Tel: +86 (0)571 8102-5280 Email:
1028385-32-1 | Dactolisib (Tosylate)

Dactolisib (Tosylate) NLT 98%

SKU : MC502985

CAS Number : 1028385-32-1

Molecular Formula : C37H31N5O4S | Molecular Weight : 641.74

Synonyms : BEZ235 (Tosylate);NVP-BEZ 235 (Tosylate)

Quote Request
Purity NLT 98%
Storage at 20ºC 2 years

* The above information is for reference only.

* If the product has intellectual property rights, a license granted is must or contact us.

Chemical Name Dactolisib (Tosylate)
CAS Number 1028385-32-1
MDL Number MFCD22124509
Molecular Formula C37H31N5O4S
Molecular Weight 641.74
Synonyms BEZ235 (Tosylate);NVP-BEZ 235 (Tosylate)
Introduction of 1028385-32-1 :

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. IC50 & Target: IC50: 4nM (PI3Kα), 75 nM (PI3Kβ), 7 nM (PI3Kγ), 5 nM (PI3Kδ)[1]
mTORC1, mTORC2[1] 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. 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]. In Vivo: Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and 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].

Related Products