CAY10505

CAY10505 is a PI3Kγ inhibitor with IC50 of 30 nM.

Catalog No.S2682
4.5 5 1 Reviews
Price Stock Quantity  
USD 50 In stock
USD 100 In stock
USD 170 In stock
USD 470 In stock

Free Overnight Delivery on all orders over $ 500.

Order now and get it on

CAY10505 Chemical Structure

CAY10505 Chemical Structure
Molecular Weight: 289.28

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

CAY10505 is available in the following compound libraries:

Product Information

  • Compare PI3K Inhibitors
    Compare PI3K Inhibitors
  • Research Area

Product Description

Biological Activity

Description CAY10505 is a PI3Kγ inhibitor with IC50 of 30 nM.
Targets PI3Kγ PI3Kα PI3Kβ PI3Kδ
IC50 30 nM 0.94 μM 20 μM 20 μM [1]
In vitro CAY10505 selectively inhibits PI3Kγ isoform, with an IC50 of 30 nM better than the PI3Kα, β, and δ isoforms, with IC50 of 0.94, 20 and 20 μM, respectively. Tested against a panel of 80 other kinases including casein kinase 2, CAY10505 significantly inhibits only the unrelated casein kinase 2 (CK20) with an IC50 of 20 nM. CAY10505 also inhibits the phosphorylation of the PI3K substrate PKB/Akt in mouse macrophages with an IC50 of 228 nM. CAY10505 inhibits C5a-mediated PKB/Akt phosphorylation in Raw-264 macrophages, with an IC50 of 0.23 nM. In 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 26 at IC50 values as low as 0.4 μM. CAY10505 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 of 53 μM. [1]
In vivo Oral administration of CAY10505 at 10 mg/kg results in moderate reduction of neutrophil recruitment by 35%, almost matching the result observed in PI3Kγ-deficient mice. [1] Five weeks of deoxycorticosterone acetate salt (DOCA) administration are followed by 7 days of daily administration of PI3Kγ inhibitor CAY10505 at a dose of 0.6 mg/kg (p.o.), which significantly improves acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. [2]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: [1]

PI3Kγ lipid kinase assay 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 as substrates. Kinase assays for IC50 value determinations of CAY10505 with PI3Kα, PI3Kβ, and PI3Kδ are carried out.

Cell Assay: [1]

Cell lines Bone marrow cells
Concentrations ~10 mM
Incubation Time 3 hours
Method Bone marrow cells are isolated, prepared, and stimulated. For in vitro chemotaxis, 107 5-day-derived BMDMs are suspended in 1 mL of medium containing 0.5% BSA and CAY10505 or DMSO and applied to the upper chamber of a transwell, 5 μm pore size, chemotaxis plate. An amount of 600 μL of medium containing MCP-1/CCL2 and inhibitors or DMSO is added to the lower chamber. After 3 hours of incubation at 37 °C and 5% CO2, the number of cells in the lower chamber is quantified with a Coulter.

Animal Study: [2]

Animal Models Wistar albino rats
Formulation
Dosages 0.6 mg/kg
Administration Administered via p.o.
1

References

Chemical Information

Download CAY10505 SDF
Molecular Weight (MW) 289.28
Formula

C14H8FNO3S

CAS No. 1218777-13-9
Synonyms N/A
Solubility (25°C)
  • DMSO 58 mg/mL
  • Water <1 mg/mL
  • Ethanol <1 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name (E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione

Research Area

Customer Reviews (1)


Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. CAY10505 purchased from Selleck
Method
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 3 h
Results

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related PI3K Inhibitors

  • BEZ235 (NVP-BEZ235)

    BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.

  • PI-103

    PI-103 is a potent, ATP-competitive PI3K inhibitor of DNA-PK, p110α, mTORC1, PI3KC2β, p110δ, mTORC2, p110β, and p110γ with IC50 of 2 nM, 8 nM, 20 nM, 26 nM, 48 nM, 83 nM, 88 nM and 150 nM, respectively.

  • GDC-0941

    GDC-0941 is a potent inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3 nM, 33 nM, 3 nM and 75 nM, respectively.

  • ZSTK474

    ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.

  • LY294002

    LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.

  • XL147

    XL147 (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.

  • TGX-221

    TGX-221 is a potent, selective PI3K inhibitor for p110β with IC50 of 8.5 nM.

  • PIK-90

    PIK-90 is a potent and cell permeable inhibitor of p110α, p110β, p110γ and p110δ with IC50 of 11 nM, 350 nM, 18 nM and 58 nM, respectively.

  • PIK-75

    PIK-75 is a selective and competitive inhibitor of p110α with IC50 of 5.8 nM and also potently inhibits DNA-PK with IC50 of 2 nM.

  • YM201636

    YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM.

Recently Viewed Items

Tags: buy CAY10505 | CAY10505 supplier | purchase CAY10505 | CAY10505 cost | CAY10505 manufacturer | order CAY10505 | CAY10505 distributor
Contact Us