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Tenalisib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tenalisib图片
CAS NO:1639417-53-0
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 415.42
Formula C23H18FN5O2
CAS No. 1639417-53-0; 1693773-94-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: N/A
Ethanol: N/A
Chemical Name (S)-2-(1-((7H-purin-6-yl)amino)propyl)-3-(3-fluorophenyl)-4H-chromen-4-one
Synonyms RP-6530; RP6530; RP 6530
SMILES Code O=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4NC=NC4=NC=N3)CC)OC5=CC=CC=C15
实验参考方法
In Vitro

In vitro activity: Tenalisib displays 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).


Kinase Assay: 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. RP6530 shows potent inhibitory effect on cancer stem cells in ovarian cancer cell lines. 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. Potent modulation of inflammatory response by RP6530 contributes to control tumor microenvironment.


Cell Assay: 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.

In VivoRP6530 has an excellent pharmacokinetics 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. 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.
Animal modelRats, dogs
Formulation & Dosage3 mg/kg
References Blood 2015 126:1495