A class I PI3K inhibitor
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XL147

Item No. 18011

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-amino-N-[3-[[[3-[(2-chloro-5-methoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-2-methyl-propanamide
CAS Number
934526-89-3
Synonyms
  • Pilaralisib
  • SAR245408
Molecular Formula
C25H25ClN6O4S
Formula Weight
541.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:30): 0.03 mg/ml
λmax
237, 272, 369 nm
SMILES
COC1=CC(NC2=NC3=CC=CC=C3N=C2NS(C4=CC=CC(NC(C(C)(N)C)=O)=C4)(=O)=O)=C(Cl)C=C1
InChi Code
InChI=1S/C25H25ClN6O4S/c1-25(2,27)24(33)28-15-7-6-8-17(13-15)37(34,35)32-23-22(29-19-9-4-5-10-20(19)30-23)31-21-14-16(36-3)11-12-18(21)26/h4-14H,27H2,1-3H3,(H,28,33)(H,29,31)(H,30,32)
InChi Key
QINPEPAQOBZPOF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $169

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    25 mg

    $356

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    Product Description

    XL147 is an inhibitor of class I PI3Ks (IC50s = 0.039, 0.036, 0.023, and 0.383 µM for p110α, -δ, -γ, and -β, respectively).1 It is selective for class I PI3Ks over the class III PI3K vacuolar protein sorting 34 (Vps34; IC50 = 6.974 µM), as well as DNA protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC50s = 4.75 and >15 µM, respectively). XL147 inhibits the proliferation of MCF-7 breast and PC3 prostate cancer cells (IC50s = 9.669 and 16.492 µM, respectively). It reduces tumor growth in a BT474 breast cancer mouse xenograft model when administered alone or in combination with trastuzumab or lapatinib (Item No. 11493).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Foster, P., Yamaguchi, K., Hsu, P.P., et al. The selective PI3K inhibitor XL147 (SAR245408) inhibits tumor growth and survival and potentiates the activity of chemotherapeutic agents in preclinical tumor models. Mol. Cancer Ther. 14(4), 931-940 (2015).

    2. Chakrabarty, A., Sánchez, V., Kuba, M.G., et al. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc. Natl. Acad. Sci. USA 109(8), 2718-2723 (2012).