1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETenalisibCat. No.: HY-17645CAS No.: 1639417-53-0Synonyms: RP6530分式: CHFNO分量: 415.42作靶點: PI3K作通路: PI3K/Akt/mTOR儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg/mL (240.72 mM)* means so

2、luble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4072 mL 12.0360 mL 24.0720 mL5 mM 0.4814 mL 2.4072 mL 4.8144 mL10 mM 0.2407 mL 1.2036 mL 2.4072 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配

3、，當天使；澄清的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.02 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.02 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE

4、3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.02 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tenalisib (RP6530)新穎，效，選擇性的PI3K和PI3K抑制劑，IC50值分別為25和33 nM。IC50 & Target PI3K PI3K25 nM (IC50) 33 nM (IC50)體外研究 Tenalisib shows selectivity over PI3K (300-fold) and (100-fold) isoforms. Tenalisib e

5、xhibits modestproliferation inhibition (33-46% inhibition 10 M) in both HEL-RS and HEL-RR cells. Addition of 10 Mtenalisib to ruxolitinib is synergistic resulting in a near-complete inhibition of proliferation (90% for HEL-RSand 70% for HEL-RR). Addition of 5 M tenalisib, 4 h prior to the addition o

6、f ruxolitinib results in a significantreduction in EC50of ruxolitinib (5.8 M) in HEL-RR cells. Incubation of 10 M tenalisib with ruxolitinib for 72 hincreases the percent of apoptotic cells (55% in HEL-RS and 37% in HEL-RR) compared to either agentalone (16-27% in HEL-RS and 17-21% in HEL-RR) 1.體內研究

7、 Tenalisib has been well tolerated in subjects with heavily pre-treated relapsed/refractory hematologicmalignancies. Reported toxicities are manageable with no DLTs. Single agent activity is evident in difficult-to-treat subjects at 200 mg BID 2.戶使本產品發表的科研獻 Exp Ther Med. 2018 Feb;15(2):1225-1232.See

8、 more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Vakkalanka S, et al. RP6530, a dual PI3K / inhibitor, potentiates ruxolitinib activity in the JAK2-V617F mutant erythroleukemia celllines. abstract. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer R

9、esearch; 2015 Apr 18-22;Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2704. doi:10.1158/1538-7445.AM2015-27042. Carmelo C, et al. A Dose Escalation Study of RP6530, a Novel Dual PI3K Delta/Gamma Inhibitor, in Patients with Relapsed/RefractoryHematologic Malignancies. Blood 2015 126:1495;McePdfHeightCaution: Product has not been fully validated for medi