AZD2858 486424-20-8

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Molecular Weight: 453.52 AZD2858 is a selective GSK-3 Inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits
tau phosphorylation at the S396 site, activates Wnt signaling pathway.
AZD2858 treatment (1 μM, 12 h) on primary isolated human osteoblast-like
cells results in a 3-fold increase of β-catenin levels. AZD2858 causes β-catenin stabilisation in human and rat mesenchymal stem
cells, stimulates hADSC commitment towards osteoblasts and osteogenic
mineralisation in vitro.





In rats, oral AZD2858 treatment causes a dose-dependent increase in
trabecular bone mass compared to control after a two-week treatment with
a maximum effect at a dose of 20 mg/kg once daily (total BMC: 172% of
control). A small but significant effect is also seen at cortical sites
(total BMC: 111% of control). AZD285 treatment (30
μmol/kg) on rats daily for up to 3 weeks shows an increase in both
mineral density (of 28% at 2 weeks and 38% at 3 weeks) and mineral
content (of 81% at 2 weeks and 93% at 3 weeks) in the calluses.


AZD285
treatment makes the fractures heals more rapidly, with a bony callus
without an obvious endochondral component. AZD2858
produces time-dependent changes in serum bone turnover biomarkers and
increases bone mass over 28 days exposure in rats. After 7 days, AZD2858
increases the bone formation biomarker P1NP, and reduces the resorption
biomarker TRAcP-5b, indicating increased bone anabolism and reduced
resorption in rats.

Tau phosphorylation assay

NIH-3T3 cells expressing 4-repeat Tau are used to assess functional activity of AZD2858 in vitro. The cells are grown in DMEM media and 2 mM L-glut, and 10% HiFCS, and plated at a concentration of 6×105 cells/well in 6-well plates. In each experiment, AZD2858 is dosed in triplicates at a concentration of 1, 10, 100, 500, 1000, 2000 and 10,000 nM. Cells are treated for 4 h prior to cell lysis using 100 μL ice cold lysis buffer (0.5% NP-40, 10 mM Tris, pH 7.2, 150 mM NaCl, 2 mM EDTA). A suspension is made with addition of protease and phosphatase Inhibitors: 50 mM NaF, 0.2 mM NaVO4 and Cocktail Protease inhibitors. The solution is then snap frozen at − 80 °C for at least 1 h, before thawing on ice and lysate clarification by centrifugation, followed by Western blot according to standard protocols. After blocking, the blots are exposed to the primary antibody, Phospho-Ser396-tau (1:1000) over night, washed and incubated with the secondary antibody (donkey anti-rabbit, 1:5000), followed by a final wash. For re-probing, the primary antibody Tau5 (1:200) and the secondary horseradish peroxidase linked antibody (sheep anti-mouse, 1:10000) are used. All blots are developed using ECL Western blot detection reagents, Kodak X-ray films, quantified using densitometric analysis, and the ratio of S396 tau to total tau (tau5) is calculated.

Cell Assay: [2]

Cell lines	Human adipose derived stem cells and rat MSCs
Concentrations	~20 mM
Incubation Time	24 h
Method	Human adipose derived stem cells and rat MSCs (isolated from bone marrow of Sprague Dawley rats at less than 8 weeks after gestation) are cultured in a basal media of DMEM containing 5% FBS and 2 mM GlutaMax. Cells are seeded in basal media into 96-well plates (3–5000 cells/well) for 18 h before treatment with AZD2858 (0.3 nM to 20 mM). After 24 h, β-catenin stabilisation is measured.

Animal Study: [2]

Animal Models	rat
Formulation	in water adjusted to pH 3.5
Dosages	30 μmol/kg/day
Administration	orally
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	453.52
Formula	C21H23N7O3S
CAS No.	486424-20-8

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	N/A

Solubility (25°C) *	In vitro	DMSO	7 mg/mL (15.43 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	2-Pyrazinecarboxamide, 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-

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