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Formula | C30H23N5O |
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Molecular Weight | 469.55 | CAS No. | 915019-65-7 | |
Solubility (25°C)* | In vitro | DMSO | 4 mg/mL (8.51 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. | |||||||||||
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In vitro | BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ235 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of BEZ235 with an average GI50 of 10-12 nM. [1] BEZ235 is an mTORC1/2 catalytic inhibitor. [2] | |||||||||||
In vivo | BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies. [1] |
Kinase Assay: |
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Cell Assay: |
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Animal Study: |
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Data from [Breast Cancer Res, 2011, 13, R52]
Data from [Breast Cancer Res, 2011, 13:R52]
Data from [Clin Cancer Res, 2010, 16, 6029-6039]
Data from [Cancer Res, 2010, 70, 4982-4994]
mTORC2-driven chromatin cGAS mediates chemoresistance through epigenetic reprogramming in colorectal cancer [ Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0] | PubMed: 39080411 |
Pericyte phenotype switching alleviates immunosuppression and sensitizes vascularized tumors to immunotherapy in preclinical models [ J Clin Invest, 2024, 134(18)e179860] | PubMed: 39286984 |
CASZ1 upregulates PI3K-AKT-mTOR signaling and promotes T-cell acute lymphoblastic leukemia [ Haematologica, 2024, 109(6):1713-1725] | PubMed: 38058200 |
Oocyte death is triggered by the stabilization of TAp63α dimers in response to cisplatin [ Cell Death Dis, 2024, 15(11):799] | PubMed: 39511162 |
The mTOR pathway controls phosphorylation of BRAF at T401 [ Cell Commun Signal, 2024, 22(1):428] | PubMed: 39223665 |
Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis [ Mol Oncol, 2024, 10.1002/1878-0261.13577] | PubMed: 38225213 |
PKC-independent PI3K signalling diminishes PKC inhibitor sensitivity in uveal melanoma [ Oncogenesis, 2024, 13(1):9] | PubMed: 38418838 |
Functional Assessments of Gynecologic Cancer Models Highlight Differences Between Single-Node Inhibitors of the PI3K/AKT/mTOR Pathway and a Pan-PI3K/mTOR Inhibitor, Gedatolisib [ Cancers (Basel), 2024, 16(20)3520] | PubMed: 39456616 |
Repurposing of sericin combined with dactolisib or vitamin D to combat non-small lung cancer cells through computational and biological investigations [ Sci Rep, 2024, 14(1):27034] | PubMed: 39505930 |
Characterization of the BH1406 non-small cell lung cancer (NSCLC) cell line carrying an activating SOS1 mutation [ Transl Lung Cancer Res, 2024, 13(11):2987-2997] | PubMed: 39670010 |
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