CAY10505

Potent PI3Kγ inhibitor CAS# 1218777-13-9

CAY10505

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Chemical structure

CAY10505

3D structure

Chemical Properties of CAY10505

Cas No. 1218777-13-9 SDF Download SDF
PubChem ID 1204893 Appearance Powder
Formula C14H8FNO3S M.Wt 289.28
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 34 mg/mL (117.53 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (5E)-5-[[5-(4-fluorophenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione
SMILES C1=CC(=CC=C1C2=CC=C(O2)C=C3C(=O)NC(=O)S3)F
Standard InChIKey UFBTYTGRUBUUIL-KPKJPENVSA-N
Standard InChI 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+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CAY10505

DescriptionCAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in 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].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].

References:
[1]. Sun YY, Lin SH et al. 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]. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39. [3]. Tyagi S. 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.

Protocol

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].

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.

References:
[1]. Sun YY, Lin SH et al. 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]. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39. [3]. Tyagi S. 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.

CAY10505 Dilution Calculator

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Preparing Stock Solutions of CAY10505

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.4569 mL 17.2843 mL 34.5686 mL 69.1372 mL 86.4215 mL
5 mM 0.6914 mL 3.4569 mL 6.9137 mL 13.8274 mL 17.2843 mL
10 mM 0.3457 mL 1.7284 mL 3.4569 mL 6.9137 mL 8.6421 mL
50 mM 0.0691 mL 0.3457 mL 0.6914 mL 1.3827 mL 1.7284 mL
100 mM 0.0346 mL 0.1728 mL 0.3457 mL 0.6914 mL 0.8642 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CAY10505

CAY10505 is a potent and selective PI3Kγ inhibitor (IC50= 30 nM)

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.

In neurons treated with 3.5 μM BA, 200 nM CAY10505 partially reduced the baicalein-induced Akt phosphorylation. [1]

In hypertensive rats, CAY10505 at 0.6 mg.kg-1 p.o. exhibited the following effects 1) effectively reduced MABP; 2) significantly ameliorated vascular endothelium dysfunction in hypertensive rats in combination of DOCA; 3) prominently increased serum nitrite and/or nitrate concentrations.4) prevented hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation.[2]

References:
[1] Tyagi S, Sharma S, Budhiraja RD.  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.
[2] Sun YY, Lin SH, Lin HC et al.  Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. PLoS One.  2013 Jul 19;8(7):e69019.

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References on CAY10505

Effect of phosphatidylinositol 3-kinase-gamma inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats.[Pubmed:22731503]

Can J Physiol Pharmacol. 2012 Jul;90(7):881-5.

This study has been designed to investigate the role of phosphatidyl-inositol 3-kinase-gamma (PI3Kgamma) in deoxycorticosterone acetate salt (DOCA) hypertension induced vascular endothelium dysfunction. Wistar rats were uninephrectomised and DOCA (40 mg.(kg body mass)(-1), subcutaneous injection) was administered twice weekly for 6 weeks to produce hypertension. Rats with mean arterial blood pressure >/= 140 mm Hg (1 mm Hg = 133.322 Pa) were selected as hypertensive. Vascular endothelium dysfunction was assessed in terms of attenuation of acetylcholine-induced endothelium-dependent relaxation (isolated aortic ring preparation), decrease in serum nitrate and (or) nitrite level, as well as reduced level of glutathione and disruption of integrity of vascular endothelium (histopathology). Five weeks of DOCA administration were followed by 7 days of daily administration of PI3Kgamma inhibitor (5-[[5-(4-fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione (CAY10505), 0.6 mg.kg(-1), per os (p.o.)), atorvastatin (30 mg.kg(-1), p.o.), and losartan (25 mg.kg(-1), p.o.) (positive control of hypertension), which significantly improved acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats.Therefore, it may be concluded that CAY10505, a specific inhibitor of PI3Kgamma, improves hypertension-associated vascular endothelial dysfunction. Thus, inhibition of PI3Kgamma might be a useful approach in the therapeutics of vascular endothelium dysfunction.

Description

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

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