Alpelisib (BYL719)

Name: Alpelisib (BYL719)
Brand: Selleck Chemicals
SKU: S2814
Rating: 5 (114 reviews)

For research use only.

Catalog No.S2814

114 publications

CAS No. 1217486-61-7

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

Selleck's Alpelisib (BYL719) has been cited by 114 publications

Cell, 2020, 25;181(7):1596-1611.e27.

PubMed: 32559461 ( click the link to review the publication )

Cancer Cell, 2020, S1535-6108(20)30427-X

PubMed: 32976773 ( click the link to review the publication )

Science, 2019, 364(6441)

PubMed: 31097636 ( click the link to review the publication )

Nat Med, 2019, 25(5):838-849

PubMed: 31011202 ( click the link to review the publication )

Nat Genet, 2019, 51(2):207-216

PubMed: 30531871 ( click the link to review the publication )

Cancer Discov, 2019, 10.1158/2159-8290.CD-18-0830

PubMed: 31594766 ( click the link to review the publication )

Cancer Discov, 2018, 8(5):568-581

PubMed: 29496664 ( click the link to review the publication )

Cancer Cell, 2018, 34(6):922-938

PubMed: 30537514 ( click the link to review the publication )

Cancer Discov, 2017, 7(9):1018-1029

PubMed: 28619981 ( click the link to review the publication )

Nat Med, 2015, 21(9):1038-47

PubMed: 26301689 ( click the link to review the publication )

Cancer Res, 2021, canres.3232.2020

PubMed: 33685991 ( click the link to review the publication )

Cell Rep, 2021, 34(7):108750

PubMed: 33596424 ( click the link to review the publication )

Oncogene, 2021, 10.1038/s41388-020-01628-x

PubMed: 33500549 ( click the link to review the publication )

PLoS Pathog, 2021, 17(1):e1009216

PubMed: 33481911 ( click the link to review the publication )

Cell Death Dis, 2021, 12(1):85

PubMed: 33446653 ( click the link to review the publication )

Mol Cancer Ther, 2021, 20(4):691-703

PubMed: 33509905 ( click the link to review the publication )

Int J Oncol, 2021, 10.3892/ijo.2021.5167

PubMed: 33491755 ( click the link to review the publication )

Cancer Med, 2021, 10(7):2370-2379

PubMed: 33665980 ( click the link to review the publication )

Oncotarget, 2021, 12(7):674-685

PubMed: 33868588 ( click the link to review the publication )

Nat Commun, 2020, 8;11(1):2291

PubMed: 32385243 ( click the link to review the publication )

EMBO Mol Med, 2020, 12(4):e11177

PubMed: 32115889 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 117(39):24427-24433

PubMed: 32929011 ( click the link to review the publication )

Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485

PubMed: 31969334 ( click the link to review the publication )

Clin Cancer Res, 2020, 10.1158/1078-0432

PubMed: 32034078 ( click the link to review the publication )
Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Cell Rep, 2020, 31(12):107800

PubMed: 32579927 ( click the link to review the publication )

Cell Rep, 2020, 30(5):1400-1416

PubMed: 32023458 ( click the link to review the publication )

Cell Rep, 2020, 9;31(10):107753

PubMed: 32521278 ( click the link to review the publication )

Oncogene, 2020, 39(19):3837-3852

PubMed: 32161312 ( click the link to review the publication )

Oncogene, 2020, 10.1038/s41388-020-1255-y

PubMed: 32157217 ( click the link to review the publication )

J Exp Clin Cancer Res, 2020, 39(1):217

PubMed: 33059733 ( click the link to review the publication )

Cancers (Basel), 2020, 12(9)E2500

PubMed: 32899250 ( click the link to review the publication )

Cancer Discov, 2020, 10(7):1058-1077

PubMed: 32341020 ( click the link to review the publication )

Mol Cancer Ther, 2020, 5;molcanther.1131.2019

PubMed: 32371585 ( click the link to review the publication )

Cell Oncol (Dordr), 2020, 8

PubMed: 32382996 ( click the link to review the publication )

Oncogenesis, 2020, 9(10):87

PubMed: 33012785 ( click the link to review the publication )

Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0549

PubMed: 32152233 ( click the link to review the publication )

Mol Cancer Res, 2020, 25

PubMed: 32098826 ( click the link to review the publication )

Int J Mol Sci, 2020,

PubMed: 32708306 ( click the link to review the publication )

Sci Rep, 2020, 1;10(1):8867

PubMed: 32483262 ( click the link to review the publication )

J Biol Chem, 2020, 14;295(7):1769-1780

PubMed: 31915252 ( click the link to review the publication )

J Biol Chem, 2020, 295(8):2336-2347

PubMed: 31959630 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Commun Biol, 2020, 3(1):546

PubMed: 33004975 ( click the link to review the publication )

Oncol Rep, 2020, 44(3):863-872

PubMed: 32705230 ( click the link to review the publication )

Viruses, 2020, 12(6):E652

PubMed: 32560319 ( click the link to review the publication )

Blood Adv, 2020, 4(18):4382-4392

PubMed: 32926124 ( click the link to review the publication )

Cancer, 2020, 10.1002/cncr.33071

PubMed: 32767682 ( click the link to review the publication )
Cold Spring Harb Mol Case Stud, 2020, 12;6(3):a004853

PubMed: 32532875 ( click the link to review the publication )

Small GTPases, 2020, 10.1080/21541248

PubMed: 32043900 ( click the link to review the publication )

Cell Death Dis, 2020, 11(7):505

PubMed: 32632138 ( click the link to review the publication )

Mol Syst Biol, 2019, 15(3):e8323

PubMed: 30858180 ( click the link to review the publication )

Cell Rep, 2019, 27(1):294-306

PubMed: 30943409 ( click the link to review the publication )

Cancer Lett, 2019, 459:145-155

PubMed: 31173854 ( click the link to review the publication )

Sci Signal, 2019, 12(585)

PubMed: 31186373 ( click the link to review the publication )

Brain Pathol, 2019, 29(3):336-350

PubMed: 30403311 ( click the link to review the publication )

Cancers (Basel), 2019, 10.3390/cancers11101586

PubMed: 31627436 ( click the link to review the publication )

Breast Cancer Res, 2019, 21(1):20

PubMed: 30709367 ( click the link to review the publication )

Cancers (Basel), 2019, 11(2)

PubMed: 30736342 ( click the link to review the publication )

J Dent Res, 2019, 98(3):304-312

PubMed: 30513244 ( click the link to review the publication )

J Immunol, 2019, 203(6):1579-1588

PubMed: 31427445 ( click the link to review the publication )

Sci Rep, 2019, 9(1):9130

PubMed: 31235758 ( click the link to review the publication )

Front Microbiol, 2019,

PubMed: 32038504 ( click the link to review the publication )

Mol Pharmacol, 2019, 95(5):528-536

PubMed: 30858165 ( click the link to review the publication )

Endocrinology, 2019, 160(11):2600-2617

PubMed: 31322702 ( click the link to review the publication )

Cancer Cell Int, 2019, 19:348

PubMed: 31889900 ( click the link to review the publication )

Cancer Manag Res, 2019, 11:6229-6244

PubMed: 31308757 ( click the link to review the publication )

Cancer Res Treat, 2019, 51(3):951-962

PubMed: 30309221 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 513(3):546-552

PubMed: 30981504 ( click the link to review the publication )

Pediatr Blood Cancer, 2019, 66(8):e27790

PubMed: 31045327 ( click the link to review the publication )

Cancer Biol Med, 2019, 16(1):66-83

PubMed: 31119047 ( click the link to review the publication )

Nat Biomed Eng, 2018, 2(8):578-588

PubMed: 31015631 ( click the link to review the publication )
Nat Commun, 2018, 9(1):4550

PubMed: 30382095 ( click the link to review the publication )

Nat Commun, 2018, 9(1):2819

PubMed: 30026551 ( click the link to review the publication )

EMBO J, 2018, 37(1):19-38

PubMed: 29150432 ( click the link to review the publication )

Cancer Res, 2018, 78(8):2000-2013

PubMed: 29437705 ( click the link to review the publication )

Cancer Res, 2018, 78(9):2383-2395

PubMed: 29440171 ( click the link to review the publication )

Sci Signal, 2018,

PubMed: 29535262 ( click the link to review the publication )

Cell Death Dis, 2018, 9(9):876

PubMed: 30158592 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(10):2091-2099

PubMed: 30045927 ( click the link to review the publication )

Anal Biochem, 2018, 547:66-76

PubMed: 29470948 ( click the link to review the publication )

J Exp Med, 2018, 215(1):159-175

PubMed: 29141866 ( click the link to review the publication )

Oncotarget, 2018, 9(51):29565-29573

PubMed: 30038704 ( click the link to review the publication )

Nat Commun, 2017, 8(1):1090

PubMed: 29061961 ( click the link to review the publication )

Nat Commun, 2017, 8(1):1278

PubMed: 29097657 ( click the link to review the publication )

Theranostics, 2017, 7(4):974-986

PubMed: 28382169 ( click the link to review the publication )

Sci Data, 2017, 4:170139

PubMed: 28972570 ( click the link to review the publication )

Signal Transduct Target Ther, 2017, 2:17063

PubMed: 29279775 ( click the link to review the publication )

Basic Res Cardiol, 2017, 112(6):66

PubMed: 29043508 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(4):729-738

PubMed: 28119490 ( click the link to review the publication )

Mol Cancer Ther, 2017, molcanther.0415.2016

PubMed: 28119489 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(3):516-528

PubMed: 28138035 ( click the link to review the publication )

Cell Discov, 2017, 3:16054

PubMed: 28224045 ( click the link to review the publication )

Mol Cancer Res, 2017,

PubMed: 28784613 ( click the link to review the publication )

Int J Oncol, 2017, 50(6):2049-2058

PubMed: 28440469 ( click the link to review the publication )

Oncotarget, 2017, 8(14):23213-23227

PubMed: 28390196 ( click the link to review the publication )
Oncotarget, 2017, 8(47):81794-81802

PubMed: 29137222 ( click the link to review the publication )

Nat Cell Biol, 2016, 18(12):1324-1335

PubMed: 27870828 ( click the link to review the publication )

Nat Commun, 2016, 7:11971

PubMed: 27321283 ( click the link to review the publication )

Cell Rep, 2016,

PubMed: 27292631 ( click the link to review the publication )

Elife, 2016, 10.7554/eLife.18489

PubMed: 27845624 ( click the link to review the publication )

Elife, 2016,

PubMed: 27700986 ( click the link to review the publication )

Oncogene, 2016, 10.1038/onc.2016.216

PubMed: 27345413 ( click the link to review the publication )

Cancer Discov, 2016, 6(10):1134-1147

PubMed: 27604488 ( click the link to review the publication )

Oncotarget, 2016,

PubMed: 27602501 ( click the link to review the publication )

Blood, 2015, 10.1182/blood-2014-11-610329

PubMed: 25957390 ( click the link to review the publication )

J Thorac Oncol, 2015, 10(12):1736-44

PubMed: 26473643 ( click the link to review the publication )

Proc Natl Acad Sci USA, 2015,

PubMed: 26508629 ( click the link to review the publication )

Endocrinology, 2015, 156(1):218-30

PubMed: 25343277 ( click the link to review the publication )

Cell Signal, 2015, 27(12):2389-400

PubMed: 26363466 ( click the link to review the publication )

Anticancer Res, 2015, 35(1):175-82

PubMed: 25550549 ( click the link to review the publication )

Oncotarget, 2015, 6(19):17501-13

PubMed: 25991673 ( click the link to review the publication )

Br J Haematol, 2014, 165(1):89-101

PubMed: 24405121 ( click the link to review the publication )

Anal Bioanal Chem, 2014, 406(15):3743-54

PubMed: 24817345 ( click the link to review the publication )

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

Targets

PI3Kα ^[1]
(Cell-free assay)

5 nM

In 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. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
Detroit562	MkXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHLuVVAxNjFvMUCwJO69VQ>?	NIfwfo04OiCq	M3LVXGlEPTB;MT6xNEDPxE1?	MkTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
SNU-1076	NWmxb29zT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4i2d\|AvOS1zMECg{txO	NUj6[\|VJPzJiaB?=	M1ywPGlEPTB;Nj64NkDPxE1?	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MEW0PUc,OjV3NUC1OFk9N2F-
SNU-1066	NHG4SYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnnUNE4yNTFyMDFOwG0>	MlPWO\|IhcA>?	MYjJR\|UxRTFwMUOg{txO	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3MEW0PUc,OjV3NUC1OFk9N2F-
FaDu	NHXNS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3vOfVAvOS1zMECg{txO	MVe3NkBp	MoX2TWM2OD1zOT62OkDPxE1?	MnHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NUC1OFkoRjJ3NUWwOVQ6RC:jPh?=
SNU1041	NXHB[FFOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MX[wMlEuOTByIN88US=>	MUi3NkBp	MljHTWM2OD1{MD62OUDPxE1?	NGGwcJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1NFU1QSd-MkW1OVA2PDl:L3G+
SCC25	M2fBS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYGwMlEuOTByIN88US=>	NFXpR4s4OiCq	M1yzfmlEPTB;NEmuN\|Ah\|ryP	M3rEeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUWwOVQ6Lz5{NUW1NFU1QTxxYU6=
BON-1	MkjoSpVv[3Srb36gRZN{[Xl?	MX:xM\|ExKM7:TR?=	MlHTOEBp	MULpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM\|Ih[WO2aY\peIlmew>?	NELvPWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyOlI6Oid-MkWwNlYzQTJ:L3G+
QGP-1	MVjGeY5kfGmxbjDBd5NigQ>?	NUnkcI83OS9zMDFOwG0>	MUW0JIg>	NFztRZBqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?=	NG[yfZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyOlI6Oid-MkWwNlYzQTJ:L3G+
MG-63	MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MluxTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?=	MlHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkG3PVAoRjJ2OU[xO\|kxRC:jPh?=
HOS	NHe4TGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NX71d4J6UUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0>	NHTYbZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NVc6OCd-MkS5OlE4QTB:L3G+
MOS-J	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NH;4[Y9KSzVyPUGwJO69Ve,:jDDJR\|kxRTN4IN88US=>	NVeydmNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlE4QTBpPkK0PVYyPzlyPD;hQi=>
POS-1	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MkjaTWM2OD16IN88Ug+9lCCLQ{mwQVM3KM7:TR?=	NYHGd2k4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5OlE4QTBpPkK0PVYyPzlyPD;hQi=>
92.1	M2DJemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVS1NFAuOjByMDDuUS=>	NWHLbZY4PSCm	MUPpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd\|KTD1dEB1dyBzIN88US=>	NFnLeoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW2N\|U1OCd-MkS1OlM2PDB:L3G+
Mel270	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFTSSXE2ODBvMkCwNEBvVQ>?	MUG1JIQ>	NVPPNVE4cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1?	NUC0S2dLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OlM2PDBpPkK0OVY{PTRyPD;hQi=>
Omm1.3	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4PKNVUxOC1{MECwJI5O	NVfmT5VVPSCm	NIjyd2JqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>?	M{DzZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NU[zOVQxLz5{NEW2N\|U1ODxxYU6=
Omm1	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NG\LXG02ODBvMkCwNEBvVQ>?	MYK1JIQ>	NEfjeo5qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>?	MnzVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3NkO1OFAoRjJ2NU[zOVQxRC:jPh?=
C918	M1;nZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MknKOVAxNTJyMECgcm0>	NFPaeGk2KGR?	NIHVNXNqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>?	NGK1O5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEW2N\|U1OCd-MkS1OlM2PDB:L3G+
Mel290	NF\YeIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3jUZ\|UxOC1{MECwJI5O	MYW1JIQ>	NEjRd5RqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>?	M1O0b\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NU[zOVQxLz5{NEW2N\|U1ODxxYU6=
OPM2	M2Lt[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVP4bZlPOC53LUKuOUDPxE1?	M13LRlQ5KGh?	NFTGXYVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NXm1PVFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
OPM1	NEXhXlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEnGTHQxNjVvMj61JO69VQ>?	MoroOFghcA>?	MmXHbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	NGfN[Ic9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESwOVEzOSd-MkS0NFUyOjF:L3G+
U266	M4rUXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXiwMlUuOi53IN88US=>	MV:0PEBp	M17CPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUGyNUc,OjR2MEWxNlE9N2F-
MM1R	MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIjt[XoxNjVvMj61JO69VQ>?	NHrBcnk1QCCq	NEixVYdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NVHibIM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
MM1S	NXrjeW1GT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4HD[\|AvPS1{LkWg{txO	M{TNbFQ5KGh?	NHX6SmFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	MkfzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MEWxNlEoRjJ2NEC1NVIyRC:jPh?=
H929	NU[1XIUxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWKwMlUuOi53IN88US=>	NHTWOJQ1QCCq	NHjqVIpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NVyxXVNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
RPMI	MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MViwMlUuOi53IN88US=>	NVvmd4hMPDhiaB?=	MlT0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	NVTYWFdQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NFUyOjFpPkK0OFA2OTJzPD;hQi=>
SKBR3	MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mof5N\|Mh\|ryP	NH;DPYM2KGR?	M2Pve4lvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To	MlzmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ\|OUG4O\|k4RC:jPh?=
MDA453	M4X1OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHfmV3k{OyEQvF2=	MYm1JIQ>	MWLpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?=	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
EFM192A	NGTheoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVzjc3FbOzNizszN	M4Xa[FUh\A>?	MUnpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?=	NHnDZ4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
AU565	Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIXsT3M{OyEQvF2=	NGfEbGQ2KGR?	NYHrVHd3cW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg>	NV;SZZB6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
MDA361	NEPUVoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX:zN{DPxE1?	Ml25OUBl	M1i3cYlvcGmkaYTzJFQ197zHIHPlcIwh\3Kxd4To	NEnpTlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
BT474	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkfuN\|Mh\|ryP	MWm1JIQ>	M{nDc4lvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To	NIfFSms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
HCC202	NUXMXpVZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkTHN\|Mh\|ryP	MoX3OUBl	NYm4eVE5cW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg>	NVrjZm56RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
KPL4	NHnYZVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1HvO\|M{KM7:TR?=	MWO1JIQ>	M4rtcYlvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To	NU\ZNG5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
NCL-N87	MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mkn3N\|Mh\|ryP	MWG1JIQ>	M2LKb4lvcGmkaYTzJFMy97zHIHPlcIwh\3Kxd4To	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
UACC812	NUjDWGRPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{\yWVM{KM7:TR?=	M4rTUFUh\A>?	NWX2TYRQcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg>	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
HCC2218	NWO4e\|kxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NG\0bXo{OyEQvF2=	M3jweVUh\A>?	NYi2bWFGcW6qaXLpeJMhOTYxvJWgZ4VtdCCpcn;3eIg>	M3zVXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OUG4O\|k4Lz5{M{mxPFc6PzxxYU6=
HCC1569	M175ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYTON2k{OzNizszN	NFLFOmI2KGR?	NETjTohqdmirYnn0d{A297zHIHPlcIwh\3Kxd4To	NWXxXmQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVg4QTdpPkKzPVE5Pzl5PD;hQi=>
OE19	MnTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2XZeFM{KM7:TR?=	MVS1JIQ>	MYDpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?=	M1H1flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OUG4O\|k4Lz5{M{mxPFc6PzxxYU6=
OE33	M36xcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2GzdlM{KM7:TR?=	M4fiR\|Uh\A>?	MX3pcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?=	MmTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ\|OUG4O\|k4RC:jPh?=
JIMT1	M4nac2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mli5N\|Mh\|ryP	MlzIOUBl	NUW0TYpzcW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=>	NGnqPIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
HCC1954	NX3uXGFDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mo\lN\|Mh\|ryP	NXPmXZRKPSCm	MkexbY5pcWKrdIOgNlnwxIViY3XscEBoem:5dHi=	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlzOEe5O{c,OjN7MUi3PVc9N2F-
NUGC4	NEjuVWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWm2Ulg1OzNizszN	M1Xub\|Uh\A>?	M1\HfolvcGmkaYTzJFE197zHIHPlcIwh\3Kxd4To	NGLFPVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mxPFc6Pyd-MkO5NVg4QTd:L3G+
ZR-75-30	M{LYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGXzSlM{OyEQvF2=	NUC4WlhXPSCm	MWjpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi=	MnW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUi3PVcoRjJ\|OUG4O\|k4RC:jPh?=
Rat1	MmHVVFEyOGGucHjhJIlvcGmkaYTpc44h[XO\|YYm=			NUPucmxZUUN3MDC9JFAvODd2IN88US=>	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF4NEG4PUc,OjZzNkSxPFk9N2F-
Rat1	M37xN3BKO0ujbIDoZUBqdmirYnn0bY9vKGG\|c3H5			NX3Lc2ZWUUN3MDC9JFAvODd2IN88US=>	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1	NWrOSmd4WDFzMHHsdIhiKGmwaHnibZRqd25iYYPzZZk>			NXmzOYNXUUN3MDC9JFAvODd2IN88US=>	NX\zVZdzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NlYxOzRpPkKzO\|I3ODN2PD;hQi=>
Rat1	NVq3WHRbWDFzMHTlcJRiKGmwaHnibZRqd25iYYPzZZk>			MlHUTWM2OCB;IEGuNkDPxE1?	NEj6Xog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG2OFE5QSd-Mk[xOlQyQDl:L3G+
Rat1	M4e0PXBKO0upYX3tZUBqdmirYnn0bY9vKGG\|c3H5			MlnXTWM2OCB;IEGuNkDPxE1?	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJyNkWwOEc,OjZ{ME[1NFQ9N2F-
Rat1	MUHQNVEx\GWudHGgbY5pcWKrdHnvckBie3OjeR?=			M2Hme2lEPTBiPTCxMlIh\|ryP	MkDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mk[wN\|QoRjJ\|N{K2NFM1RC:jPh?=
Rat1	M2j6[HAyOTCkZYThJIlvcGmkaYTpc44h[XO\|YYm=			MXjJR\|UxKD1iMj6yJO69VQ>?	Ml;BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzNkSxPFkoRjJ4MU[0NVg6RC:jPh?=
Rat1	Mmj6VGk{U2KndHGgbY5pcWKrdHnvckBie3OjeR?=			MkP4TWM2OCB;IEKuNkDPxE1?	NXHPfXN6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNFY2ODRpPkK2NlA3PTB2PD;hQi=>
Rat1	M4rveHAyOTCjbIDoZUBqdmirYnn0bY9vKGG\|c3H5			NIHjcHNKSzVyIE2gNk4zKM7:TR?=	M{T5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K2NFM1Lz5{M{eyOlA{PDxxYU6=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AKT(S473) / p-AKT(T308); PubMed: 25544637 Cancer Cell PIK3CA hot-spot mutant cell lines were treated with 1 µM BYL719 for the indicated period of time. Lysates were immunoblotted to detect the indicated proteins. p100β / p110α / p85 / p-ERBB3(Y1289); PubMed: 25544637 Cancer Cell BT474 cells were treated with 1 µM BYL719 alone for different durations of time and lysates were immunoprecipitated with ERBB3 antibody. Precipitates were analyzed by western blot with the indicated antibodies. p-HER2 / IGF-1R; PubMed: 25544637 Cancer Cell Cells were treated with 1 μM BYL719 for 24 hr and lysates were immunoblotted to detect the indicated proteins. pS6 (Ser235-236); PubMed: 27048245 Breast Cancer Res Immunoblots of lysates from parental and resistant cells treated for 24 hours as indicated. PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD; PubMed: 27604488 Cancer Discov T47D cells cultured to resistance in the presence of BYL719. Both parental (T47D) and resistant (T47DR) cells were treated with BYL719 at 1μM, and cell lysates were prepared at 0, 4, 24 hours for immunoblotting for the indicated proteins.	25544637 27048245 27604488
Growth inhibition assay	Cell viability; PubMed: 27602501 Oncotarget The effect of BYL719 on cellular viability was evaluated in HCT116 (A) and SW480 (B) CRC cells. Briefly, cells were grown, treated with increasing concentrations of BYL719 (5, 10 and 20 μM) and cellular viability determined by MTS assay 72h after treatments. Controls included cells that remained untreated (media ctrl) and vehicle-treated controls (DMSO). Data represent means ± SEM of at least triplicate experiments normalized to controls. All conditions were compared with DMSO. Ctrl, control; DMSO, dimethyl sulfoxide. , p< 0.01; , p< 0.001; ***, p< 0.0001.	27602501
Immunofluorescence	LC3; PubMed: 26637440 Breast Cancer Res SKBR3 GFP-LC3 cells were cultured for 5 days with DMSO, 500 nM BKM120 or 500 nM BYL719. Cells were treated with DMSO or 1 μM Lapatinib for the final 18 h. GFP-LC3 localization was captured by fluorescent microscopy.	26637440

In vivo

BYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. BYL719(270mg/d) shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients. ^[1]

Protocol

References

[1] Dejan Juric, et al. 2012, AACR 103rd Annual Meeting. Abst CT-01.

Solubility (25°C)

In vitro	DMSO	88 mg/mL (199.33 mM)
	Ethanol	2 mg/mL (4.53 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+40%PEG300+5%Tween80+50%ddH2O For best results, use promptly after mixing.	4.4 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Alpelisib (BYL719) SDF

Molecular Weight	441.47
Formula	C₁₉H₂₂F₃N₅O₂S
CAS No.	1217486-61-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04589650	Not yet recruiting	Drug: Alpelisib\|Drug: Placebo	PIK3CA-related Overgrowth Spectrum (PROS)	Novartis Pharmaceuticals\|Novartis	February 2 2021	Phase 2
NCT04544189	Not yet recruiting	Drug: Alpelisib\|Drug: Fulvestrant\|Drug: Placebo	Breast Neoplasms	Novartis Pharmaceuticals\|Novartis	December 31 2020	Phase 2
NCT04524000	Recruiting	Drug: Alpelisib\|Drug: Fulvestrant	Advanced Breast Cancer	Novartis Pharmaceuticals\|Novartis	November 20 2020	Phase 2
NCT04300790	Recruiting	Drug: Alpelisib\|Drug: Metformin\|Drug: Fulvestrant	Breast Cancer	MedSIR\|Novartis	October 23 2020	Phase 2
NCT04526470	Not yet recruiting	Drug: Alpelisib\|Drug: Paclitaxel	Solid Tumor\|Stomach Cancer	Seoul National University Bundang Hospital	September 1 2020	Phase 1\|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Features:A beta isoform-sparing PI3K inhibitor.
Pilaralisib (XL147) ^New

Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
GNE-317 ^New

GNE-317 is a potent, brain-penetrant PI3K inhibitor.
LY294002

LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
3-Methyladenine (3-MA)

3-Methyladenine (3-MA, NSC 66389) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.
Idelalisib (CAL-101, GS-1101)

Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Wortmannin

Wortmannin (KY 12420, SL-2052) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Dactolisib (BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Buparlisib (BKM120)

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
Pictilisib (GDC-0941)

Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.

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Alpelisib (BYL719)