Alpelisib
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 204780

CAS#: 1217486-61-7

Description: Alpelisib, also known as BLY719, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BYL719 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Check for active clinical trials or closed clinical trials using this agent.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 750
Size
Price

25mg
USD 250
500mg
USD 1850
Size
Price

50mg
USD 450
1g
USD 2950

Alpelisib (BYL-719), purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 1g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 204780
Name: Alpelisib
CAS#: 1217486-61-7
Chemical Formula: C19H22F3N5O2S
Exact Mass: 441.14463
Molecular Weight: 441.47
Elemental Analysis: C, 51.69; H, 5.02; F, 12.91; N, 15.86; O, 7.25; S, 7.26


Synonym: BYL719; BYL-719; BYL 719; Alpelisib

IUPAC/Chemical Name: (S)-N1-(4-methyl-5-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)pyrrolidine-1,2-dicarboxamide.

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

SMILES Code: O=C(N1[C@H](C(N)=O)CCC1)NC2=NC(C)=C(C3=CC(C(C)(C)C(F)(F)F)=NC=C3)S2


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

 
 


References

1: Azab F, Vali S, Abraham J, Potter N, Muz B, de la Puente P, Fiala M, Paasch J, Sultana Z, Tyagi A, Abbasi T, Vij R, Azab AK. PI3KCA plays a major role in multiple myeloma and its inhibition with BYL719 decreases proliferation, synergizes with other therapies and overcomes stroma-induced resistance. Br J Haematol. 2014 Jan 9. doi: 10.1111/bjh.12734. [Epub ahead of print] PubMed PMID: 24405121.

2: Brady SW, Zhang J, Seok D, Wang H, Yu D. Enhanced PI3K p110α Signaling Confers Acquired Lapatinib Resistance That Can Be Effectively Reversed by a p110α-Selective PI3K Inhibitor. Mol Cancer Ther. 2014 Jan;13(1):60-70. doi: 10.1158/1535-7163.MCT-13-0518. Epub 2013 Nov 18. PubMed PMID: 24249715; PubMed Central PMCID: PMC3902650.

3: Garrett JT, Sutton CR, Kurupi R, Bialucha CU, Ettenberg SA, Collins SD, Sheng Q, Wallweber J, Defazio-Eli L, Arteaga CL. Combination of antibody that inhibits ligand-independent HER3 dimerization and a p110α inhibitor potently blocks PI3K signaling and growth of HER2+ breast cancers. Cancer Res. 2013 Oct 1;73(19):6013-23. doi: 10.1158/0008-5472.CAN-13-1191. Epub 2013 Aug 5. PubMed PMID: 23918797; PubMed Central PMCID: PMC3790862.

4: Elkabets M, Vora S, Juric D, Morse N, Mino-Kenudson M, Muranen T, Tao J, Campos AB, Rodon J, Ibrahim YH, Serra V, Rodrik-Outmezguine V, Hazra S, Singh S, Kim P, Quadt C, Liu M, Huang A, Rosen N, Engelman JA, Scaltriti M, Baselga J. mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. Sci Transl Med. 2013 Jul 31;5(196):196ra99. doi: 10.1126/scitranslmed.3005747. PubMed PMID: 23903756.

5: Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R, Hamon J, Fabbro D, Caravatti G. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14. Erratum in: Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723. PubMed PMID: 23726034.

6: Young CD, Pfefferle AD, Owens P, Kuba MG, Rexer BN, Balko JM, Sánchez V, Cheng H, Perou CM, Zhao JJ, Cook RS, Arteaga CL. Conditional loss of ErbB3 delays mammary gland hyperplasia induced by mutant PIK3CA without affecting mammary tumor latency, gene expression, or signaling. Cancer Res. 2013 Jul 1;73(13):4075-85. doi: 10.1158/0008-5472.CAN-12-4579. Epub 2013 Apr 30. PubMed PMID: 23633485; PubMed Central PMCID: PMC3702683.