CAY10505Potent PI3Kγ inhibitor CAS# 1218777-13-9 |
- BYL-719
Catalog No.:BCC3707
CAS No.:1217486-61-7
- VS-5584 (SB2343)
Catalog No.:BCC2047
CAS No.:1246560-33-7
- PI-103
Catalog No.:BCC1162
CAS No.:371935-74-9
- CAL-101 (Idelalisib, GS-1101)
Catalog No.:BCC1270
CAS No.:870281-82-6
- BKM120
Catalog No.:BCC1279
CAS No.:944396-07-0
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| 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. | ||
| Description | CAY10505 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: | |||||
CAY10505 Dilution Calculator
CAY10505 Molarity Calculator
| 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. | |||||
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
- Pidotimod
Catalog No.:BCC4823
CAS No.:121808-62-6
- Xylometazoline HCl
Catalog No.:BCC4879
CAS No.:1218-35-5
- Ac-Trp-OH
Catalog No.:BCC3109
CAS No.:1218-34-4
- 5-Iodo-A-85380 dihydrochloride
Catalog No.:BCC7099
CAS No.:1217837-17-6
- RS 16566 dihydrochloride
Catalog No.:BCC6890
CAS No.:1217788-97-0
- SB 258719 hydrochloride
Catalog No.:BCC5937
CAS No.:1217674-10-6
- SB 205607 dihydrobromide
Catalog No.:BCC5687
CAS No.:1217628-73-3
- BYL-719
Catalog No.:BCC3707
CAS No.:1217486-61-7
- threo-1-C-Syringylglycerol
Catalog No.:BCN6110
CAS No.:121748-11-6
- NAS-181
Catalog No.:BCC7056
CAS No.:1217474-40-2
- (+)-UH 232 maleate
Catalog No.:BCC6790
CAS No.:1217473-50-1
- Isochandalone
Catalog No.:BCN4767
CAS No.:121747-90-8
- LDE225 Diphosphate
Catalog No.:BCC1693
CAS No.:1218778-77-8
- GKT137831
Catalog No.:BCC5460
CAS No.:1218942-37-0
- Dorsomorphin 2HCl
Catalog No.:BCC4361
CAS No.:1219168-18-9
- (-)-MK 801
Catalog No.:BCC4593
CAS No.:121917-57-5
- CCT 031374 hydrobromide
Catalog No.:BCC6258
CAS No.:1219184-91-4
- Aurothioglucose
Catalog No.:BCC5446
CAS No.:12192-57-3
- Sophoraflavanone C
Catalog No.:BCN3543
CAS No.:121927-91-1
- Dihydrodaidzin
Catalog No.:BCN2879
CAS No.:121927-96-6
- PKA inhibitor fragment (6-22) amide
Catalog No.:BCC1042
CAS No.:121932-06-7
- 4,5-Diepipsidial A
Catalog No.:BCN3920
CAS No.:1219603-97-0
- PF 4778574
Catalog No.:BCC6322
CAS No.:1219633-99-4
- (±)-Anatoxin A fumarate
Catalog No.:BCC6796
CAS No.:1219922-30-1
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.
