10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Desiccated,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC 50 values of 4, 75, 7, 5 nM for PI3Kα , β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2 .
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 IC 50 s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3Kα E545K or PI3Kα H1047R with IC 50 s 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- cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI 50 of 10 to 12 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 C max of 1.68 μM at 0.5 h and a C 24h of 0.03 μM . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:p110α 4 nM (IC 50 ) p110α-H1047R 4.6 nM (IC 50 ) p110α-E545K 5.7 nM (IC 50 ) p110γ 5 nM (IC 50 ) p110δ 7 nM (IC 50 ) p110β 75 nM (IC 50 ) mTOR 20.7 nM (IC 50 ) mTORC1 mTORC2 Autophagy
| 異性体SMILES | CC1=CC=C(C=C1)S(=O)(=O)O.CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5 |
|---|---|
| 代替CAS番号 | 1028385-32-1 |
| PubChem CID | 49803145 |
| NSC番号 | 753146 |
| 分子量 | 641.74 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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