An inhibitor of PI3Kα
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BYL719

Item No. 16986

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide
CAS Number
1217486-61-7
Synonyms
  • Alpelisib
  • NVP-BYL719
Molecular Formula
C19H22F3N5O2S
Formula Weight
441.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
317 nm
SMILES
CC(C)(C(F)(F)F)C1=NC=CC(C2=C(C)N=C(NC(N3[C@H](C(N)=O)CCC3)=O)S2)=C1
InChi Code
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1
InChi Key
STUWGJZDJHPWGZ-LBPRGKRZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $32

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    10 mg

    $58

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    25 mg

    $104

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    50 mg

    $128

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    Product Description

    BYL719 is an inhibitor of phosphoinositide 3-kinase α (PI3Kα; IC50s = 4.6, 4, and 4.8 nM for wild-type, E545K mutant, and H1047R mutant PI3K, respectively).1 It is selective for PI3Kα over PI3Kβ, PI3Kδ, PI3Kγ, and PI4Kβ (IC50s = 1,156, 290, 250, and 581 nM, respectively), as well as VPS34, mTOR, DNA-PK, and ATR (IC50s = >9,100 nM for all). BYL719 (12.5, 25, and 50 mg/kg) reduces tumor volume in a PI3Kα-dependent Rat1-myr-p110α mouse xenograft model. It also reduces tumor burden in THP-1 acute myeloid leukemia (AML) and MCF-7 breast cancer mouse xenograft models.2,3 Formulations containing BYL719 have been used in the treatment of advanced or metastatic breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fritsch, C., Huang, A., Chatenay-Rivauday, C., et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol. Cancer Ther. 13(5), 1117-1129 (2014).

    2. Gritsman, K., Yuzugullu, H., Von, T., et al. Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α. J. Clin. Invest. 124(4), 1794-1809 (2014).

    3. Elkabets, M., Vora, S., Juric, D., et al. mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. Sci. Transl. Med. 5(196), 196ra199 (2013).