Dactolisib Tosylate
Based on 73 publication(s) in Google Scholar
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.87%
- CAS 番号: 1028385-32-1
- 分子式: C37H31N5O4S
- 分子量:641.74
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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HY-10422
AZD-8055mTOR Inhibitor -
HY-70063
BuparlisibPI3K Inhibitor -
HY-15244
AlpelisibPI3Kα Inhibitor -
HY-12046
PIK-93Virus Protease Inhibitor -
HY-13328
SapanisertibmTORC1/mTORC2 Inhibitor -
HY-15346
CopanlisibPI3K Inhibitor -
HY-50673
DactolisibPI3K/mTOR Inhibitor -
HY-10474
TorkinibmTOR Inhibitor -
HY-15247
VistusertibmTORC Inhibitor -
HY-19962
PaxalisibPI3K/mTOR Inhibitor -
HY-50094
PictilisibPI3Kα/δ Inhibitor -
HY-13003
Torin 1mTOR Inhibitor
MedChemExpress（MCE）の使用を引用している文献 Dactolisib Tosylate
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Nature. 2018 Aug;560(7719):499-503. [Abstract]
- Cell. 2026 Oct 29;189(22):6951-6967.e12.
- Cell. 2025 Dec 11;188(25):7155-7174.e25. [Abstract]
- Cell Res. 2019 Nov;29(11):895-910. [Abstract]
- Blood. 2019 Oct 17;134(16):1323-1336. [Abstract]
- Cancer Res. 2025 Jan 2;85(1):32-51. [Abstract]
- Nat Commun. 2025 Dec 15. [Abstract]
- Nat Commun. 2017 Jun 8:8:15617. [Abstract]
- Exp Hematol Oncol. 2016 Jul 29:5:22. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Nanobiotechnology. 2022 Apr 12;20(1):187. [Abstract]
- J Exp Clin Cancer Res. 2018 Aug 9;37(1):188. [Abstract]
- Adv Sci (Weinh). 2025 Aug 19:e05656. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(24):e2300881. [Abstract]
- Sci Adv. 2023 Mar 22;9(12):eadd5028. [Abstract]
- Cell Death Dis. 2026 Jun 16. [Abstract]
- Cell Death Dis. 2020 Jun 30;11(6):491. [Abstract]
- Cell Commun Signal. 2023 May 24;21(1):120. [Abstract]
- EBioMedicine. 2015 Nov 19;2(12):1944-56. [Abstract]
- NPJ Precis Oncol. 2025 Nov 21;9(1):373. [Abstract]
- Leukemia. 2025 Dec 19. [Abstract]
- Leukemia. 2014 Sep;28(9):1819-27. [Abstract]
- BMC Med. 2021 Oct 15;19(1):247. [Abstract]
- Haematologica. 2020 Mar;105(3):674-686. [Abstract]
- Br J Cancer. 2022 Jul;127(1):30-42. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cancer Cell Int. 2023 Sep 27;23(1):217. [Abstract]
- Sci Signal. 2021 Jun 22;14(688):eabe6156. [Abstract]
- Mol Cancer Ther. 2020 Jun;19(6):1351-1362. [Abstract]
- JCI Insight. 2022 Aug 22;7(16):e155899. [Abstract]
- Eur J Med Chem. 2023 Oct 5:258:115543. [Abstract]
- Biochem Pharmacol. 2022 Jul:201:115093. [Abstract]
- Cancer Gene Ther. 2021 Apr;28(3-4):335-349. [Abstract]
- Front Pharmacol. 2020 Nov 11:11:580407. [Abstract]
- Molecules. 2025 May 27;30(11):2347. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Molecules. 2019 Apr 1;24(7):1260. [Abstract]
- Sci Rep. 2024 Oct 28;14(1):25815. [Abstract]
- Sci Rep. 2019 Oct 22;9(1):15099. [Abstract]
- J Mol Cell Cardiol. 2018 May:118:133-146. [Abstract]
- Cancers (Basel). 2022 Oct 10;14(19):4966. [Abstract]
- Cell Signal. 2024 Dec:124:111415. [Abstract]
- Exp Mol Pathol. 2025 Jul 24:143:104988. [Abstract]
- J Biol Chem. 2020 May 22;295(21):7431-7441. [Abstract]
- J Orthop Surg Res. 2025 Jul 9;20(1):631. [Abstract]
- Int J Med Sci. 2024 Jul 9;21(10):1814-1823. [Abstract]
- Anim Cells Syst. 2021 Oct 11;25(5):312-322. [Abstract]
- Arch Pharm (Weinheim). 2024 Sep;357(9):e2400066. [Abstract]
- Front Oncol. 2022 Oct 6:12:1011762. [Abstract]
- Kaohsiung J Med Sci. 2026 Jun 1:e70235. [Abstract]
- Biomed Res Int. 2021 Apr 16:2021:5556306. [Abstract]
- Biomed Res Int. 2018 Aug 5:2018:8372085. [Abstract]
- Gene. 2025 May 20:950:149369. [Abstract]
- Onco Targets Ther. 2020 Nov 27:13:12225-12241. [Abstract]
- Onco Targets Ther. 2020 Apr 30:13:3501-3510. [Abstract]
- J Chemother. 2023 Apr;35(2):95-103. [Abstract]
- Am J Transl Res. 2019 Sep 15;11(9):5573-5585. [Abstract]
- SSRN. 2026 Aug 1.
- bioRxiv. 2026 Jun 7.
- Res Sq. 2026 Jan 9.
- Patent. US20210236501A1.
- Actome. 2024.
- bioRxiv. 2024 September 10.
- Oxid Med Cell Longev. 2021 Oct 22:2021:5806602. [Abstract]
- University of North Carolina. 2021.
- Oncotarget. 2018 Feb 1;9(35):23878-23889. [Abstract]
- Oncotarget. 2017 Jul 11;8(28):45470-45483. [Abstract]
- Am J Dig Dis (Madison). 2015;2(2):95-99.
- J Clin Toxicol. 2014 October 4, 4:5.
- J Clin Toxicol 2014, 4:5
Customer Validation & Images
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生物活性
製品説明
IC50 & Target
[1]|
p110α 4 nM (IC50) |
p110α-H1047R 4.6 nM (IC50) |
p110α-E545K 5.7 nM (IC50) |
p110γ 5 nM (IC50) |
p110δ 7 nM (IC50) |
p110β 75 nM (IC50) |
mTOR 20.7 nM (IC50) |
mTORC1 |
mTORC2 |
Autophagy |
体外実験
Dactolisib (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC50s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI50 of 10 to 12 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1028385-32-1
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性状 Solid
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分子量 641.74
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分子式 C37H31N5O4S
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Color Off-white to light yellow
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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.CC7=CC=C(S(=O)(O)=O)C=C7
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別名
BEZ235 Tosylate; NVP-BEZ 235 Tosylate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (73)
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Journal Impact Factor
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Most Recent
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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
2018 Aug;560(7719):499-503. PMID: 30051890 -
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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
2025 Dec 15. PMID: 41397976 -
Nat Commun
2017 Jun 8:8:15617. PMID: 28593995
Dactolisib Tosylate 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).
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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 -
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 -
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 -
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 Tosylate 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.
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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 -
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 -
Cell Death Dis
Pictilisib and nutrient stress synergize to induce methuosis via PI(4,5)P2-dependent macropinocytic dysregulation in cancer cells. [Abstract]2026 Jun 16. PMID: 42303628 -
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 -
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 -
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 -
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 Tosylate 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.
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BMC Med
HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]2021 Oct 15;19(1):247. PMID: 34649530 -
Haematologica
2020 Mar;105(3):674-686. PMID: 31289206 -
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 -
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 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
Cancers (Basel)
2022 Oct 10;14(19):4966. PMID: 36230889 -
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 Dec:124:111415. PMID: 39293743 -
Exp Mol Pathol
NVP-BEZ235 enhances autophagy and ameliorates cognitive deficits by targeting tauopathies. [Abstract]2025 Jul 24:143:104988. PMID: 40712456 -
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 -
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 -
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 -
Arch Pharm (Weinheim)
Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]2024 Sep;357(9):e2400066. PMID: 38809025 -
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 -
Kaohsiung J Med Sci
WDR72 Drives Esophageal Squamous Cell Carcinoma Progression by Inhibiting Autophagy via the PI3K/Akt/mTOR Pathway. [Abstract]2026 Jun 1:e70235. PMID: 42224092 -
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 Tosylate 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.
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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 -
Onco Targets 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 -
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 -
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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 -
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Oncotarget
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 Tosylate 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.
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J Clin Toxicol 2014, 4:5
溶剤 & 溶解度
体外:
DMSO : 31.82 mg/mL (49.58 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)
H2O : < 0.1 mg/mL (insoluble)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 16.67 mg/mL (25.98 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5583 mL | 7.7913 mL | 15.5826 mL | 38.9566 mL |
| 5 mM | 0.3117 mL | 1.5583 mL | 3.1165 mL | 7.7913 mL | |
| 10 mM | 0.1558 mL | 0.7791 mL | 1.5583 mL | 3.8957 mL | |
| 15 mM | 0.1039 mL | 0.5194 mL | 1.0388 mL | 2.5971 mL | |
| 20 mM | 0.0779 mL | 0.3896 mL | 0.7791 mL | 1.9478 mL | |
| 25 mM | 0.0623 mL | 0.3117 mL | 0.6233 mL | 1.5583 mL | |
| 30 mM | 0.0519 mL | 0.2597 mL | 0.5194 mL | 1.2986 mL | |
| 40 mM | 0.0390 mL | 0.1948 mL | 0.3896 mL | 0.9739 mL |
Dactolisib Tosylate 関連分類
HY-15174 関連分類
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