Tenalisib (RP6530)

For research use only.

Catalog No.S8672

Tenalisib (RP6530) Chemical Structure

CAS No. 1639417-53-0

Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.

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Description Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
PI3Kδ [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
24.5 nM 33.2 nM
In vitro

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[1]. RP6530 shows potent inhibitory effect on cancer stem cells in ovarian cancer cell lines[2]. 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[3]. Potent modulation of inflammatory response by RP6530 contributes to control tumor microenvironment[1].

In vivo 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. RP6530 has an excellent pharmacokinetic profile 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[1].


Cell Research:


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  • Cell lines: MM cell lines, namely, MM-1S and MM-1R
  • Concentrations: 1 μM
  • Incubation Time: 72 h
  • Method:

    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.

    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (180.54 mM)
Ethanol 75 mg/mL (180.54 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.42


CAS No. 1639417-53-0
Storage powder
in solvent
Synonyms N/A
Smiles CCC(C1=C(C(=O)C2=CC=CC=C2O1)C3=CC(=CC=C3)F)NC4=NC=NC5=C4NC=N5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03770000 Active not recruiting Drug: Tenalisib|Drug: Romidepsin T Cell Lymphoma Rhizen Pharmaceuticals SA March 12 2019 Phase 1|Phase 2
NCT03471351 Terminated Drug: Tenalisib|Biological: Pembrolizumab Classical Hodgkin Lymphoma Rhizen Pharmaceuticals SA July 18 2018 Phase 1
NCT02567656 Completed Drug: RP6530 Lymphoma T-Cell Peripheral|Lymphoma T-Cell Cutaneous Rhizen Pharmaceuticals SA September 2015 Phase 1
NCT02017613 Completed Drug: RP6530 Lymphoma B-Cell|T-Cell Lymphoma Rhizen Pharmaceuticals SA November 2013 Phase 1

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID