BEZ235

BEZ235

Names
IUPAC name 2-Methyl-2-{4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
Other names NVP-BEZ235; BEZ-235; Dactolisib
Identifiers
CAS Number	915019-65-7
ChEMBL	ChEMBL1879463
ChemSpider	10151099
IUPHAR/BPS	7950
Jmol interactive 3D	Image
PubChem	11977753
InChI InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3 Key: JOGKUKXHTYWRGZ-UHFFFAOYSA-N InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3
SMILES N#CC(c6ccc(N5c4c(cnc3ccc(c1cc2ccccc2nc1)cc34)N(C5=O)C)cc6)(C)C
Properties
Chemical formula	C30H23N5O
Molar mass	469.55 g·mol^−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

BEZ235 or NVP-BEZ235 is an imidazoquinoline derivative and PI3K inhibitor^[1] being investigated as a possible cancer treatment.^[2]

It has been shown to be toxic to Waldenström's macroglobulinemia cells.^[3]

It was the first PI3K inhibitor to enter clinical trials, in 2006 (primary outcome results due in 2010).^[4]

References

1. "NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas".
2. Maira; et al. (2009). "PI3K inhibitors for cancer treatment: where do we stand?" (PDF). doi:10.1042/BST0370265.
3. Sacco, A.; Roccaro, A.; Ghobrial, I. M. (2010). "Role of dual PI3/Akt and mTOR inhibition in Waldenstrom's Macroglobulinemia". Oncotarget 1 (7): 578–582. doi:10.18632/oncotarget.192. PMC 3248138. PMID 21317453.
4. "A Phase I/II Study of BEZ235 in Patients With Advanced Solid Malignancies Enriched by Patients With Advanced Breast Cancer".