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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. 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.
| 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)
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| 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.
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| 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.
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| 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).
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| Cell Assay |
Alpelisib (0–1000 nM) was applied to cells in escalating concentrations for 72 hours. Using the CyQuant assay, cell viability was measured.
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| Animal Protocol |
Female athymic nu/nu mice
40 mg/kg o.g. |
| References |
| Molecular Formula |
C19H22F3N5O2S
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|---|---|
| Molecular Weight |
441.47
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| Exact Mass |
441.14463
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| Elemental Analysis |
C, 51.69; H, 5.02; F, 12.91; N, 15.86; O, 7.25; S, 7.26
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| CAS # |
1217486-61-7
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| Related CAS # |
Alpelisib hydrochloride;1584128-91-5
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| Appearance |
white solid powder
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| SMILES |
CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
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| InChi Key |
STUWGJZDJHPWGZ-LBPRGKRZSA-N
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| 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
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| 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
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| Synonyms |
Alpelisib; NVP-BYL-719; NVP-BYL719; NVP-BYL 719; BYL-719; BYL719; BYL 719
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| 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.
Calculation results
Working concentration： mg/mL；
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.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| 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 |
 PK/PD/efficacy relationship of NVP-BYL719 in PI3Kα-dependent tumor mouse modelsin vivo.Mol Cancer Ther.2014 May;13(5):1117-29. |
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 Determination of NVP-BYL719 safety profile compared with pan-class I PI3K inhibitors.Mol Cancer Ther.2014 May;13(5):1117-29. |
 PTENmutation andPIK3CAamplification/copy number modulate response to NVP-BYL719.Mol Cancer Ther.2014 May;13(5):1117-29. |
 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.Mol Cancer Ther.2014 May;13(5):1117-29. |
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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.Mol Cancer Ther.2014 May;13(5):1117-29. |
 Identification of selectivity index of small molecule inhibitors forPIK3CAmutant versusPIK3CAwild-type (WT) cell line populations across ∼1,000 different compounds.Mol Cancer Ther.2014 May;13(5):1117-29. |
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