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Tenalisib

Cat. No. M7538
Tenalisib Structure
Synonym:

RP6530

Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 340 In stock
25mg USD 700 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. 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.

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.

Protocol
Cell Experiment
Cell lines MM cell lines, namely, MM-1S and MM-1R
Preparation 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.
Concentrations 1 μM
Incubation time 72 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 415.42
Formula C23H18FN5O2
CAS Number 1639417-53-0
Purity >98%
Solubility 75 mg/mL in DMSO
Storage at -20°C
References

Dual PI3Kδ/γ Inhibition By RP6530 Induces Apoptosis and Cytotoxicity In B-Lymphoma Cells
Swaroop Vakkalanka, et al. Blood 2013;122:4411.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tenalisib, RP6530 supplier, PI3K, inhibitors

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