A-4477 Alpelisib, Free Base, >99%

Synonyms : [BYL-719] [NVP-BYL719]

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  • 5 mg
  • 59
  • 50
  • 45
  • 6,200
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  • In stock
  • 10 mg
  • 83
  • 71
  • 64
  • 8,700
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  • 25 mg
  • 113
  • 96
  • 87
  • 11,800
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  • 50 mg
  • 144
  • 123
  • 111
  • 15,100
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  • 100 mg
  • 232
  • 198
  • 179
  • 24,300
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  • 200 mg
  • 397
  • 340
  • 307
  • 41,500
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  • 500 mg
  • 878
  • 752
  • 679
  • 91,900
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  • 1 g
  • 1,625
  • 1,392
  • 1,257
  • 170,000
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  • In stock

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  • M.W. 441.47
  • C19H22F3N5O2S
  • [1217486-61-7]

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  • Alpelisib, also known as BYL719, is a potent and selective phosphatidylinositol-3 kinase [alpha] inhibitor. It inhibited P110[alpha], p110[beta], p110[delta], and p110[gamma] with IC50 values of 5 nM, 1.2 µM, 0.29 µM and 0.25 µM, respectively, in biochemical assays. It inhibited the Akt phosphorylation with IC50 values of 74 nM in Rat1-myr-p110[alpha] cells, 2.2 µM in Rat1-myr-p110[beta] cells, and 1.2 µM in Rat1-myr-p110[delta] cells. Furet P., et al. "Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation." Bioorg. Med. Chem. Lett. 23: 3741-3748 (2013).
  • Alpelisib showed dose- and time-dependent inhibition of PI3K[alpha] signaling in vivo and demonstrated robust anti-tumor response and tolerability in PIK3CA-dependent tumor models. Fritsch 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: 1117-1129 (2014).
  • mTORC1 inhibition is necessary for sensitivity to PI3K p110[alpha] inhibition by alpelisib in PIK3CA-mutant breast cancer. Elkabets M., et al. "mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer." Sci. Transl. Med. 5: 196ra99 (2013).
  • Related CAS numbers: 1584128-91-5 for the hydrochloride salt.
  • Another CAS number previously assigned to BYL-719 free base, namely 1361185-44-5, has been deleted by CAS and is no longer in use.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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