Alpelisib (BLY-719; Piqray; NVP-BYL719)

Alias: Alpelisib; NVP-BYL-719; NVP-BYL719; NVP-BYL 719; BYL-719; BYL719; BYL 719
Cat No.:V0114 Purity: ≥98%
Alpelisib (formerly also known as BLY719; trade name: Piqray) is a novel, potent, newly approved, orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with antineoplastic activity.
Alpelisib (BLY-719; Piqray; NVP-BYL719) Chemical Structure CAS No.: 1217486-61-7
Product category: PI3K
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
25mg
50mg
100mg
250mg
500mg
1g
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Other Forms of Alpelisib (BLY-719; Piqray; NVP-BYL719):

  • Alpelisib hydrochloride (BLY719; Piqray)
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: =100%

Purity: ≥98%

Purity: ≥98%

Product Description

Alpelisib (formerly also known as BLY719; trade name: Piqray) is a novel, potent, newly approved, orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with antineoplastic activity. As of May 2019, the FDA has approved it as the first PI3K inhibitor to treat postmenopausal women and men with hormone receptor (HR) positive, human epidermal growth factor receptor 2 (HER2) negative, PIK3CA-mutated, advanced or metastatic breast cancer following progression on or after an endocrine-based regimen. BYL719, a PI3K inhibitor, specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, preventing the PI3K signaling pathway from being activated. In populations of susceptible tumor cells, this may prevent tumor cell growth and survival. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may be a factor in the tumors' resistance to various anti-cancer medications. Clinical evidence indicates that BYL719 has a manageable safety profile with a disabler.

Biological Activity I Assay Protocols (From Reference)
Targets
p110α (IC50 = 5 nM); p110γ (IC50 = 250 nM); p110δ (IC50 = 290 nM); p110β (IC50 = 1200 nM); p110α-H1047R (IC50 = 4 nM); p110α-E545K (IC50 = 4 nM)
ln Vitro
BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway.
ln vivo
In PIK3CA mutant xenograft models in rodents, BYL719 (>270 mg/d) demonstrates statistically significant dose-dependent anti-tumor efficacy. BYL719 has a low half-life of 8.5 hours, a low inter-individual variability in Cmax, and an exposure that increases dose proportionally between 30 mg/d and 450 mg/d in humans. First indications of clinical efficacy for BYL719 (270 mg/d) include 1 confirmed partial response in a patient with ER+ breast cancer and significant PET responses (PMR) and/or tumor shrinkage in 8 of the 17 patients evaluated.
Enzyme Assay
Alpelisib (NVP-BYL719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50~4 nM). Alpelisib (NVP-BYL719) potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74±15 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα).
Cell Assay
Alpelisib (0–1000 nM) was applied to cells in escalating concentrations for 72 hours. Using the CyQuant assay, cell viability was measured.
Animal Protocol
Female athymic nu/nu mice
40 mg/kg
o.g.
References

[1]. Cancer Cell . 2021 Aug 9;39(8):1099-1114.e8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H22F3N5O2S
Molecular Weight
441.47
Exact Mass
441.14463
Elemental Analysis
C, 51.69; H, 5.02; F, 12.91; N, 15.86; O, 7.25; S, 7.26
CAS #
1217486-61-7
Appearance
white solid powder
SMILES
CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
InChi Key
STUWGJZDJHPWGZ-LBPRGKRZSA-N
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
Chemical Name
(2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
Synonyms
Alpelisib; NVP-BYL-719; NVP-BYL719; NVP-BYL 719; BYL-719; BYL719; BYL 719
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~88 mg/mL (~199.3 mM)
Water: 2 mg/mL (~4.5 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
30% PEG400+0.5% Tween80+5%Propylene glycol: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2652 mL 11.3258 mL 22.6516 mL
5 mM 0.4530 mL 2.2652 mL 4.5303 mL
10 mM 0.2265 mL 1.1326 mL 2.2652 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Clinical Trial Information
NCT Number Status Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03056755 Active
Recruiting
Drug: Alpelisib
Drug: Fulvestrant
Breast Cancer Novartis Pharmaceuticals August 14, 2017 Phase 2
NCT04729387 Active
Recruiting
Drug: Alpelisib
Drug: Olaparib
Ovarian Cancer Zenyaku Kogyo Co., Ltd. July 2, 2021 Phase 1
NCT03439046 Active
Recruiting
Drug: Alpelisib
Drug: Ribociclib
Breast Cancer Novartis Pharmaceuticals February 2, 2018 Phase 3
NCT04300790 Active
Recruiting
Drug: Alpelisib
Drug: Metformin
Breast Cancer MedSIR October 23, 2020 Phase 2
NCT01872260 Active
Recruiting
Drug: Alpelisib
Drug: LEE011
Breast Cancer Novartis Pharmaceuticals October 22, 2013 Phase 1
Phase 2
Biological Data
  • Alpelisib


    PK/PD/efficacy relationship of NVP-BYL719 in PI3Kα-dependent tumor mouse modelsin vivo.2014 May;13(5):1117-29.

  • Alpelisib


    Determination of NVP-BYL719 safety profile compared with pan-class I PI3K inhibitors.2014 May;13(5):1117-29.

  • Alpelisib


    PTENmutation andPIK3CAamplification/copy number modulate response to NVP-BYL719.2014 May;13(5):1117-29.

  • Alpelisib


    A, genetic alterations inPIK3CApredict NVP-BYL719in vivoefficacy.B, PDX models carrying aPIK3CAmutation and/or amplification were established by implanting surgical tumor tissues from treatment-naïve cancer patients into athymic mice.2014 May;13(5):1117-29.

  • Alpelisib

    PIK3CAmutation is the top positive predictor for NVP-BYL719 sensitivity. A, NVP-BYL719 sensitivity profile. Scatter plot showingAmax(%) by EC50values expressed in μmol/L of NVP-BYL719 in cell viability assays assessed on 474 cancer cell lines.2014 May;13(5):1117-29.

  • Alpelisib

    Alpelisib

    Alpelisib


    Identification of selectivity index of small molecule inhibitors forPIK3CAmutant versusPIK3CAwild-type (WT) cell line populations across ∼1,000 different compounds.2014 May;13(5):1117-29.

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