Thursday 19 May 2022 - 04:59
Reminder: Genuine LC Laboratories® brand PMA, which we have been manufacturing in the U.S. for more
than 40 years, is available directly from us: Cat No. P-1680 Phorbol 12-Myristate 13-Acetate, >99.5%.
Our PMA is also available from our >50 U.S. and international distributors, and from more than a dozen
major biochemical reagent "resellers" (who sell our PMA under their own brand names and labels)
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A-4477 Alpelisib, Free Base, >99%
Synonyms : [BYL-719] [NVP-BYL719]
Related Terms : [Piqray]
- Size
- US $
- €
- £
- ¥
- 5 mg
- 59
- 56
- 47
- 7,600
- In stock
- 10 mg
- 83
- 78
- 66
- 10,700
- In stock
- 25 mg
- 113
- 107
- 91
- 14,600
- In stock
- 50 mg
- 144
- 136
- 116
- 18,600
- In stock
- 100 mg
- 232
- 220
- 186
- 30,000
- In stock
- 200 mg
- 397
- 377
- 319
- 51,300
- In stock
- 500 mg
- 878
- 834
- 707
- 113,500
- In stock
- 1 g
- 1,625
- 1,545
- 1,309
- 210,100
- In stock
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- M.W. 441.47
- C19H22F3N5O2S
- [1217486-61-7]
- 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.
- Alpelisib is the active ingredient in the drug product sold under the trade name Piqray®. This drug is currently approved in at least one country for treatment of postmenopausal women, and men, with hormone receptor positive, human epidermal growth factor receptor 2 - negative, PIK 3CA - mutated, advanced or metastatic breast cancer. NOTE: THE ALPELISIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT PIQRAY®, AND IS NOT FOR HUMAN 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.