AdipoGen Life Sciences

Alpelisib

Product Code:
 
SYN-1230
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Shipping:
 
Ambient
Storage:
 
4°C
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Chemical Structure
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Chemical Structure

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SYN-1230-M100100 mgEnquire
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Further Information

Alternate Names/Synonyms:
(2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide; BYL719; NVP-BYL719
Appearance:
Solid.
CAS:
1217486-61-7
EClass:
32160000
Form (Short):
liquid
InChi:
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
InChiKey:
STUWGJZDJHPWGZ-LBPRGKRZSA-N
Long Description:
Chemical. CAS: 1217486-61-7. Formula: C19H22F3N5O2S. MW: 441.5. Selective PI3Kalpha inhibitor with IC50 of 5nM. Has minimal effect on other PI3K isoforms. Exhibits favorable pharmacokinetics and excellent oral bioavailability in animal models. In xenografts using nude mice, it showed dose-dependent effects of tumour inhibition. In a phase Ib study, it showed synergistic anti-tumor activity with endocrine therapy against ER+/PIK3CA mutated breast cancer cells.
MDL:
MFCD22417085
Molecular Formula:
C19H22F3N5O2S
Molecular Weight:
441.5
Package Type:
Plastic Vial
Product Description:
Selective PI3Kalpha inhibitor with IC50 of 5nM. Has minimal effect on other PI3K isoforms. Exhibits favorable pharmacokinetics and excellent oral bioavailability in animal models. In xenografts using nude mice, it showed dose-dependent effects of tumour inhibition. In a phase Ib study, it showed synergistic anti-tumor activity with endocrine therapy against ER+/PIK3CA mutated breast cancer cells.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO or DMF.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

References

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation: P. Furet, et al.; Bioorg. Med. Chem. Lett. 23, 3741 (2013) | Characterization of the novel and specific PI3Kalpha inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials: C. Fritsch, et al.; Mol. Cancer Ther. 13, 1117 (2014) | A Phase Ib Study of Alpelisib (BYL719), a PI3Kalpha-specific Inhibitor, with Letrozole in ER+/HER2-Negative Metastatic Breast Cancer: I.A. Mayer, et al.; Clin. Cancer Res. (Epub ahead of print) (2016)