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.

MedKoo Cat#: 204520 Name: Vistusertib (AZD-2014) CAS#: 1009298-59-2 Chemical Formula: C25H30N6O3 Exact Mass: 462.23794 Molecular Weight: 462.54 Elemental Analysis: C, 64.92; H, 6.54; N, 18.17; O, 10.38

Synonym: AZD2014, AZD-2014, AZD 2014, Vistusertib

IUPAC/Chemical Name: 3-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]pyrimidin-7-yl]-N-methylbenzamide

InChi Key: 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 Code: O=C(NC)C1=CC=CC(C2=CC=C3C(N4[C@@H](C)COCC4)=NC(N5[C@@H](C)COCC5)=NC3=N2)=C1

Technical Data

Appearance: Yellow solid powder

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

Certificate of Analysis: View CoA: current batch, Lot#CRB51228 View CoA: previous batch, Lot#CRB40225

QC Data: View QC data: current batch, Lot#CRB51228 View QC data: previous batch, Lot#CRB40225

Safety Data Sheet (MSDS): View Material Safety Data Sheet (MSDS)

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).

Harmonized System Code: 293490

Additional Information

   

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: 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.