Tenalisib

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Chemical Structure| 1639417-53-0 同义名 : RP6530
CAS号 : 1639417-53-0
货号 : A183178
分子式 : C23H18FN5O2
纯度 : 98%
分子量 : 415.42
MDL号 : MFCD28502205
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(252.76 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:33.2 nM

  • p110δ

    PI3Kδ, IC50:24.5 nM
描述 Tenalisib is characterized by its preferential action against the α (>300-fold) and β (>100-fold) isoforms of PI3K. It moderately inhibits cell proliferation (33-46% @ 10 μM) in both HEL-RS and HEL-RR cell lines. A synergistic effect is observed when 10 μM of tenalisib is combined with ruxolitinib, leading to almost complete proliferation inhibition (>90% for HEL-RS and >70% for HEL-RR). Pre-treating with 5 μM of tenalisib 4 hours before adding ruxolitinib significantly decreases the EC50 for ruxolitinib to 5.8 μM in HEL-RR cells. A 72-hour incubation of 10 μM tenalisib with ruxolitinib enhances apoptotic cell percentage (55% in HEL-RS and 37% in HEL-RR) compared to the use of each drug alone (16-27% in HEL-RS and 17-21% in HEL-RR)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.04mL

2.41mL

1.20mL

24.07mL

4.81mL

2.41mL
参考文献

[1]Vakkalanka S, et al. RP6530, a dual PI3K δ/γ inhibitor, potentiates ruxolitinib activity in the JAK2-V617F mutant erythroleukemia cell lines. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr

[2]Carmelo C, et al. A Dose Escalation Study of RP6530, a Novel Dual PI3K Delta/Gamma Inhibitor, in Patients with Relapsed/Refractory Hematologic Malignancies. Blood 2015 126:1495;