An inhibitor of PI3Kδ and PI3Kγ
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Tenalisib

Item No. 30949

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(3-fluorophenyl)-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4H-1-benzopyran-4-one
CAS Number
1639417-53-0
Synonyms
  • RP 6530
Molecular Formula
C23H18FN5O2
Formula Weight
415.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C(C2=CC=CC(F)=C2)=C([C@H](CC)NC3=C4C(N=CN4)=NC=N3)OC5=CC=CC=C51
InChi Code
InChI=1S/C23H18FN5O2/c1-2-16(29-23-19-22(26-11-25-19)27-12-28-23)21-18(13-6-5-7-14(24)10-13)20(30)15-8-3-4-9-17(15)31-21/h3-12,16H,2H2,1H3,(H2,25,26,27,28,29)/t16-/m0/s1
InChi Key
HDXDQPRPFRKGKZ-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

    $149

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    50 mg

    $413

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    100 mg

    $578

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    Product Description

    Tenalisib is an inhibitor of PI3Kδ and PI3Kγ (IC50s = 24.5 and 33.2 nM, respectively).1 It is greater than 300- and 120-fold selective for PI3Kδ and PI3Kγ, respectively, over PI3Kα and PI3Kβ. Tenalisib (10 µM) induces cell death in L-540, KM-H2, and L-428 Hodgkin lymphoma cells. It induces cell cycle arrest at the G0/G1 phase in the same cells. In vivo, tenalisib reduces tumor growth and vasculature, induces tumor necrosis, and induces the M1 phenotype in tumor-associated macrophages (TAMs) in an L-540 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Locatelli, S.L., Careddu, G., Serio, S., et al. Targeting cancer cells and tumor microenvironment in preclinical and clinical models of hodgkin lymphoma using the dual PI3Kδ/γ inhibitor RP6530. Clin. Cancer Res. 25(3), 1098-1112 (2019).