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MK2206 (1032350-13-2)

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed….

Not Intended for Therapeutic Use. For research use only.

CAS: 1032350-13-2 Category

MK2206 (1032350-13-2) Description:

MK2206 is a Akt inhibitor, is also an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor MK2206 binds to and inhibits the activity of Akt in a non-ATP competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis.

MK2206 (1032350-13-2) Specifications:

Product Name MK2206
Synonym MK2206; MK-2206; MK 2206; MK2206 dihydrochloride; MK2206 HCl.
Chemical Name 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-8,9-dihydro-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1032350-13-2
Molecular Formula C25H25Cl2N5O
Molecular Weight 409.48483
Monoisotopic Mass 481.14362 g/mol
MDL number MFCD14584463
InChIKey AVWUIYMDWOYEFM-UHFFFAOYSA-N
InChi Code InChI=1S/C25H23N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31;;/h1-3,5-11,14-15,19,22H,4,12-13,26H2,(H,29,31);2*1H
SMILES O=C1NN=C2C3=CC(C4=CC=CC=C4)C(C5=CC=C(C6(N)CCC6)C=C5)N=C3C=CN21.[H]Cl.[H]Cl
Form Powder
Color Yellow
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application MK-2206 is a novel allosteric Akt inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Meng J, Majidi M, Fang B, Ji L, Bekele BN, Minna JD, Roth JA. The tumor suppressor gene TUSC2 (FUS1) sensitizes NSCLC to the AKT inhibitor MK2206 in LKB1-dependent manner. PLoS One. 2013 Oct 17;8(10):e77067. doi: 10.1371/journal.pone.0077067. eCollection 2013. PubMed PMID: 24146957; PubMed Central PMCID: PMC3798310.

[2]. Ding W, Shanafelt TD, Lesnick CE, Erlichman C, Leis JF, Secreto C, Sassoon TR, Call TG, Bowen DA, Conte M, Kumar S, Kay NE. Akt inhibitor MK2206 selectively targets CLL B-cell receptor induced cytokines, mobilizes lymphocytes and synergizes with bendamustine to induce CLL apoptosis. Br J Haematol. 2013 Sep 20. doi: 10.1111/bjh.12564. [Epub ahead of print] PubMed PMID: 24111951.

[3]. Liu R, Liu D, Xing M. The Akt inhibitor MK2206 synergizes, but perifosine antagonizes, the BRAF(V600E) inhibitor PLX4032 and the MEK1/2 inhibitor AZD6244 in the inhibition of thyroid cancer cells. J Clin Endocrinol Metab. 2012 Feb;97(2):E173-82. doi: 10.1210/jc.2011-1054. Epub 2011 Nov 16. PubMed PMID: 22090271; PubMed Central PMCID: PMC3275354.

[4]. Liu R, Liu D, Trink E, Bojdani E, Ning G, Xing M. The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathway. J Clin Endocrinol Metab. 2011 Apr;96(4):E577-85. doi: 10.1210/jc.2010-2644. Epub 2011 Feb 2. PubMed PMID: 21289267; PubMed Central PMCID: PMC3070256.