PI3KΔ和PI3KΓ抑制剂(TENALISIB)
Tenalisib
CAS: 1639417-53-0
Molecular Formula: C23H18FN5O2
PI3KΔ和PI3KΓ抑制剂(TENALISIB) - Names and Identifiers
| Name | Tenalisib |
| Synonyms | RP6530 RP-6530 RP6530 RP 6530 Tenalisib RP6530, Tenalisib Tenalisib (RP6530) 4H-1-Benzopyran-4-one, 3-(3-fluorophenyl)-2-[(1S)-1-(9H-purin-6-ylamino)propyl]- |
| CAS | 1639417-53-0 |
PI3KΔ和PI3KΓ抑制剂(TENALISIB) - Physico-chemical Properties
| Molecular Formula | C23H18FN5O2 |
| Molar Mass | 415.42 |
| Density | 1.434±0.06 g/cm3(Predicted) |
| Boling Point | 706.1±60.0 °C(Predicted) |
| Solubility | DMSO |
| pKa | 10.06±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | RP6530 is a specific dual PI3K δ/γ inhibitor that is several-fold more selective than other PI3K subtypes and 245 kinases. RP6530 inhibits the growth of immortalized B- cell lymphoma cells (Raji, TOLEDO, KG-1, JEKO, REC-1) in a concentration-dependent manner. Its cytostatic effect is more prominent in the DLBCL cell lines OCI-LY-1 and OCI-LY-10: the reduction of its cell viability by RP6530 is usually accompanied by inhibition of pAKT, with EC50 of 6 and 70 nM, respectively. Treatment of patient-derived primary cells at 4 µm RP6530 resulted in increased cell death. Treatment with RP6530 had no effect on early cell apoptosis. RP6530 has potent inhibitory effect on cancer stem cells in ovarian cancer cells. Treatment of MM-1S and MM1-R cells with 1 μm RP6530 resulted in cell cycle arrest at G2/M, while very few cells were in SubG0 phase. It also causes a 70-90% reduction in pAKT levels in MM-1S and MM-1R cells. The effective regulation of RP6530 on inflammatory response can be involved in the regulation of tumor microenvironment. |
| In vivo study | In humans, the predicted T1/2, Cmax, and AUC0-t of RP6530 at a dose of 10 mg are 9.5 h, 14.0 μm, and 342.0 μm, respectively. In rats and dogs, administered at a dose of 3 mg/kg, RP6530 had a good pharmacokinetic profile 6-12 H after administration, with higher blood concentrations than E75. In addition, the oral bioavailability of RP6530 is greater than 70% and greater than 100 in rats and dogs, respectively, with half-lives of 2 hours and 3 hours, respectively. |
PI3KΔ和PI3KΓ抑制剂(TENALISIB) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.407 ml | 12.036 ml | 24.072 ml |
| 5 mM | 0.481 ml | 2.407 ml | 4.814 ml |
| 10 mM | 0.241 ml | 1.204 ml | 2.407 ml |
| 5 mM | 0.048 ml | 0.241 ml | 0.481 ml |
Last Update：2024-01-02 23:10:35
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Tel: 609-228-6898
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CAS: 1639417-53-0
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