Tenalisib

製品コードS8672 バッチS867203

印刷

化学情報

Chemical Structure Synonyms RP6530 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H18FN5O2
分子量 415.42 CAS No. 1639417-53-0
Solubility (25°C)* 体外 DMSO 25 mg/mL (60.18 mM)
Ethanol 25 mg/mL (60.18 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.31mg/ml Taking the 1 mL working solution as an example, add 50 μL of 6.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.625mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
in vitro RP6530 is a specific dual PI3K δ/γ inhibitor exhibiting several-fold selectivity against the other PI3K isoforms and 245-kinases. RP6530 causes a dose-dependent inhibition (>50% @ 2-7 μM) in growth of immortalized (Raji, TOLEDO, KG-1, JEKO, REC-1) B-cell lymphoma cells. Effect is more pronounced in the DLBCL cell lines, OCI-LY-1 and OCI-LY-10 (>50% inhibition @ 0.1-0.7 μM), and the reduction in viability is accompanied by corresponding inhibition of pAKT with EC50 of 6 & 70 nM respectively. Treatment of patient-derived primary cells with 4 µM RP6530 causes an increase in cell death. Cells in early apotosis (Annexin V+/PI-) are not different between the DMSO blank and RP6530 samples[1]. RP6530 shows potent inhibitory effect on cancer stem cells in ovarian cancer cell lines[2]. Treatment with 1 μM RP6530 results in G2/M arrest in MM-1S and MM-1R lines with very few cells in the SubG0 phase. It also results in a 70−90% inhibition of pAKT in MM-1S and MM-1R cell lines[3]. Potent modulation of inflammatory response by RP6530 contributes to control tumor microenvironment[1].
in vivo The predicted T1/2, Cmax, and AUC0-t at 10 mg dose in human are 9.5 h, 14.0 μM, and 342.0 μM respectively. RP6530 has an excellent pharmacokinetic profile with plasma concentrations reaching well above the EC75 at doses as low as 3 mg/kg in rat and dog for 6-12 h. In addition, RP6530 shows >70 and >100% oral bioavailability with a half-life of 2 and 3 h in rat and dog respectively[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MM cell lines, namely, MM-1S and MM-1R
濃度 1 μM
反応時間 72 h
実験の流れ

Potential of the combination (1 μM RP6530 + BORT between 0.1 nM and 1 μM) is studied in MM cell lines, namely, MM-1S and MM-1R. Proliferation is determined by a MTT assay after incubating with compound for 72 h at 37ºC. Apoptotic potential of the combination is estimated by AnnexinV/PI staining.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。