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Dactolisib Tosylate

Catalog No. T14552 CAS 1028385-32-1

Synonyms: BEZ235 Tosylate, NVP-BEZ 235 Tosylate

Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor that targets PI3K and mTOR. dactolisib Tosylate exhibits IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. dactolisib Tosylate inhibits mTORC1 and mTORC2.

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Dactolisib Tosylate, CAS 1028385-32-1

Pack Size	Availability	Price/USD
25 mg	In stock	$ 42.00
50 mg	In stock	$ 59.00
1 mL * 10 mM (in DMSO)	In stock	$ 65.00

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Purity: 99.85%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor that targets PI3K and mTOR. dactolisib Tosylate exhibits IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. dactolisib Tosylate inhibits mTORC1 and mTORC2.
Targets&IC50	mTOR:20.7 nM, p110α-E545K:5.7 nM, p110α:4 nM, p110γ:5 nM, p110δ:7 nM, p110α-H1047R:4.6 nM, p110β:75 nM
In vitro	Dactolisib (BEZ235) exhibits IC50 values of 4 nM, 75 nM, 7 nM, and 5 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Furthermore, it demonstrates significant activity against mutant forms of PI3Kα, specifically PI3KαE545K and PI3KαH1047R, with IC50 values of 5.7 nM and 4.6 nM, respectively. Treatment with increasing concentrations of Dactolisib (BEZ235) leads to a dose-dependent reduction in cell proliferation in PTEN-null cell lines PC3M and U87MG, with an average GI50 ranging from 10 to 12 nM. Notably, in human tumor cell lines, it effectively and specifically blocks the aberrant activation of the PI3K pathway, leading to G1 arrest.[1]
In vivo	Dactolisib (BEZ235) (50 mg/kg) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM. BEZ235 is well tolerated, and displays disease stasis when administered orally. It enhances the efficacy of other anticancer agents.[1]

Synonyms	BEZ235 Tosylate, NVP-BEZ 235 Tosylate
Molecular Weight	641.74
Formula	C37H31N5O4S
CAS No.	1028385-32-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 0.1 mg/mL (insoluble)

DMSO: 30.6 mg/mL (47.7 mM), Sonification and heating are recommended.

References and Literature

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.

Citations

1. Liu Z, Meng D, Wang J, et al. GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response to paclitaxel by forming a vicious cycle with IGF1/IGF1R signaling pathway. Cell death & disease. 2022, 13(8): 1-12.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Anti-Obesity Compound Library Metabolism Compound Library Bioactive Compounds Library Max

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Keywords

Dactolisib Tosylate 1028385-32-1 PI3K/Akt/mTOR signaling PI3K mTOR BEZ-235 Tosylate BEZ 235 Tosylate BEZ235 Tosylate NVP-BEZ235 Tosylate NVP-BEZ 235 Tosylate NVP-BEZ-235 Tosylate inhibitor inhibit

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