Dactolisib

Dactolisib
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
Identifiers
CAS Number	915019-65-7 ;
3D model (JSmol)	Interactive image;
ChEMBL	ChEMBL1879463 ;
ChemSpider	10151099 ;
IUPHAR/BPS	7950;
KEGG	D10552;
PubChem CID	11977753;
CompTox Dashboard (EPA)	DTXSID10238599 ;
	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 ;
	SMILES N#CC(c6ccc(N5c4c(cnc3ccc(c1cc2ccccc2nc1)cc34)N(C5=O)C)cc6)(C)C;
Properties
Chemical formula	C30H23N5O
Molar mass	469.548 g·mol−1
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). verify (what is ?) Infobox references

Dactolisib (codenamed NVP-BEZ235 and BEZ-235) is an imidazoquinoline derivative acting as a PI3K inhibitor.^[1] It also inhibits mTOR.^[2] It is being investigated as a possible cancer treatment.^[3]

It has been shown to be toxic to Waldenström's macroglobulinemia cells.^[4]

It was the first PI3K inhibitor to enter clinical trials, in 2006.^[5]

A phase IB/II clinical trial for locally advanced or metastatic HER2 negative breast cancer has completed.^[6]

A phase II clinical trial for advanced pancreatic neuroendocrine tumors (pNET) has reported results.^[7]

References

^ Liu, TJ; Koul, D; LaFortune, T; Tiao, N; Shen, RJ; Maira, SM; Garcia-Echevrria, C; Yung, WKA (11 August 2009). "NVP-BEZ235, a Novel Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor, Elicits Multifaceted Antitumor Activities in Human Gliomas". Molecular Cancer Therapeutics. 8 (8): 2204–10. doi:10.1158/1535-7163.MCT-09-0160. PMC 2752877. PMID 19671762.
^ Awasthi, N; Yen, PL; Schwarz, MA; Schwarz, RE (March 2012). "The Efficacy of a Novel, Dual PI3K/mTOR Inhibitor NVP-BEZ235 to Enhance Chemotherapy and Antiangiogenic Response in Pancreatic Cancer". Journal of Cellular Biochemistry. 113 (3): 784–91. doi:10.1002/jcb.23405. PMID 22020918.
^ Maira, SM; Stauffer, F; Schnell, C; García-Echeverría, C (1 February 2009). "PI3K Inhibitors for Cancer Treatment: Where Do We Stand?" (PDF). Biochemical Society Transactions. 37 (1): 265–72. doi:10.1042/BST0370265. PMID 19143644. Retrieved 16 July 2016.
^ Sacco, A; Roccaro, A; Ghobrial, IM (November 2010). "Role of Dual PI3/Akt and mTOR Inhibition in Waldenström's Macroglobulinemia". Oncotarget. 1 (7): 578–82. doi:10.18632/oncotarget.101105 (inactive 2017-08-12). PMC 3248138. PMID 21317453.{{cite journal}}: CS1 maint: DOI inactive as of August 2017 (link)
^ "A Phase I/II Study of BEZ235 in Patients with Advanced Solid Malignancies Enriched by Patients with Advanced Breast Cancer". ClinicalTrials.gov. Retrieved 16 July 2016.
^ Phase Ib/II Trial of BEZ235 With Paclitaxel in Patients With HER2 Negative, Locally Advanced or Metastatic Breast Cancer
^ BEZ235 Phase II Trial in Patients With Advanced Pancreatic Neuroendocrine Tumors (pNET) After Failure of mTOR Inhibitor Therapy.

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[1] Liu, TJ; Koul, D; LaFortune, T; Tiao, N; Shen, RJ; Maira, SM; Garcia-Echevrria, C; Yung, WKA (11 August 2009). "NVP-BEZ235, a Novel Dual Phosphatidylinositol 3-kinase/Mammalian Target of Rapamycin Inhibitor, Elicits Multifaceted Antitumor Activities in Human Gliomas". Molecular Cancer Therapeutics. 8 (8): 2204–10. doi:10.1158/1535-7163.MCT-09-0160. PMC 2752877. PMID 19671762.

[2] Awasthi, N; Yen, PL; Schwarz, MA; Schwarz, RE (March 2012). "The Efficacy of a Novel, Dual PI3K/mTOR Inhibitor NVP-BEZ235 to Enhance Chemotherapy and Antiangiogenic Response in Pancreatic Cancer". Journal of Cellular Biochemistry. 113 (3): 784–91. doi:10.1002/jcb.23405. PMID 22020918.

[3] Maira, SM; Stauffer, F; Schnell, C; García-Echeverría, C (1 February 2009). "PI3K Inhibitors for Cancer Treatment: Where Do We Stand?" (PDF). Biochemical Society Transactions. 37 (1): 265–72. doi:10.1042/BST0370265. PMID 19143644. Retrieved 16 July 2016.

[4] Sacco, A; Roccaro, A; Ghobrial, IM (November 2010). "Role of Dual PI3/Akt and mTOR Inhibition in Waldenström's Macroglobulinemia". Oncotarget. 1 (7): 578–82. doi:10.18632/oncotarget.101105 (inactive 2017-08-12). PMC 3248138. PMID 21317453.{{cite journal}}: CS1 maint: DOI inactive as of August 2017 (link)

[5] "A Phase I/II Study of BEZ235 in Patients with Advanced Solid Malignancies Enriched by Patients with Advanced Breast Cancer". ClinicalTrials.gov. Retrieved 16 July 2016.

[6] Phase Ib/II Trial of BEZ235 With Paclitaxel in Patients With HER2 Negative, Locally Advanced or Metastatic Breast Cancer

[7] BEZ235 Phase II Trial in Patients With Advanced Pancreatic Neuroendocrine Tumors (pNET) After Failure of mTOR Inhibitor Therapy.

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