Tenalisib | MedChemExpress (MCE)-产品咨询-资讯-生物在线

Tenalisib | MedChemExpress (MCE)

作者:MedChemExpress LLC 暂无发布时间 (访问量:971)

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Tenalisib

CAS No. : 1639417-53-0

MCE 国际站:Tenalisib

产品活性:Tenalisib (RP6530)是新颖,高效,选择性的PI3KδPI3Kγ抑制剂,IC50值分别为25和33 nM。

研究领域:PI3K/Akt/mTOR

作用靶点:PI3K

In Vitro: Tenalisib shows selectivity over PI3K α (>300-fold) and β (>100-fold) isoforms. Tenalisib exhibits modest proliferation inhibition (33-46% inhibition @ 10 μM) in both HEL-RS and HEL-RR cells. Addition of 10 μM tenalisib to ruxolitinib is synergistic resulting in a near-complete inhibition of proliferation (>90% for HEL-RS and >70% for HEL-RR). Addition of 5 μM tenalisib, 4 h prior to the addition of ruxolitinib results in a significant reduction in EC50of ruxolitinib (5.8 μM) in HEL-RR cells. Incubation of 10 μM tenalisib with ruxolitinib for 72 h increases the percent of apoptotic cells (55% in HEL-RS and 37% in HEL-RR) compared to either agent alone (16-27% in HEL-RS and 17-21% in HEL-RR).

In Vivo: Tenalisib has been well tolerated in subjects with heavily pre-treated relapsed/refractory hematologic malignancies. Reported toxicities are manageable with no DLTs. Single agent activity is evident in difficult-to-treat subjects at ≥ 200 mg BID.

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