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Tenalisib (RP6530) (RP6530) is a potent and selective inhibitor of PI3Kδ and PI3Kγ(IC50 values of 25 and 33 nM, respectively.)
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
2 mg | $45 | In Stock | |
5 mg | $74 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $320 | In Stock | |
100 mg | $482 | In Stock | |
1 mL x 10 mM (in DMSO) | $81 | In Stock |
Description | Tenalisib (RP6530) (RP6530) is a potent and selective inhibitor of PI3Kδ and PI3Kγ(IC50 values of 25 and 33 nM, respectively.) |
Targets&IC50 | PI3Kδ:25 nM, PI3Kγ:33 nM |
In vitro | In both HEL-RS and HEL-RR cells, Tenalisib exhibits modest proliferation inhibition (33-46% inhibition @ 10 μM). 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. |
In vivo | Single agent(Tenalisib) activity is evident in difficult-to-treat subjects at ≥ 200 mg BID[2]. |
Alias | RP6530 |
Molecular Weight | 415.42 |
Formula | C23H18FN5O2 |
Cas No. | 1639417-53-0 |
Smiles | CC[C@H](Nc1ncnc2nc[nH]c12)c1oc2ccccc2c(=O)c1-c1cccc(F)c1 |
Relative Density. | 1.434 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (240.72 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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