IC50)

PI3Kβ

20 μM (IC50)

In Vitro

AS-252424 also inhibits PI3Kα, PI3Kβ and PI3Kδ with IC50s of 935±150 nM, 20 μM and 20 μM, respectively. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. In the human monocytic cell line THP-1, MCP-1 binding to the GPCR chemokine receptor CCR2, strongly induces phosphorylation of PKB/Akt, which is effectively inhibited by AS-252424 at IC50 values as low as 0.4 μM. In contrast, induction of PKB/Akt phosphorylation by colony stimulating factor (CSF-1), binding to the growth factor receptor c-fms, is only blocked by AS-252424 at IC50 values as high as 4.7 μM[1].

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

AS-252424 Related Antibodies
In Vivo

Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))[1].

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

305.28

Formula

C14H8FNO4S
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(NC/1=O)SC1=C/C2=CC=C(C3=CC=C(F)C=C3O)O2
Shipping

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

DMSO : 25 mg/mL (81.89 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 3.2757 mL 16.3784 mL 32.7568 mL
5 mM 0.6551 mL 3.2757 mL 6.5514 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.71%

SDS (393 KB)

COA (252 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

A PI3Kγ lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[γ33P]ATP and PtdIns. Kinase assays for IC50 value determinations with PI3Kα, PI3Kβ, and PI3Kδ are carried out[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

After 3 h of starvation in serum-free medium, Raw-264 macrophages are pretreated with inhibitors (e.g., AS-252424, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM and 100 μM) or DMSO for 30 min and stimulated for 5 min with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
PI3Kγ knockout (KO) mice are used. Oral administration of AS-252424 at 10 mg/kg is performed in PI3Kγ-deficient mice.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2757 mL 16.3784 mL 32.7568 mL 81.8920 mL
5 mM 0.6551 mL 3.2757 mL 6.5514 mL 16.3784 mL
10 mM 0.3276 mL 1.6378 mL 3.2757 mL 8.1892 mL
15 mM 0.2184 mL 1.0919 mL 2.1838 mL 5.4595 mL
20 mM 0.1638 mL 0.8189 mL 1.6378 mL 4.0946 mL
25 mM 0.1310 mL 0.6551 mL 1.3103 mL 3.2757 mL
30 mM 0.1092 mL 0.5459 mL 1.0919 mL 2.7297 mL
40 mM 0.0819 mL 0.4095 mL 0.8189 mL 2.0473 mL
50 mM 0.0655 mL 0.3276 mL 0.6551 mL 1.6378 mL
60 mM 0.0546 mL 0.2730 mL 0.5459 mL 1.3649 mL
80 mM 0.0409 mL 0.2047 mL 0.4095 mL 1.0237 mL
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AS-252424 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:

AS-252424900515-16-4AS252424AS 252424PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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