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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 an inhibitor of dual PI3K and mTOR kinase(IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively). Dactolisib Tosylate also inhibits mTORC1 and mTORC2.

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Dactolisib Tosylate, CAS 1028385-32-1

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Dactolisib Tosylate (BEZ235 Tosylate) is an inhibitor of dual PI3K and mTOR kinase(IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively). Dactolisib Tosylate also inhibits mTORC1 and mTORC2.
Targets&IC50	p110α:4 nM, p110α-E545K:5.7 nM, mTOR:20.7 nM, p110γ:5 nM, p110β:75 nM, p110α-H1047R:4.6 nM, p110δ:7 nM
In vitro	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, and it is also found to be as active against the mutant PI3KαE545K or PI3KαH1047R with IC50s of 5.7 and 4.6 nM, respectively. 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]. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest.
In vivo	Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally. It enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a Cmax of 1.68 μM at 0.5 h and a C24h of 0.03 μM[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 2 years

Solubility Information

DMSO: 34 mg/mL (52.98 mM), Need ultrasonic and warming

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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.

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Keywords

Dactolisib Tosylate 1028385-32-1 PI3K/Akt/mTOR信号通路自噬 mTOR Autophagy PI3K BEZ235 Tosylate NVP-BEZ 235 Tosylate Inhibitor inhibitor inhibit

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