Home PI3K/Akt/mTOR PI3K inhibitor Tenalisib For research use only.

Tenalisib

Synonyms: RP6530

Tenalisib 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.

Tenalisib Chemical Structure

Tenalisib Chemical Structure

CAS No. 1639417-53-0

Purity & Quality Control

Tenalisib Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Biological Activity

Description Tenalisib 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.
Targets
PI3Kδ [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)
24.5 nM 33.2 nM
In vitro
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].
Cell Research 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.
In Vivo
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06189209 Recruiting
Triple Negative Breast Cancer (TNBC)
Rhizen Pharmaceuticals SA|Incozen Therapeutics Pvt Ltd
 March 4 2024 Phase 2
NCT03770000 Completed
T Cell Lymphoma
Rhizen Pharmaceuticals SA
 March 12 2019 Phase 1|Phase 2
NCT03471351 Terminated
Classical Hodgkin Lymphoma
Rhizen Pharmaceuticals SA
 July 18 2018 Phase 1
NCT02567656 Completed
Lymphoma T-Cell Peripheral|Lymphoma T-Cell Cutaneous
Rhizen Pharmaceuticals SA
 September 2015 Phase 1
NCT02017613 Completed
Lymphoma B-Cell|T-Cell Lymphoma
Rhizen Pharmaceuticals SA
 November 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 415.42 Formula

C23H18FN5O2
CAS No. 1639417-53-0 SDF --
Smiles CCC(C1=C(C(=O)C2=CC=CC=C2O1)C3=CC(=CC=C3)F)NC4=NC=NC5=C4NC=N5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (120.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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