dactolisib

Also known as BEZ235, NVP-BEZ235, BEZ-235, NVP-BEZ 235, NVP BEZ235, NVPBEZ235, BEZ 235

Dactolisib (codenamed NVP-BEZ235 and BEZ-235, also known as RTB101) is an imidazoquinoline derivative acting as a PI3K inhibitor. It also inhibits mTOR. It is being investigated as a possible cancer treatment.

In the Vinony graph

Within Vinony's link graph, dactolisib is referenced by 8 other articles, and connects out to tiazofurin, digital object identifier and chemical formula.

It sits within the topics 4-Aminophenyl compounds, Chembox image size set and Experimental cancer drugs.

Its subject is documented across 4 Wikipedia language editions.

Chemical data

Formula: C30H23N5O
Molecular weight: 469.5 g/mol
IUPAC name: 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile
SMILES: CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5
InChIKey: JOGKUKXHTYWRGZ-UHFFFAOYSA-N
XLogP: 5.2
Polar surface area: 73.1 Å²
H-bond donors: 0
H-bond acceptors: 4
Formal charge: 0

via PubChem

Drug data · ChEMBL

Max clinical phase: Phase 3
Molecule type: Small molecule
Indications: neoplasm, Transitional Cell Carcinoma, infection, pancreatic neuroendocrine tumor

via ChEMBL · EBI

Research

498 papers

Folate-dactolisib conjugates for targeting tubular cells in polycystic kidneys.Journal of controlled release : official journal of the Controlled Release Society · 2019
Synergistic effect of Dactolisib/Lys05 combination on autophagy in A549 cells.Acta biochimica Polonica · 2023
Dactolisib (NVP-BEZ235) toxicity in murine brain tumour models.BMC cancer · 2016
PI3K/mTOR Inhibitor Dactolisib Attenuates Allergic Response Through Inhibitions of the Sensitization and Mast Cell Activation.Die Pharmazie · 2023
Repurposing of sericin combined with dactolisib or vitamin D to combat non-small lung cancer cells through computational and biological investigations.Scientific reports · 2024

via PubMed

Wikidata facts

Subclass of: chemical compound
Mass: 469.19026

Show 5 more facts

chemical formula: C₃₀H₂₃N₅O
canonical SMILES: CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5
subject has role: antineoplastic
World Health Organisation international non-proprietary name: dactolisib
Commons category: Dactolisib

Sources (3)

via Wikidata · CC0

~2 min read

Encyclopedic overview

1 sections

Contents

References

{{Chembox | Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 458976997 | ImageFile = Dactolisib.svg | ImageClass = skin-invert-image | ImageSize = 220px | ImageFile1 = Dactolisib molecule ball.png | ImageClass1 = bg-transparent | ImageSize1 = 240 | ImageAlt1 = Ball-and-stick model of the BEZ235 molecule | PIN = 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 | OtherNames = NVP-BEZ235; BEZ-235; RTB101

| Section1 =

Excerpted from Wikipedia’s “dactolisib” article, available under the CC BY-SA 4.0 licence.