CAY10505

Alias: CAY 10505; CAY10505; CAY-10505
Cat No.:V0139 Purity: ≥98%
CAY10505, the dehydroxylated form of AS-252424, is a novel,potent and selective inhibitor ofPI3Kγ (phosphoinositide 3-kinase) with a potential toimprove hypertension-associated vascular endothelial dysfunction.
CAY10505 Chemical Structure CAS No.: 1218777-13-9
Product category: PI3K
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

CAY10505, the dehydroxylated form of AS-252424, is a novel, potent and selective inhibitor of PI3Kγ (phosphoinositide 3-kinase) with a potential to improve hypertension-associated vascular endothelial dysfunction.

Biological Activity I Assay Protocols (From Reference)
Targets
PI3Kγ ( IC50 = 30 nM, Neurons)
ln Vitro
Baicalein induces Akt phosphorylation in neurons, which is partially inhibited by the class IB PI3K isoform inhibitor CAY10505 at a concentration of 200 nM (IC50=30 nM). An extensive panel of multiple myeloma (MM) cell lines and recently isolated primary MM samples are used to test the pharmacological PI3K inhibitor CAY10505 (PIK3CG). MM cells are given a CAY10505 treatment for 3 days in the case of MM cell lines or 5 days in the case of primary MM cells, and the survival is then examined using flow cytometry (annexin V-FITC/PI staining). The PIK3CA inhibitor CAY10505 has anti-survival effects on bone marrow stromal cells (BMSCs)-co-cultured primary MM samples (mean survival relative to DMSO-treated controls: CAY10505: tested at 10 M: 8414%).
ln Vivo
The effects of CAY10505 at 0.6 mg.kg-1 p.o. were as follows in hypertensive rats 1) Significantly improved vascular endothelium dysfunction in hypertensive rats when combined with DOCA; 2) markedly increased serum nitrite and/or nitrate concentrations; and 3) significantly decreased MABP. 4) prevented the endothelium-dependent relaxation brought on by ACh from being diminished by hypertension.
Cell Assay
In neurons treated with 3.5 μM BA, 200 nM CAY10505 partially reduced the baicalein-induced Akt phosphorylation.
Animal Protocol
Wistar albino rats (180-240 g) of either sex are employed in the present study. The number of rats used (n) for each group is 6. Rats are kept in Group I (normal control) on a diet of standard chow and water. Rats in Group II (hypertensive control) are unilaterally nephrectomized (uninephrectomized), given subcutaneous injections of DOCA (40 mg/kg) twice a week for six weeks, and then the untreated drinking water is changed to a 1% NaCl solution. After receiving treatment with DOCA for five weeks, rats in Group III (hypertensive rats) were given CAY10505 (0.6 mg/kg, per os (p.o)) for one week. Rats in Group IV (hypertensive rats) receive treatment with Losartan (25 mg/kg, p.o.) for one week following five weeks of DOCA treatment. Rats in Group V (hypertensive rats) receive Atorvastatin (30 mg/kg, p.o.) for 1 week after receiving DOCA for 5 weeks. Wistar albino rats
References

[1]. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. 2013 Jul 19;8(7):e69019.

[2]. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats. Can J Physiol Pharmacol. 2012 Jul, 90(7), 881-5.

[3]. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39.

[4]. MiR-1976 Knockdown Promotes Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties Inducing Triple-Negative Breast Cancer Metastasis. Cell Death Dis. 2020 Jul 3;11(7):500.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H8FNO3S
Molecular Weight
289.28162
Exact Mass
289.02
Elemental Analysis
C, 58.13; H, 2.79; F, 6.57; N, 4.84; O, 16.59; S, 11.08
CAS #
1218777-13-9
Related CAS #
1218777-13-9
Appearance
Solid powder
SMILES
O=C(NC/1=O)SC1=C\C2=CC=C(C3=CC=C(F)C=C3)O2
InChi Key
UFBTYTGRUBUUIL-KPKJPENVSA-N
InChi Code
InChI=1S/C14H8FNO3S/c15-9-3-1-8(2-4-9)11-6-5-10(19-11)7-12-13(17)16-14(18)20-12/h1-7H,(H,16,17,18)/b12-7+
Chemical Name
(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
Synonyms
CAY 10505; CAY10505; CAY-10505
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

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~58 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 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
10 mM 0.3457 mL 1.7284 mL 3.4569 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.

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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.

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Biological Data
  • CAY10505

    Effects of PI3K inhibitors on the baicalein–activated HIF1α and Epo/VEGF gene transcription in neurons. Neurons were treated with 3.5 μM BA with or without 1 h pretreatment with the pan PI3K inhibitor LY294002 (LY, 10 μM), PI3Kα/β inhibitor (PI3K α inhibitor-2, 50 nM), or PI3Kγ inhibitor (CAY10505, 200 nM). PLoS One, 2013, 8(7):e69019.

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