Dactolisib
Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
Product Specifications
CAS Number
[915019-65-7]
Product Name Alternative
BEZ235; NVP-BEZ235
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Autophagy; mTOR; PI3K
Type
Reference compound
Related Pathways
Autophagy; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/BEZ235.html
Purity
99.94
Solubility
5% TFA in Water : 8.33 mg/mL (ultrasonic; warming; heat to 60°C) |DMF : 2 mg/mL (ultrasonic) |DMSO : 1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
CN(C1=C2C3=CC(C4=CC5=CC=CC=C5N=C4)=CC=C3N=C1)C(N2C6=CC=C(C=C6)C(C)(C#N)C)=O
Molecular Formula
C30H23N5O
Molecular Weight
469.54
Precautions
H302, H315, H319, H335
References & Citations
[1]Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7 (7), 1851-1863.|[2]Roper J, et al. The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer. PLoS One, 2011, 6 (9), e25132.|[3]Lee M, et al. Targeting PI3K/mTOR Signaling Displays Potent Antitumor Efficacy against Nonfunctioning Pituitary Adenomas. Clin Cancer Res. 2015 Jul 15;21 (14) :3204-15.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
MTOR; mTORC1; mTORC2; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
Citation 01
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