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S6 kinase&PKD-1

AZD2014 (1009298-59-2)

AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM; highly selective against multiple PI3K isoforms (α/β/γ/δ).

Not Intended for Therapeutic Use. For research use only.

CAS: 1009298-59-2 Category

AZD2014 (1009298-59-2) Description

Vistusertib, also known as AZD2014, is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor AZD2014 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR, a serine/threonine kinase that is upregulated in a variety of tumors, plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.

AZD2014 (1009298-59-2) Specifications

Product Name AZD2014
Synonym AZD2014, AZD-2014, AZD 2014, Vistusertib
Chemical Name 3-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]pyrimidin-7-yl]-N-methylbenzamide
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1009298-59-2
Molecular Formula C25H30N6O3
Molecular Weight 462.54
Monoisotopic Mass 462.23794 g/mol
MDL number MFCD22628784
InChIKey JUSFANSTBFGBAF-IRXDYDNUSA-N
InChi Code InChI=1S/C25H30N6O3/c1-16-14-33-11-9-30(16)23-20-7-8-21(18-5-4-6-19(13-18)24(32)26-3)27-22(20)28-25(29-23)31-10-12-34-15-17(31)2/h4-8,13,16-17H,9-12,14-15H2,1-3H3,(H,26,32)/t16-,17-/m0/s1
SMILES O=C(NC)C1=CC=CC(C2=CC=C3C(N4[[email protected]@H](C)COCC4)=NC(N5[[email protected]@H](C)COCC5)=NC3=N2)=C1
Form Powder
Color Yellow
Solubility  Soluble in DMSO, not 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 Vistusertib (AZD2014) is a novel mTOR inhibitor

 


RIDADR NONH for all modes of transport

References:

[1]. Huo HZ, Zhou ZY, Wang B, Qin J, Liu WY, Gu Y. Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. doi: 10.1016/j.bbrc.2013.11.099. Epub 2013 Dec 2. PubMed PMID: 24309100.

[2]. Kahn J, Hayman TJ, Jamal M, Rath BH, Kramp T, Camphausen K, Tofilon PJ. The mTORC1/mTORC2 inhibitor AZD2014 enhances the radiosensitivity of glioblastoma stem-like cells. Neuro Oncol. 2014 Jan;16(1):29-37. doi: 10.1093/neuonc/not139. Epub 2013 Dec 4. PubMed PMID: 24311635; PubMed Central PMCID: PMC3870843.

[3]. Rastogi R, Jiang Z, Ahmad N, Rosati R, Liu Y, Beuret L, Monks R, Charron J, Birnbaum MJ, Samavati L. Rapamycin induces mitogen-activated protein (MAP) kinase phosphatase-1 (MKP-1) expression through activation of protein kinase B and mitogen-activated protein kinase kinase pathways. J Biol Chem. 2013 Nov 22;288(47):33966-77. doi: 10.1074/jbc.M113.492702. Epub 2013 Oct 14. PubMed PMID: 24126911; PubMed Central PMCID: PMC3837136.

[4]. Cosimo E, Tarafdar A, Moles MW, Holroyd AK, Malik N, Catherwood MA, Hay J, Dunn KM, Macdonald AM, Guichard SM, O’Rourke DM, Leach MT, Sansom OJ, Cosulich SC, McCaig AM, Michie AM.

Clin Cancer Res. 2018 Dec 17. pii: clincanres.2036.2018. doi: 10.1158/1078-0432.CCR-18-2036. [Epub ahead of print]

PMID: 30559170

[5]. Pike KG, Malagu K, Hummersone MG, Menear KA, Duggan HM, Gomez S, Martin NM, Ruston L, Pass SL, Pass M. Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6. doi: 10.1016/j.bmcl.2013.01.019. Epub 2013 Jan 18. PubMed PMID: 23375793.