AZD-2858
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MedKoo CAT#: 522421

CAS#: 486424-20-8 (free base)

Description: AZD2858 is a potent and GSK-3 inhibitor with an IC50 of 68 nM. AZD-2858 inhibits tau phosphorylation at the S396 site, and it activates Wnt signaling pathway. AZD2858 has a substantial impact on fracture healing. The fractures healed with a bony callus without an obvious endochondral component, suggesting that AZD2858 drives mesenchymal cells into the osteoblastic pathway.


Chemical Structure

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AZD-2858
CAS# 486424-20-8 (free base)

Theoretical Analysis

MedKoo Cat#: 522421
Name: AZD-2858
CAS#: 486424-20-8 (free base)
Chemical Formula: C21H23N7O3S
Exact Mass: 453.15831
Molecular Weight: 453.52
Elemental Analysis: C, 55.62; H, 5.11; N, 21.62; O, 10.58; S, 7.07

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 850.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2850.0 2 Weeks
2.0g USD 4850.0 2 Weeks
5.0g USD 7450.0 2 Weeks
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Related CAS #: 2108876-05-5 (HCl)   486424-21-9 (xHCl)   486424-20-8 (free base)    

Synonym: AZD-2858; AZD 2858; AZD2858;

IUPAC/Chemical Name: 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamid

InChi Key: FHCSBLWRGCOVPT-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H23N7O3S/c1-27-9-11-28(12-10-27)32(30,31)17-6-4-15(5-7-17)18-14-24-20(22)19(26-18)21(29)25-16-3-2-8-23-13-16/h2-8,13-14H,9-12H2,1H3,(H2,22,24)(H,25,29)

SMILES Code: NC1=NC=C(C2=CC=C(S(N3CCN(C)CC3)(=O)=O)C=C2)N=C1C(NC4=CC=CN=C4)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 453.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Gilmour PS, O'Shea PJ, Fagura M, Pilling JE, Sanganee H, Wada H, Courtney PF,  Kavanagh S, Hall PA, Escott KJ. Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in rats. Toxicol Appl Pharmacol. 2013 Oct 15;272(2):399-407. doi: 10.1016/j.taap.2013.07.001. Epub 2013 Jul 18. PubMed PMID: 23872097.
 
2: Sisask G, Marsell R, Sundgren-Andersson A, Larsson S, Nilsson O, Ljunggren O,  Jonsson KB. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone. 2013 May;54(1):126-32. doi: 10.1016/j.bone.2013.01.019. Epub 2013 Jan 19. PubMed PMID: 23337038.
 
3: Marsell R, Sisask G, Nilsson Y, Sundgren-Andersson AK, Andersson U, Larsson S, Nilsson O, Ljunggren O, Jonsson KB. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012 Mar;50(3):619-27. doi: 10.1016/j.bone.2011.11.007. Epub 2011 Nov 25. PubMed PMID: 22142634.  

AZD-2858

25.0mg / USD 150.0