An inhibitor of class I PI3K isoforms
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CH5132799

Item No. 26410

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[6,7-dihydro-7-(methylsulfonyl)-2-(4-morpholinyl)-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-pyrimidinamine
CAS Number
1007207-67-1
Molecular Formula
C15H19N7O3S
Formula Weight
377.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 12 mg/mL
λmax
276, 337 nm
SMILES
NC(N=C1)=NC=C1C2=NC(N3CCOCC3)=NC4=C2CCN4S(C)(=O)=O
InChi Code
InChI=1S/C15H19N7O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21/h8-9H,2-7H2,1H3,(H2,16,17,18)
InChi Key
JEGHXKRHKHPBJD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $218

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    10 mg

    $371

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    25 mg

    $763

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    50 mg

    $981

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    Product Description

    CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively).1 It is selective for these PI3K isoforms over PI3KC2α and PI3KC2β, which are class II PI3Ks, Vps34, a class III PI3K, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM). CH5132799 inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cancer cells expressing the activating mutation PI3KαH1047R (IC50s = 200, 32, 56, and 120 nM, respectively). It also reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 25 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ohwada, J., Ebiike, H., Kawada, H., et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg. Med. Chem. Lett. 21(6), 1767-1772 (2011).