1. PI3K/Akt/mTOR Apoptosis
  2. PI3K Apoptosis
  3. CAY10505

CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.

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

CAY10505 Chemical Structure

CAY10505 Chemical Structure

CAS No. : 1218777-13-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 44 In-stock
Solution
10 mM * 1 mL in DMSO USD 44 In-stock
Solid
10 mg USD 40 In-stock
25 mg USD 65 In-stock
50 mg USD 115 In-stock
100 mg USD 190 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CAY10505 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jul 3;11(7):500.  [Abstract]

    The protein expression levels of PIK3CG, AKT, and p-AKT are measured by Western blot. The properties of EMT in SUM-1315 and ZR-75-1 transfected with CAY10505 is determined by wound healing assay.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.

    IC50 & Target[1]

    PI3Kγ

    30 nM (IC50, Neurons)

    In Vitro

    A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons[1]. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM)[2].

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

    In Vivo

    Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation[3].

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

    Molecular Weight

    289.28

    Formula

    C14H8FNO3S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NC/1=O)SC1=C\C2=CC=C(C3=CC=C(F)C=C3)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 : ≥ 34 mg/mL (117.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4569 mL 17.2843 mL 34.5686 mL
    5 mM 0.6914 mL 3.4569 mL 6.9137 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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    This equation is commonly abbreviated as: C1V1 = C2V2

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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: 99.75%

    References
    Cell Assay
    [2]

    Up to 5×104 multiple myeloma (MM) cells/100 μL of medium per well are seeded in 96-well-plates. Primary MM cells are always seeded into wells containing primary bone marrow stromal cells. Drugs (e.g., CAY10505) are dissolved in either DMSO or acidified ethanol (in the case of melphalan) and kept as frozen stock solutions of 10-50 mM. Working dilutions in fullmedium are always freshly prepared. In the case of Bortezomib small volumes of single-thaw stock solution aliquots are prepared. Drug dilutions (e.g., CAY10505, 2.5, 5, 7.5 and 10 μM) are added to MM cells as 100 μL of 2× the final concentration per well for single-drug treatments, and in appropriate volumes of higher concentrations for drug combinations. Solvent controls are always included[2].

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

    Animal Administration
    [3]

    Rats[3]
    Wistar albino rats (180-240 g) of either sex are employed in the present study. For each group, the number of rats used (n) is 6. Group I (normal control): Rats are maintained on a diet of normal chow with drinking water. Group II (hypertensive control): Rats are unilaterally nephrectomized (uninephrectomised) and DOCA (40 mg/kg) is administered by subcutaneous injection (s.c.) twice weekly for 6 weeks, and then the untreated drinking water is replaced with a 1% NaCl solution. Group III (hypertensive rats): Rats are treated with CAY10505 (0.6 mg/kg, per os (p.o)) for 1 week after 5 weeks of treatment with DOCA. Group IV (hypertensive rats): Rats are treated with Losartan (25 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA. Group V (hypertensive rats): Rats are treated with Atorvastatin (30 mg/kg, p.o.) for 1 week after 5 weeks of treatment with DOCA.

    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 3.4569 mL 17.2843 mL 34.5686 mL 86.4215 mL
    5 mM 0.6914 mL 3.4569 mL 6.9137 mL 17.2843 mL
    10 mM 0.3457 mL 1.7284 mL 3.4569 mL 8.6421 mL
    15 mM 0.2305 mL 1.1523 mL 2.3046 mL 5.7614 mL
    20 mM 0.1728 mL 0.8642 mL 1.7284 mL 4.3211 mL
    25 mM 0.1383 mL 0.6914 mL 1.3827 mL 3.4569 mL
    30 mM 0.1152 mL 0.5761 mL 1.1523 mL 2.8807 mL
    40 mM 0.0864 mL 0.4321 mL 0.8642 mL 2.1605 mL
    50 mM 0.0691 mL 0.3457 mL 0.6914 mL 1.7284 mL
    60 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4404 mL
    80 mM 0.0432 mL 0.2161 mL 0.4321 mL 1.0803 mL
    100 mM 0.0346 mL 0.1728 mL 0.3457 mL 0.8642 mL
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    • 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.

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    Product Name:
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    Cat. No.:
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