Art. -Nr.: HY-50673A

Dactolisib hydrochloride

(Synonyms: BEZ235 hydrochloride; NVP-BEZ235 hydrochloride)

65 Cited Publications

Kundenbewertung

Based on 65 publication(s) in Google Scholar

Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC₅₀ of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.

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Reinheit: 99.41%
CAS. Nr.: 2319647-83-9
Formel: C₃₀H₂₄ClN₅O
Molecular Weight:506.00

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Dactolisib hydrochloride Chemical Structure

CAS. Nr.: 2319647-83-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
Chemical Information
Publications (65)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Chemical Information

CAS. Nr. 2319647-83-9
Appearance Solid
Molecular Weight 506.00
Formel C₃₀H₂₄ClN₅O
Color White to light yellow
SMILES

CN(C1=O)C2=C(C3=CC(C4=CC5=C(N=C4)C=CC=C5)=CC=C3N=C2)N1C6=CC=C(C=C6)C(C)(C#N)C.Cl
Synonyms

BEZ235 hydrochloride; NVP-BEZ235 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (65)

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Nature

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. [Abstract]

2018 Aug;560(7719):499-503. PMID: 30051890
Cell

Innate immune and metabolic signals induce mitochondria-dependent membrane lysis via mitoxyperiosis. [Abstract]

2025 Dec 11;188(25):7155-7174.e25. PMID: 41317732
Cell Res

Endothelial CDS2 deficiency causes VEGFA-mediated vascular regression and tumor inhibition. [Abstract]

2019 Nov;29(11):895-910. PMID: 31501519
Blood

Suz12 inactivation cooperates with JAK3 mutant signaling in the development of T-cell acute lymphoblastic leukemia. [Abstract]

2019 Oct 17;134(16):1323-1336. PMID: 31492675
Cancer Res

H4K20me3-Mediated Repression of Inflammatory Genes Is a Characteristic and Targetable Vulnerability of Persister Cancer Cells. [Abstract]

2025 Jan 2;85(1):32-51. PMID: 39476057
Nat Commun

Intrinsic resistance to RAS inhibitors is driven by dysregulation of KRAS degradation. [Abstract]

2025 Dec 15. PMID: 41397976
Nat Commun

Codon bias imposes a targetable limitation on KRAS-driven therapeutic resistance. [Abstract]

2017 Jun 8;8:15617. PMID: 28593995

Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]

Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors BEZ235 (Dactolisib).
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

EETs Reduction Contributes to Granulosa Cell Senescence and Endometriosis-Associated Infertility via the PI3K/AKT/mTOR Signaling Pathway. [Abstract]

2025 Aug 19:e05656. PMID: 40827571
Adv Sci (Weinh)

ANO1-Mediated Inhibition of Cancer Ferroptosis Confers Immunotherapeutic Resistance through Recruiting Cancer-Associated Fibroblasts. [Abstract]

2023 Aug;10(24):e2300881. PMID: 37341301
Exp Hematol Oncol

Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]

2016 Jul 29:5:22. PMID: 27478685
Leukemia

BET inhibitor-based combinations targeting novel dependencies in MECOM-rearranged (r) AML. [Abstract]

2025 Dec 19. PMID: 41419608
Leukemia

Repression of BIM mediates survival signaling by MYC and AKT in high-risk T-cell acute lymphoblastic leukemia. [Abstract]

2014 Sep;28(9):1819-27. PMID: 24552990

Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Leukemia. 2014 Sep;28(9):1819-27. [Abstract]

Western blot analysis of human T-ALL cell lines treated for 24 hours using DMSO (vehicle control), 1 μM JQ1, 500 nM BEZ235, or both drugs in combination, using the indicated antibodies. Western blot analysis of these T-ALL cell lines following treatment with JQ1, BEZ235 or both drugs in combination reveals cooperative upregulation of BIM protein expression coupled to induction of apoptosis, as assessed by PARP cleavage.
J Exp Clin Cancer Res

TSSC3 promotes autophagy via inactivating the Src-mediated PI3K/Akt/mTOR pathway to suppress tumorigenesis and metastasis in osteosarcoma, and predicts a favorable prognosis. [Abstract]

2018 Aug 9;37(1):188. PMID: 30092789

Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 9;37(1):188. [Abstract]

Representative images of the western blotting analysis of TSSC3, ATG5, P62, LC3, Src, Akt, mTOR and their phosphorylated versions in MTF and SaOS2 cells. Cells are treated with TSSC3-overexpression, IGF-1, p-YEEI, and BEZ235 separately or in combination.
J Nanobiotechnology

Carbonic anhydrase IX-targeted H-APBC nanosystem combined with phototherapy facilitates the efficacy of PI3K/mTOR inhibitor and resists HIF-1α-dependent tumor hypoxia adaptation. [Abstract]

2022 Apr 12;20(1):187. PMID: 35413842
Sci Adv

Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding. [Abstract]

2023 Mar 22;9(12):eadd5028. PMID: 36947620
EBioMedicine

PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. [Abstract]

2015 Nov 19;2(12):1944-56. PMID: 26844273
Cell Death Dis

A novel 4-aminoquinazoline derivative, DHW-208, suppresses the growth of human breast cancer cells by targeting the PI3K/AKT/mTOR pathway. [Abstract]

2020 Jun 30;11(6):491. PMID: 32606352
Cell Commun Signal

Autophagy modulators influence the content of important signalling molecules in PS-positive extracellular vesicles. [Abstract]

2023 May 24;21(1):120. PMID: 37226246
BMC Med

HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]

2021 Oct 15;19(1):247. PMID: 34649530
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086
Haematologica

Human BCR/ABL1 induces chronic myeloid leukemia-like disease in zebrafish. [Abstract]

2020 Mar;105(3):674-686. PMID: 31289206
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Br J Cancer

METTL14-mediated N6-methyladenosine modification of Pten mRNA inhibits tumour progression in clear-cell renal cell carcinoma. [Abstract]

2022 Jul;127(1):30-42. PMID: 35249103
Sci Signal

TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]

2021 Jun 22;14(688):eabe6156. PMID: 34158398
JCI Insight

ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors. [Abstract]

2022 Aug 22;7(16):e155899. PMID: 35852858
Cancer Cell Int

FAP promotes clear cell renal cell carcinoma progression via activating the PI3K/AKT/mTOR signaling pathway. [Abstract]

2023 Sep 27;23(1):217. PMID: 37752545
Eur J Med Chem

Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia. [Abstract]

2023 Oct 5:258:115543. PMID: 37329712
Biochem Pharmacol

DZW-310, a novel phosphoinositide 3-kinase inhibitor, attenuates the angiogenesis and growth of hepatocellular carcinoma cells via PI3K/AKT/mTOR axis. [Abstract]

2022 Jul:201:115093. PMID: 35580648
Mol Cancer Ther

A Novel Combination Approach Targeting an Enhanced Protein Synthesis Pathway in MYC-driven (Group 3) Medulloblastoma. [Abstract]

2020 Jun;19(6):1351-1362. PMID: 32371591
Cancer Gene Ther

METTL3-mediated maturation of miR-126-5p promotes ovarian cancer progression via PTEN-mediated PI3K/Akt/mTOR pathway. [Abstract]

2021 Apr;28(3-4):335-349. PMID: 32939058
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
J Mol Cell Cardiol

MicroRNA-223 protects neonatal rat cardiomyocytes and H9c2 cells from hypoxia-induced apoptosis and excessive autophagy via the Akt/mTOR pathway by targeting PARP-1. [Abstract]

2018 May:118:133-146. PMID: 29608885
Molecules

A PI3K Inhibitor with Low Cardiotoxicity and Its Synergistic Inhibitory Effect with Gilteritinib in Acute Myelogenous Leukemia (AML) Cells. [Abstract]

2025 May 27;30(11):2347. PMID: 40509234
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Molecules

Screening of PI3K-Akt-targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. [Abstract]

2019 Apr 1;24(7):1260. PMID: 30939726
Cancers (Basel)

Early Mechanisms of Chemoresistance in Retinoblastoma. [Abstract]

2022 Oct 10;14(19):4966. PMID: 36230889
Sci Rep

Glutamine and serum starvation alters the ATP production, oxidative stress, and abundance of mitochondrial RNAs in extracellular vesicles produced by cancer cells. [Abstract]

2024 Oct 28;14(1):25815. PMID: 39468126
J Biol Chem

The mTOR inhibitor manassantin B reveals a crucial role of mTORC2 signaling in Epstein-Barr virus reactivation. [Abstract]

2020 May 22;295(21):7431-7441. PMID: 32312752
Sci Rep

Drug-induced PD-L1 expression and cell stress response in breast cancer cells can be balanced by drug combination. [Abstract]

2019 Oct 22;9(1):15099. PMID: 31641154
Exp Mol Pathol

NVP-BEZ235 enhances autophagy and ameliorates cognitive deficits by targeting tauopathies. [Abstract]

2025 Jul 24:143:104988. PMID: 40712456
Cell Signal

MEK inhibitor trametinib combined with PI3K/mTOR inhibitor BEZ-235 as an effective strategy against NSCLC through impairment of glucose metabolism. [Abstract]

2024 Sep 16:111415. PMID: 39293743
Front Oncol

FGF1 protects FGFR1-overexpressing cancer cells against drugs targeting tubulin polymerization by activating AKT via two independent mechanisms. [Abstract]

2022 Oct 6:12:1011762. PMID: 36276073
Int J Med Sci

Dual PI3K/mTOR Inhibitor BEZ235 combined with BMS-1166 Promoting Apoptosis in Colorectal Cancer. [Abstract]

2024 Jul 9;21(10):1814-1823. PMID: 39113885
Anim Cells Syst

UCH-L1 and UCH-L3 regulate the cancer stem cell-like properties through PI3 K/Akt signaling pathway in prostate cancer cells. [Abstract]

2021 Oct 11;25(5):312-322. PMID: 34745437
J Orthop Surg Res

Epimedium Brevicornu and Curculigo orchioides inhibit osteoclast autophagy by degrading the level of miRNA-199 to regulate the mTOR signaling pathway. [Abstract]

2025 Jul 9;20(1):631. PMID: 40635043
Oncotargets Ther

The Immunostimulative Effect and Mechanisms of a Novel Mouse Anti-Human PD-1 Monoclonal Antibody on Jurkat Lymphocytic Cells Cocultured with Hepatoma Cells. [Abstract]

2020 Nov 27;13:12225-12241. PMID: 33273828
Onco Targets Ther

FNDC3B, Targeted by miR-125a-5p and miR-217, Promotes the Proliferation and Invasion of Colorectal Cancer Cells via PI3K/mTOR Signaling. [Abstract]

2020 Apr 30;13:3501-3510. PMID: 32431508
Gene

Epigenetic activation of PTEN by valproic acid inhibits PI3K/AKT signaling and Burkitt lymphoma cell growth. [Abstract]

2025 May 20:950:149369. PMID: 40021103
Biomed Res Int

BEZ235 Increases the Sensitivity of Hepatocellular Carcinoma to Sorafenib by Inhibiting PI3K/AKT/mTOR and Inducing Autophagy. [Abstract]

2021 Apr 16:2021:5556306. PMID: 33987439
Biomed Res Int

Study on Biological Characteristics and Mechanism of Paclitaxel Induced Drug Resistance in Endometrial Carcinoma Cells. [Abstract]

2018 Aug 5:2018:8372085. PMID: 30175145

Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2018 Aug 5:2018:8372085. [Abstract]

Changes of p-AKT and p-p70 S6K proteins after treatment with NVP-BEZ235 in Ishikawa and Ishikawa-TAX cells. Changes of p-AKT and p-p70 S6K proteins after treatment of Ishikawa and Ishikawa-TAX cells with NVP-BEZ235.
J Chemother

BEZ235 reduction of cisplatin resistance on wild-type EGFR non-small cell lung cancer cells. [Abstract]

2023 Apr;35(2):95-103. PMID: 35238281
Am J Transl Res

BEZ235 increases sorafenib inhibition of hepatocellular carcinoma cells by suppressing the PI3K/AKT/mTOR pathway. [Abstract]

2019 Sep 15;11(9):5573-5585. PMID: 31632530
bioRxiv

2026 Jun 7.
Res Sq

2026 Jan 9.
Patent

US20210236501A1.
bioRxiv

2024 September 10.
Actome

2024.
Oxid Med Cell Longev

SPP1 Promotes Enzalutamide Resistance and Epithelial-Mesenchymal-Transition Activation in Castration-Resistant Prostate Cancer via PI3K/AKT and ERK1/2 Pathways. [Abstract]

2021 Oct 22:2021:5806602. PMID: 34721759
University of North Carolina

2021.
Oncotarget

Oridonin inhibits aberrant AKT activation in breast cancer. [Abstract]

2018 Feb 1;9(35):23878-23889. PMID: 29844859
Oncotarget

The effect of rapamycin, NVP-BEZ235, aspirin, and metformin on PI3K/AKT/mTOR signaling pathway of PIK3CA-related overgrowth spectrum (PROS). [Abstract]

2017 Jul 11;8(28):45470-45483. PMID: 28525374

Dactolisib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jul 11;8(28):45470-45483. [Abstract]

Activity of PI3K/AKT/mTOR is monitored by examining phosphorylation of AKT-S473, AKT-T308, and S6 by western blotting.
Am J Dig Dis (Madison)

2015;2(2):95-99.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 2 mg/mL (3.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9763 mL

9.8814 mL

19.7628 mL

5 mM

---

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9763 mL	9.8814 mL	19.7628 mL	49.4071 mL

Keywords

Dactolisib hydrochloride

65 Cited Publications

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Dactolisib hydrochloride

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Dactolisib hydrochloride

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (65)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dactolisib hydrochloride Related Classifications

Art. -Nr.: HY-50673A