CAY10505

ArtNr	S2682-10
Hersteller	Selleckchem
CAS-Nr.	1218777-13-9
Menge	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 25 mg 50 mg 5 g
Kategorie	Oncology Food Safety Allergenes Neuroscience Neuroinflammation Inhibitors & Compound Libraries Small Molecules By Organ Gastric Cancer Bone Cancer
Typ	Inhibitors
Specific against	other
Smiles	C1=CC(=CC=C1C2=CC=C(O2)C=C3C(=O)NC(=O)S3)F
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1218777-13-9 '
Similar products	CAY10505
Lieferbar
Manufacturer - Targets	PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	289, 28
Administration	Administered via p.o.
Animal Models	Wistar albino rats
Cell lines	Bone marrow cells
Concentrations	ca.10 mM
Dosages	0.6 mg/kg
IC50	30 nM, 30 nM, 30 nM, 30 nM, 30 nM, 30 nM
In vitro	CAY10505 selectively inhibits PI3Kgamma isoform, with an IC50 of 30 nM better than the PI3Kalpha, beta, and delta isoforms, with IC50 of 0.94, 20 and 20 uM, 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 uM. CAY10505 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 of 52 uM, as well as in the monocytic cell line THP-1 with an IC50 of 53 uM. [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 PI3Kgamma-deficient mice. [1] Five weeks of deoxycorticosterone acetate salt (DOCA) administration are followed by 7 days of daily administration of PI3Kgamma 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]
Incubation Time	3 hours
Kinase Assay	PI3Kgamma lipid kinase assay, A PI3Kgamma lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[gamma33P]ATP and PtdIns as substrates. Kinase assays for IC50 value determinations of CAY10505 with PI3Kalpha, PI3Kbeta, and PI3Kdelta are carried out.
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 um pore size, chemotaxis plate. An amount of 600 uL 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.
Solubility (25C)	DMSO 58 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.
Chemical Name	(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2, 4-dione

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