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.

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 PI3Kα^E545K or PI3Kα^H1047R 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

641.74

C₃₇H₃₁N₅O₄S

1028385-32-1

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

H₂O : < 0.1 mg/mL (insoluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 50% PEG300    50% saline

  Solubility: 16.67 mg/mL (25.98 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 1 mg/mL (1.56 mM); Clear solution

  此方案可获得 ≥ 1 mg/mL (1.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

Mice: The NVP-Dactolisib (BEZ235) powder is dissolved in NMP on sonication, and the remaining volume of polyethylene glycol 300 is added to a concentration of 5 mg/mL. The application volume is 10 mL/kg. For analytics, frozen tissues are minced and then homogenized in an equal volume of ice-cold PBS and centrifugation, supernatants are analyzed. Samples are then eluted with a linear gradient of 10% to 90% (v/v) acetonitrile in water containing 0.05% (v/v) trifluoroacetic acid over a period of 20 min at a flow rate of 1 mL/min. The compounds are detected by UV absorbance at 340 nm, and concentrations are determined by the external standard method using peak heights^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.