Buparlisib (BKM120)

Catalog No.S2247 Synonyms: NVP-BKM120

For research use only.

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.

Buparlisib (BKM120) Chemical Structure

CAS No. 944396-07-0

Selleck's Buparlisib (BKM120) has been cited by 222 publications

Purity & Quality Control

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Biological Activity

Description 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.
Targets
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
Vps34 [1]
(Cell-free assay)
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52 nM 116 nM 166 nM 262 nM 2.4 μM
In vitro

BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. [1] BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. [2] BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. [3] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
glioma cell lines MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL5N2E4Omh? MUnJR|UxRTFvMt88US=> M4\rcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{ME[1NFgxLz5{MkC2OVA5ODxxYU6=
U87 M3TLbWFxd3C2b4Ppd{BCe3OjeR?= NU\VWXRvOs7:TR?= NGPaW4Q4Omh? MXXpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?= M1;R[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{ME[1NFgxLz5{MkC2OVA5ODxxYU6=
SNU-601 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHyN2lpPzKq MUXEUXNQ NUW4elRYUUN3ME2wMlgyPsLzMD6wOlPPxE1? NVPXNoQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxOVk5OTRpPkKyNVU6QDF2PD;hQi=>
SNU-1 M3mxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe4Vog4Omh? NEfDb5pFVVOR MnPTTWM2OD1zLkC4NuKyOC5yMklOwG0> MnuzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-668 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\OO|Jp M4fYZmROW09? Mn7ITWM2OD1zLkW3PeKyOC5yN{VOwG0> NGDH[GI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
AGS NFfT[XNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXq3Nog> Ml3PSG1UVw>? MWDJR|UxRTFwN{G0xtExNjFzN988US=> M2LGWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-216 MlnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37QNlczcA>? NVu3fJpETE2VTx?= NF\RfGdKSzVyPUKuOlkzyrFyLkC4Nu69VQ>? MojwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJzNUm4NVQoRjJ{MUW5PFE1RC:jPh?=
SNU-5 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrhd4Y4Omh? NH3lSG1FVVOR M{S5TWlEPTB;MT6zOVHDuTBwMEmx{txO MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF3OUixOEc,OjJzNUm4NVQ9N2F-
SNU-638 NHP6VmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGroemQ4Omh? MYXEUXNQ M2XU[2lEPTB;Mj6yPFLDuTBwMEWz{txO NEH3UFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-16 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfxPGJKPzKq MmDNSG1UVw>? MkH1TWM2OD1zLkW3N:KyOC5yMEJOwG0> NEHwXHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
SNU-484 M2O3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\NO|Jp M4ewbGROW09? Mn72TWM2OD1zLkeyPOKyOC5yNEZOwG0> M{HZOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-620 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV63Nog> MY\EUXNQ NIHtNnNKSzVyPUKuPVM6yrFyLkCwNe69VQ>? M3TITlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUW5PFE1Lz5{MkG1PVgyPDxxYU6=
SNU-719 M{DWRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1KyTlczcA>? MkHkSG1UVw>? NUHVVoM{UUN3ME2zMlA{P8LzMD6wN|LPxE1? NGOxdoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkG1PVgyPCd-MkKxOVk5OTR:L3G+
MM cell lines M2jKfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCxNO69VQ>? M3zKSlI1cA>? NEe1c3BFVVOR M4DpRWlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? MormQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MEe0PFUoRjJ{MkC3OFg2RC:jPh?=
ARP-1 NWLJV2pNSXCxcITvd4l{KEG|c3H5 MVyxNO69VQ>? MknZNlRp NHzscYVFVVOR NWHXNXpzcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyN{S4OUc,OjJ{MEe0PFU9N2F-
colon cancer cell lines MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrlNE0yOM7:TR?= NEjmSlE4Omh? MkjxSG1UVw>? M3XTNGlEPTB;Md88US=> NVvCTpNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OFM5PTdpPkKyOVQ{QDV5PD;hQi=>
gastric cancer cell lines MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPiRW9ZOC1zMN88US=> NIXRRZU4Omh? NITrNmFFVVOR NIrFV2dKSzVyPUKtOe69VQ>? NHHFbnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0N|g2Pyd-MkK1OFM5PTd:L3G+
HCT-116/HT-29/MKN-45 NILKZphCeG:ydH;zbZMhSXO|YYm= MYSy{txO MnHaOFhp M2PZUZNpcW[2IHnuJGczKHCqYYPl MnuyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NEO4OVcoRjJ{NUSzPFU4RC:jPh?=
HT-29 and HCT-116 NH7BXW1E[XOyYYPlJIF{e2G7 MnnzOe69VQ>? MV6yOIg> NEn0UI5qdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= NHLy[oo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0N|g2Pyd-MkK1OFM5PTd:L3G+
PIK3CA-mutant MCF7 M1LpV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TUfmdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P MnPkO|Jp NXvle3VNT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NH3CTWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3Pyd-MkK2OVM6Pjd:L3G+
PIK3CA-mutant MCF7 MkTzT4lv[XOnIFHzd4F6 NFzqV2dKSzVyPUGxOOKyO26P MU[3Nog> NFn4XJFKSzVyPUGxOOKyO26PIHnuJJJm\HWlaX7nJGFsfCCyaH;zdIhwenmuYYTpc44hdGW4ZXzz NVLCVFVLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVM6PjdpPkKyOlU{QTZ5PD;hQi=>
MCF7-myr-Akt MlnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;HTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? MXq3Nog> NHTH[IVIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= NFv5NJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1N|k3Pyd-MkK2OVM6Pjd:L3G+
Y1 cell line M{DnPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmwMlHPxE1xMd88US=> NUH0OWJyOjSq MoHCSG1UVw>? NU\qXYVlcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= M{LQVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkmyPVA1Lz5{Mk[5NlkxPDxxYU6=
human NSCLC NIOwR4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfvNE42NTMQvF2= M13YcFczcA>? NFf6TXZKSzVyPUJOwG0> MnnrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5OEGzPVMoRjJ{N{ixN|k{RC:jPh?=
human NSCLC Mm\YT4lv[XOnIFHzd4F6 NIi4fHky|ryP NWL1S4J2OjSq MYXpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 MkTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5OEGzPVMoRjJ{N{ixN|k{RC:jPh?=
JVM2 M1vsWWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3\UZ|AvOi1{MN88US=> MmT6O|Jp M1PuR2ROW09? M1zkWWlEPTB;MD65{txO NIPzfZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{KzPFY{QSd-MkOyN|g3Ozl:L3G+
EHEB Mk\ZR5l1d3SxeHnjbZR6KGG|c3H5 NUOxOoNPOC5{LUKw{txO MlfFO|Jp NYjqZZU6TE2VTx?= NFi1[FFKSzVyPUCuO:69VQ>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
MEC2 MnjvR5l1d3SxeHnjbZR6KGG|c3H5 MofhNE4zNTJyzszN MmrOO|Jp Ml3wSG1UVw>? NUGwWHBmUUN3ME2wMlfPxE1? MnzqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{i2N|koRjJ|MkO4OlM6RC:jPh?=
primary B-CLL lymphocytes M3zGfmFxd3C2b4Ppd{BCe3OjeR?= NF\iUWhKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NUS1W3VLOjSq NHTMWoVFVVOR M2DpO2lEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
primary B-CLL lymphocytes NX;qeHV[U2mwYYPlJGF{e2G7 MXnJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m NYn1bZZnOjSq NVT3eGROcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ|OE[zPUc,OjN{M{i2N|k9N2F-
SK-HEP1 NVXOXoNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLvNU0zOM7:TR?= MUC3Nog> MXHEUXNQ MX7JR|Ux97zeMd88US=> NH\Fdo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S3PVE{Pid-MkO0O|kyOzZ:L3G+
786-0 M4PCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEixSFkyNTJyzszN NXfNSmp{PzKq MXPEUXNQ NVnwWohVUUN3MP-8oFHPxE1? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5OUGzOkc,OjN2N{mxN|Y9N2F-
human HCC cell lines NEnmPHRE\WyuII\pZYJqdGm2eTDhd5NigQ>? M{DHd|AvODB3LUJOwG0> Mmf6OFhp NVzCe|ZpUUN3ME2x{txO NIfQUI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4PVk6QSd-MkO0PFk6QTl:L3G+
Huh7 NVTJbJUxU2mwYYPlJGF{e2G7 M2Dze|HPxE1? MlfzOFhp NYW0Z3dIe2mpbnpvsKFk[W62bImgdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gRYt1 NWHqUlJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFk6QTlpPkKzOFg6QTl7PD;hQi=>
human NSCLC cell lines NGrpR|BCeG:ydH;zbZMhSXO|YYm= Mo\MNE4yOjVvNN88US=> NHvzZnEzPGh? NF;qSYNFVVOR MUPJR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?= M13od|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NU[yOFczLz5{M{W2NlQ4OjxxYU6=
Primary CLL cells M2HwPGFxd3C2b4Ppd{BCe3OjeR?= M2fVS|EuOTEQvF2= M1X6VFQ5cA>? M32wbYlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> MojxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUC4NFcoRjJ|OEWwPFA4RC:jPh?=
Primary CLL cells M2rXc2tqdmG|ZTDBd5NigQ>? M{nK[lLPxE1? M4\pe|MxdWmw MU\k[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>? MoHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUC4NFcoRjJ|OEWwPFA4RC:jPh?=
Primary CLL cells M3G3WWN6fG:2b4jpZ{BCe3OjeR?= MWWy{txO MVqyOIg> M1jMfIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= NIWyOZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFgxPyd-MkO4OVA5ODd:L3G+
LC-1/SQSF NFvnOYlHfW6ldHnvckBCe3OjeR?= NIm3Spg{|ryP M3qxRlI1cA>? NXXLSG1DTE2VTx?= Mo\n[IVkemWjc3WgUnJHOiCycn;0[YlvKGyndnXs MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl6MEC5N{c,OjN7OECwPVM9N2F-
BCR-ABL M1vB[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTxe|JEOC5{NT2xNO69VQ>? NEmyZlU1\A>? NYfVZohbe2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= NXqxclRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFQ3OTJpPkK0NlQ1PjF{PD;hQi=>
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H1975 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGi2[GkxNjNvOT62{txO NEXt[pY4Omh? M3q2emROW09? M4nkSmlEPTB;MT6zPFXPxE1? NF3WXXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzO|g1Pid-MkSzN|c5PDZ:L3G+
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BT-37 M{nOfpFJXFNiYYPzZZk> MnjWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| Mo[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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BT-12 M1TWfpFJXFNiYYPzZZk> M2LwWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MoHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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NB1643 NWXOdXh6eUiWUzDhd5NigQ>? NEH4empyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz MonrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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SK-N-SH M4TiTJFJXFNiYYPzZZk> MlqydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? M3rwcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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insect MWfGeY5kfGmxbjDhd5NigQ>? MlPWTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCKaYOteIFo\2WmIIC4OYFteGijL4CxNVBidHCqYTDFOVQ2UyCvdYThcpQh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{whUUN3MDC9JFAvODFzIN88UU4> MlvSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{S2NFcoRjNyMEO0OlA4RC:jPh?=
insect M1TJSWZ2dmO2aX;uJIF{e2G7 MVjJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKEircz30ZYdo\WRicEi1ZYxxcGFxcEGxNIFteGijIFW1OFJMKG23dHHueEBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzMEBKSzVyIE2gNE4xOjlizszNMi=> NE\CN4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYxPyd-M{CwN|Q3ODd:L3G+
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Assay
Methods Test Index PMID
Western blot p-AKT (T308) / p-AKT (S473) / AKT ; p-FOXO3a (S253) / FOXO3a ; Nuclear NF-κB p65 / NF-κB p65 ; p-ERK / ERK / LC3 ; p-STAT3 / STAT3 / p-ERK / ERK / p-S6 ; p-MET / MET 27283525 28036259 26673665 27572309 29928341
Immunofluorescence FOXO3a 28036259
Growth inhibition assay Cell viability 26673665
In vivo BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. [1] BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. [2]

Protocol (from reference)

Kinase Assay:[1]
  • PI3K biochemical assay (ATP depletion assay):

    BKM120 is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 µL per well. To start the reaction, 25 µL of 10 nM PI3 kinase and 5 µg/mL 1-α-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 µL of 2 µM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted and then stopped by the addition of 25 µL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence.

Cell Research:[1]
  • Cell lines: A2780 cells.
  • Concentrations: 0-6.6 μM
  • Incubation Time: 3 days.
  • Method: A2780 cells are cultured in DMEM supplemented with 10% FBS, L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 103 cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux.
Animal Research:[1]
  • Animal Models: U87MG and A2780 xenografts are established in female nu/nu mice.
  • Dosages: ~60 mg/kg.
  • Administration: Dosed orally daily (q.d.).

Solubility (25°C)

In vitro

DMSO 82 mg/mL
(199.8 mM)
Ethanol 2 mg/mL
(4.87 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

15mg/mL

Chemical Information

Molecular Weight 410.39
Formula

C18H21F3N6O2

CAS No. 944396-07-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04338399 Recruiting Drug: Buparlisib & Paclitaxel Head and Neck Cancer Adlai Nortye Biopharma Co. Ltd. December 12 2020 Phase 3
NCT02614508 Terminated Drug: Buparlisib|Drug: Ibrutinib|Biological: Ofatumumab Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma Emory University|Novartis January 2016 Phase 1
NCT01613677 Withdrawn Drug: BKM120 Treatment for Metastatic or Locally Advanced Cervical Cancer Novartis Pharmaceuticals|Novartis November 2015 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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