A PI3Kδ inhibitor
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Roginolisib

Item No. 44445

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[6-fluoro-1,4-dihydro-1-[4-(4-morpholinylmethyl)phenyl]-5,5-dioxido[1]benzothiopyrano[4,3-c]pyrazol-3-yl]-4-morpholinyl-methanone
CAS Number
1305267-37-1
Synonyms
  • IOA-244
  • MSC2360844
Molecular Formula
C26H27FN4O5S
Formula Weight
526.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/ml
SMILES
O=S1(CC2=C(N(C3=CC=C(CN4CCOCC4)C=C3)N=C2C(N5CCOCC5)=O)C6=C1C(F)=CC=C6)=O
InChi Code
InChI=1S/C26H27FN4O5S/c27-22-3-1-2-20-24-21(17-37(33,34)25(20)22)23(26(32)30-10-14-36-15-11-30)28-31(24)19-6-4-18(5-7-19)16-29-8-12-35-13-9-29/h1-7H,8-17H2
InChi Key
NFHSJYKXENYICE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $215

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    10 mg

    $366

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    25 mg

    $699

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    50 mg

    $1,183

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    Product Description

    Roginolisib is an inhibitor of PI3Kδ (IC50 = 0.019 µM).1 It is selective for PI3Kδ over PI3Kα, PI3Kβ, PI3Kγ, VPS34, and PI3KC2β (IC50s = 0.43, 1.5, 10.3, 5.6, and 5.9 µM, respectively). Roginolisib inhibits the growth of SU-DHL-6 B cell lymphoma cells that endogenously express PI3Kδ (GI50 = 0.24 µM) but not cancer cell lines endogenously expressing PI3Kα, PI3Kβ, or PI3Kγ. In vivo, roginolisib (30 mg/kg twice daily) alone or in combination with an anti-PD-1 antibody slows tumor growth and decreases tumor volume in a murine Lewis lung carcinoma model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Johnson, Z., Tarantelli, C., Civanelli, E., et al. IOA-244 is a non-ATP-competitive, highly selective, tolerable PI3K delta inhibitor that targets solid tumors and breaks immune tolerance. Cancer Res. Commun. 3(4), 576-591 (2023).