Buparlisib (BKM120)

For research use only.

Catalog No.S2247 Synonyms: NVP-BKM120

154 publications

Buparlisib (BKM120) Chemical Structure

Molecular Weight(MW): 410.39

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.

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Selleck's Buparlisib (BKM120) has been cited by 154 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

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)
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
MCF7 NV3EUI83S3m2b4TvfIlkKEG|c3H5 MkGzO|IhcA>? MV7EUXNQ MnnWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?= NGT0dFkzPDlyMEK2Oi=>
DU145 MmXpR5l1d3SxeHnjJGF{e2G7 NVHxbld7PzJiaB?= M1rDcGROW09? NGO3[pFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= NGrXfIszPDlyMEK2Oi=>
A2780 NY\JZW9XS3m2b4TvfIlkKEG|c3H5 NXTW[49xPzJiaB?= M{DpOGROW09? M3ztNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= MoLENlQ6ODB{Nk[=
U87MG NG\WbYJEgXSxdH;4bYMhSXO|YYm= MmXsO|IhcA>? M4[z[GROW09? NF;YbIdEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN M1LZNlI1QTByMk[2
A2780 M3:3NGZ2dmO2aX;uJGF{e2G7 MV:xJIg> NHjmdpBFVVOR NXfOeGU1UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlA2PSEQvF2= M{fQRVI1QTByMk[2
DU145 Mn76SpVv[3Srb36gRZN{[Xl? M{O3OVEhcA>? M{XjXWROW09? NY\keIxsUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKESXMUS1JINmdGy|IHjhdoJwemmwZzDMT2IyKG23dHH0bY9vKHerdHigSWM2OCCxZjCwMlA4OyEQvF2= MX:yOFkxODJ4Nh?=
A2780 Ml35SpVv[3Srb36gRZN{[Xl? NVLKfWI1OSCq NFPyZlFFVVOR NIOzU|VKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDFR|UxKG:oIECuNFc1KM7:TR?= M1XmbVI1QTByMk[2
MCF7 NIKwOJNHfW6ldHnvckBCe3OjeR?= NYrESlM3OSCq MWHEUXNQ NXr6WnNLUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP NGDxbJMzPDlyMEK2Oi=>
U87MG MYDGeY5kfGmxbjDBd5NigQ>? NGjIbHQyKGh? MV3EUXNQ M3v4XWlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFXDOVAhd2ZiMD6xN{DPxE1? M1;HO|I1QTByMk[2
A2780 NVLkUW9JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYm3NkBp M4Ll[GROW09? M4nCOmVEPTB;MD61NkDPxE1? Mme0NlQ6ODB{Nk[=
SKMES-1 NVmxXlNSS3m2b4TvfIlkKEG|c3H5 M3;HTlEh|ryP MkTPO|IhcA>? MUHJcoR2[2W|IHPlcIwh\GWjdHi= M4TJdlI3ODF|M{G4
H596 MXTGeY5kfGmxbjDBd5NigQ>? MV:xJO69VQ>? NH\3WotKdXCjaYLzJINmdGxibXnndoF1cW:w NEPq[3UzPjBzM{OxPC=>
HCC2450 NIDscGVHfW6ldHnvckBCe3OjeR?= NUTPcXp7OSEQvF2= NHzrcHpKdXCjaYLzJINmdGxiaX72ZZNqd25? Mn3PNlYxOTN|MUi=
A549 M4DCV2Z2dmO2aX;uJGF{e2G7 NFjudpk2ODBibl2= MnO4OFghcA>? NHTENVJFVVOR MnvKTY5pcWKrdIOgRYt1KGGldHn2ZZRqd25? MW[yOVk{PzJ7OR?=
A549 NV;hW5plT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnzNUDPxE1? NHjmTFY4OiCq M1Tv[2ROW09? NG\rWoRKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NX;6VIQ{OjV7M{eyPVk>
H522 NIraV2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XMT|Eh|ryP MmLCO|IhcA>? NVzEPG1YTE2VTx?= M{W4WWlvcGmkaYTzJINmdGxiZ4Lve5Rp NFvaeGczPTl|N{K5PS=>
LNCaP MmHmSpVv[3Srb36gRZN{[Xl? M4D4dFEh|ryP MWnTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? MXKyOVM3ODd7OR?=
LNCaP95 M1jzOmZ2dmO2aX;uJGF{e2G7 NYT5NY5xOSEQvF2= Mmj3V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MWqyOVM3ODd7OR?=
HCT-15 MlfORZBwfG:|aYOgRZN{[Xl? MYSxNEDPxE1? NXPK[m5oPDhiaB?= M4[zNGROW09? NHjud4ZKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVUh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= Mlm0NlUyPTJ{NEW=
HCT-116 M1\W[2Fxd3Sxc3nzJGF{e2G7 MUSxNEDPxE1? NGT3Wlg1QCCq MXvEUXNQ Mn3HTY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUGxOkBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NUTQVFJ1OjVzNUKyOFU>
NCI-H460 M4XYV2Fxd3Sxc3nzJGF{e2G7 NHzaO|IyOCEQvF2= NWnkNJNCPDhiaB?= M3zMNGROW09? M3Xie2lv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MV6yOVE2OjJ2NR?=
SKOV-3 MWfBdI91d3OrczDBd5NigQ>? MXuxNEDPxE1? NG\wUWc1QCCq M1\aTWROW09? NWLhNFdGUW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= M4e4VFI2OTV{MkS1
BSY-1 M{TKbmFxd3Sxc3nzJGF{e2G7 M1m4ZVExKM7:TR?= NXPLS4VxPDhiaB?= NXPPTJEyTE2VTx?= M3nqb2lv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M2nldVI2OTV{MkS1
MKN-1 NI\vd29CeG:2b4Ppd{BCe3OjeR?= NUHCVGg{OTBizszN NI\GWHU1QCCq MULEUXNQ NX;leY5mUW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NH2xR3kzPTF3MkK0OS=>
NCI-H522 M3jIN2Fxd3Sxc3nzJGF{e2G7 MYWxNEDPxE1? MUe0PEBp M3LuZmROW09? M13tXmlv\HWlZYOgZZBweHSxc3nz MXmyOVE2OjJ2NR?=
OVCAR-3 M1;WcmFxd3Sxc3nzJGF{e2G7 NGG4bYYyOCEQvF2= NUfQOolLPDhiaB?= NFi3cXhFVVOR M3zK[Glv\HWlZYOgZZBweHSxc3nz NVH5XXRYOjVzNUKyOFU>
HBC-5 M{K1VmFxd3Sxc3nzJGF{e2G7 NEnzOFEyOCEQvF2= MorwOFghcA>? Mkm4SG1UVw>? NFmxNWVKdmS3Y3XzJIFxd3C2b4Ppdy=> MUSyOVE2OjJ2NR?=
RXF-631L NFrzSGNCeG:2b4Ppd{BCe3OjeR?= MYixNEDPxE1? NIiwNIk1QCCq M1XWbmROW09? NUHWNFJDUW6mdXPld{BieG:ydH;zbZM> M3\LWVI2OTV{MkS1
MKN-45 NUHtUXBZSXCxdH;zbZMhSXO|YYm= MVexNEDPxE1? M4TSflQ5KGh? NHjYPZBFVVOR NHH0e25KdmS3Y3XzJIFxd3C2b4Ppdy=> MmDaNlUyPTJ{NEW=
BON-1 NEn0VmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\JOVAxKG6P M{LsS|ExKGR? MorlSG1UVw>? MoH1TY5pcWKrdIOgZ4VtdCCpcn;3eIg> M17iSVI2ODJ4Mkmy
BON-1 MoO2SpVv[3Srb36gRZN{[Xl? M1XwZlUxOCCwTR?= NG\ydZo1KGh? MVTEUXNQ M2HGN2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= MYGyOVAzPjJ7Mh?=
QGP-1 MWLGeY5kfGmxbjDBd5NigQ>? MVK1NFAhdk1? MUm0JIg> MX3EUXNQ MoXsTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= NWPsVlJ7OjVyMk[yPVI>
Huh7 NWjRXJlrTnWwY4Tpc44hSXO|YYm= M131OVEh|ryP NYLhdIFKOSCq M4XMNmROW09? MkTYTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? NYnJWXhvOjVyMES0NFM>
BNL M1;VfGZ2dmO2aX;uJGF{e2G7 MWmxJO69VQ>? NV[yZ|ZkOSCq MlzVSG1UVw>? NGPJNnJKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? NWTvepo5OjVyMES0NFM>
MDA-MB-175 NYH5S5FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXTZXBGOSEQvF2= MV61JIQ> MlzESG1UVw>? Ml20TWM2ODxzIN88US=> MWGyOFg4QTd7Nh?=
MDA-MB-134 M4nTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XG[|Eh|ryP M322b|Uh\A>? MUfEUXNQ M3\RdGlEPTB:MTFOwG0> NGjNVGIzPDh5OUe5Oi=>
HCC1500 M3LTRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnPS5cyKM7:TR?= MkH1OUBl M3zkb2ROW09? Mn2zTWM2ODxzIN88US=> NWnY[GZsOjR6N{m3PVY>
EFM-19 MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmSzNUDPxE1? Mk\kOUBl NHL0WZBFVVOR NX3mXW9DUUN3MEyxJO69VQ>? M3\6SVI1QDd7N{m2
ZR-75-30 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLrNUDPxE1? NVG5NJl7PSCm Ml;1SG1UVw>? NYj4fZV1UUN3MEyxJO69VQ>? MVuyOFg4QTd7Nh?=
MDA-MB-361 M3XyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxJO69VQ>? M17leFUh\A>? M2nZW2ROW09? Mn:2TWM2ODxzIN88US=> MUKyOFg4QTd7Nh?=
T-47D NIXNZlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrqeVkyKM7:TR?= NVzRenN5PSCm M3HOfGROW09? MlrzTWM2ODxzIN88US=> MlPpNlQ5Pzl5OU[=
SK-BR-3 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrlc5VYOSEQvF2= MnXVOUBl NV\WZVFVTE2VTx?= MX;JR|UxRDFizszN MkewNlQ5Pzl5OU[=
UACC-732 Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYmw[3Z5OSEQvF2= NYLFRlBNPSCm NWPuZWpQTE2VTx?= NXL2UIluUUN3MEyxJO69VQ>? NXSydZgxOjR6N{m3PVY>
BT-474 M2f5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[yfFMzOSEQvF2= MljzOUBl MWPEUXNQ MUPJR|UxRDFizszN NIDCTlAzPDh5OUe5Oi=>
HCC202 MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOxJO69VQ>? NWTIOJFsPSCm Mlu5SG1UVw>? M1zNdWlEPTB:MTFOwG0> M3TF[lI1QDd7N{m2
MCF7 MlPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\vcFEh|ryP M{TrVFUh\A>? NXPQW5l5TE2VTx?= NYXyPHdyUUN3MEyxJO69VQ>? MXWyOFg4QTd7Nh?=
MDA-MB-415 NVPjTpJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M16wb|Eh|ryP MVm1JIQ> MoD0SG1UVw>? M3HXeGlEPTB:MTFOwG0> M2G4PVI1QDd7N{m2
MDA-MB-453 M2qzZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDmNUDPxE1? M2nhdFUh\A>? NIfoVHJFVVOR M3vxZWlEPTB:MTFOwG0> NEPmZmMzPDh5OUe5Oi=>
ZR-75-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml71NUDPxE1? NH;wXW42KGR? MkHvSG1UVw>? MWfJR|UxRDFizszN M3XVeFI1QDd7N{m2
HCC38 M2rXOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;JSFEh|ryP MoLOOUBl Ml\jSG1UVw>? NEe4bG9KSzVyPEGg{txO NF;sRlIzPDh5OUe5Oi=>
HCC1419 M4LpdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17GSFEh|ryP NH;GeG02KGR? NEX2XmxFVVOR MkLRTWM2ODxzIN88US=> MVGyOFg4QTd7Nh?=
UACC-812 NUL5cIR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHBNUDPxE1? MnL5OUBl MXnEUXNQ M4rCUWlEPTB:MTFOwG0> NVrScYQ3OjR6N{m3PVY>
HCC1187 NVXJTYc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnB[3UyKM7:TR?= NV3QVmNlPSCm MXfEUXNQ M4PBVWlEPTB:MTFOwG0> MkTjNlQ5Pzl5OU[=
KPL-1 NEPUWWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XjSVEh|ryP MnLLOUBl NUDPcVJZTE2VTx?= NVfPSJFsUUN3MEyxJO69VQ>? NUXDb2w1OjR6N{m3PVY>
SUM-225 NXi3OW96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF36SFIyKM7:TR?= MVG1JIQ> MXHEUXNQ NIHkRo5KSzVyPEGg{txO NE[zOWczPDh5OUe5Oi=>
EFM-192A M4T5VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITN[pEyKM7:TR?= MnfKOUBl M{nWZWROW09? NGr6d|lKSzVyPEGg{txO NXS0S2ttOjR6N{m3PVY>
JIMT-1 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTGNUDPxE1? NHTaWZc2KGR? M4n5VmROW09? NI[1fJFKSzVyPEGg{txO MnvUNlQ5Pzl5OU[=
HCC1143 NIjoTXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\HRXEyKM7:TR?= MkW1OUBl M1flT2ROW09? NXWyXWw1UUN3MEyxJO69VQ>? NIXnUGMzPDh5OUe5Oi=>
HCC2218 MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zMZlEh|ryP NEn3XWE2KGR? NIP3WoFFVVOR MXHJR|UxRDFizszN NFPRTpczPDh5OUe5Oi=>
MDA-MB-468 NXjkd|dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXPU5p3OSEQvF2= MYi1JIQ> NXzMeWNqTE2VTx?= Mkj3TWM2ODxzIN88US=> NF7QVXYzPDh5OUe5Oi=>
BT-20 NHHV[GRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37ZcVEh|ryP NILWdW02KGR? NGH4O4lFVVOR MUjJR|UxRDFizszN NXj3bVRJOjR6N{m3PVY>
MDA-MB-435 NEC3VYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYruNJpZOSEQvF2= NVX1VYNVPSCm MX;EUXNQ Mm\mTWM2ODxzIN88US=> NXztb4lPOjR6N{m3PVY>
BT-549 NFrFSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XqdlEh|ryP NUCwZ5VuPSCm MkW5SG1UVw>? Mm\xTWM2ODxzIN88US=> MlvNNlQ5Pzl5OU[=
HCC1806 M37JXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjWNUDPxE1? NYjqSpN{PSCm MUDEUXNQ NF7Fc|JKSzVyPEGg{txO NXnmW2ROOjR6N{m3PVY>
HCC1937 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLadogyKM7:TR?= MoTiOUBl MlmxSG1UVw>? M{HObmlEPTB:MTFOwG0> M3XxfFI1QDd7N{m2
Hs578T NYq3[YRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rxXFEh|ryP NY[3bWhjPSCm MUXEUXNQ MULJR|UxRDFizszN MlPnNlQ5Pzl5OU[=
LN18 M1vZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHpU29JOjBizszN NHXLd484OiCq M4fodWROW09? NWDsd|RnUUN3MEy1JO69VQ>? M2HRNVI1PzRzMEe0
LN229 NYTtV|FmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjZVoMzOCEQvF2= MXG3NkBp MoLESG1UVw>? M{D2dGlEPTB:NTFOwG0> MlqzNlQ4PDFyN{S=
LNZ308 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi2WXF1OjBizszN NYHvSGFxPzJiaB?= MmW2SG1UVw>? NHPI[25KSzVyPEWg{txO MXOyOFc1OTB5NB?=
T98G MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[yNEDPxE1? NUH0Wmk{PzJiaB?= NYjyZ5ljTE2VTx?= NHPQVlJKSzVyPEWg{txO MnLINlQ4PDFyN{S=
U87 MkLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXyyNEDPxE1? NXm5eJpCPzJiaB?= NGK0eJVFVVOR MV\JR|UxRDVizszN Ml\CNlQ4PDFyN{S=
LN18 M{ixTWZ2dmO2aX;uJGF{e2G7 NGfiT|U2KM7:TR?= NXXBUId6OjRiaB?= NV3EU2R1TE2VTx?= M3PqdmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? Mnj6NlQ4PDFyN{S=
LNZ308 NX61c|ZMTnWwY4Tpc44hSXO|YYm= NEDw[Hc2KM7:TR?= MX2yOEBp NVrFe4tXTE2VTx?= Mo\hTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? MlH3NlQ4PDFyN{S=
Saos-2 NHiz[IVHfW6ldHnvckBCe3OjeR?= NV\p[3c4PTBizszN NV;GZVJXPDhiaB?= MVTJcohq[mm2czDj[YxtKGmwdnHzbY9v NVK4W3ZlOjR5Mke2OlA>
MG-63 MoPmSpVv[3Srb36gRZN{[Xl? MojvOVAh|ryP M2niZVQ5KGh? M37wUGlvcGmkaYTzJINmdGxiaX72ZZNqd25? MVyyOFczPzZ4MB?=
SJSA-1 NG\r[2tHfW6ldHnvckBCe3OjeR?= MmrIOVAh|ryP NU\aRVhWPDhiaB?= M4TTcGlvcGmkaYTzJINmdGxiaX72ZZNqd25? MlnrNlQ4Ojd4NkC=
Saos-2 NYXKXoZ5TnWwY4Tpc44hSXO|YYm= M1W3bVUxKM7:TR?= M1LkOFQ5KGh? NFLDXJZKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v MWOyOFczPzZ4MB?=
MG-63 NYXU[|VKTnWwY4Tpc44hSXO|YYm= MUC1NEDPxE1? MWS0PEBp MXzJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NWHpOnJHOjR5Mke2OlA>
SJSA-1 NUjkO4huTnWwY4Tpc44hSXO|YYm= NITaXGk2OCEQvF2= MnzKOFghcA>? NFTWVo1KdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v Mk[3NlQ4Ojd4NkC=
Saos-2 MlnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYSzfmtzPTBizszN NHLB[|I1QCCq M{jtRWlvcGmkaYTzJINmdGxidnnhZoltcXS7 M3:2U|I1PzJ5Nk[w
MG-63 MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LhZlUxKM7:TR?= MnzvOFghcA>? NGjLSJlKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MX[yOFczPzZ4MB?=
SJSA-1 NF3SdGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;hWnZJPTBizszN NETxS4E1QCCq NWG5WWZnUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= NUjxbohKOjR5Mke2OlA>
FaDu NHzuO2lHfW6ldHnvckBCe3OjeR?= NGLqT2M2KM7:TR?= M13HfFI1KGh? NXmzUZFtTE2VTx?= NH3NPW1T\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MV:yOFY{OTF2Nx?=
EMT6 MlfMSpVv[3Srb36gRZN{[Xl? NXjUWXBXPSEQvF2= MVqyOEBp MVvEUXNQ MUHS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NH3sVmczPDZ|MUG0Oy=>
HCT116 NWHVTIVyTnWwY4Tpc44hSXO|YYm= NY\VOWJVPSEQvF2= MnTGNlQhcA>? M4PNbmROW09? NYHUSGNzWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MYKyOFY{OTF2Nx?=
U87 MV;GeY5kfGmxbjDBd5NigQ>? MoTSOUDPxE1? M2f1flI1KGh? MVrEUXNQ M2HLeHJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u NHLTVIQzPDZ|MUG0Oy=>
GBM NELjTYFCeG:ydH;zbZMhSXO|YYm= NYTxSFNrOs7:TR?= NXTjNGx5PDiq MmHxSG1UVw>? M3;sdolv\HWlZXSgbIlocGW{IHzleoVteyCxZjDhdI9xfG:|aYOsJIFv\CCmZXPy[YF{\WRiY3XscEB3cWGkaXzpeJk> NGTEVWszPDVyMES5Ni=>
BON NX7PNVFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWxMVXPxE1? M3zLUVczcA>? NF20U|Bl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v M{fFR|I1PDR|NUKz
BON M2jqWGFxd3C2b4Ppd{BCe3OjeR?= Mmq1NU02|ryP NEnKZXIzPGh? Mn\sbY5kemWjc3XzJIFxd3C2b4Ppdy=> M37TOVI1PDR|NUKz
H1975 NXfhZ3NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWGwMlMuQS54zszN MmO2O|Jp NFS1VIVFVVOR MlHxTWM2OD1zLkO4Oe69VQ>? NI\aRnczPDN|N{i0Oi=>
H1975 NFf4epBCeG:ydH;zbZMhSXO|YYm= MXmy{txO NVztcIpCOjSq MV3EUXNQ M4GyWYlv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 NX3CfFkzOjR|M{e4OFY>
T-ALL NXSzbYp{SXCxcITvd4l{KEG|c3H5 NXnENllT[mW2d3XlckAyNjRiYX7kJFUvOyCvTTDheEAzPGhiYX7kJFAvQSCjbnSgOU42KG2PIHH0JFQ5cCCrbjDkbYZn\XKnboSgZ4VtdCCuaX7l NX3WSmJ7OjRib4KgOFhp MYXEUXNQ MWLh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= NXmwOXFDOjR|MUC3N|Y>
BCR-ABL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3HSFdJOC5{NT2xNO69VQ>? NXW3bYJiPGR? MlrNd4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>? MXeyOFI1PDZzMh?=
LC-1/SQSF M13peWZ2dmO2aX;uJGF{e2G7 NWXqVWluO87:TR?= NFfwPWIzPGh? M{jWXmROW09? M4T0W4Rm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> NInzNHozOzl6MEC5Ny=>
Primary CLL cells NEPFbmtCeG:ydH;zbZMhSXO|YYm= M3u2NVEuOTEQvF2= M{jWSFQ5cA>? MorjbY5lfWOnczDhdI9xfG:|aYOgbY4hS0yOIHPlcIx{KGmwZHXw[Y5l\W62IH;mJJBzd2ewb4P0bYMhdWG{a3Xydy=> NVHt[GxmOjN6NUC4NFc>
Primary CLL cells M13ZcGtqdmG|ZTDBd5NigQ>? Ml[zNu69VQ>? M4XJNFMxdWmw NEjSfI1l\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= NEj1UlkzOzh3MEiwOy=>
Primary CLL cells NHe2SGVEgXSxdH;4bYMhSXO|YYm= MWqy{txO Mn\tNlRp NU\t[YlWcW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=> M3fIZVI{QDVyOEC3
human NSCLC cell lines NYWwVGM1SXCxcITvd4l{KEG|c3H5 Mn;NNE4yOjVvNN88US=> NV\xbYRKOjSq Mn[xSG1UVw>? NFPoe|hKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> MkDrNlM2PjJ2N{K=
human HCC cell lines NUjiVJZqS2WubDD2bYFjcWyrdImgZZN{[Xl? NHfWVm4xNjByNT2x{txO NX7QVWlPPDiq MmPCTWM2OD1zzszN MoDSNlM1QDl7OUm=
Huh7 MoHMT4lv[XOnIFHzd4F6 NHP4Uncy|ryP M{Lwe|Q5cA>? MXnzbYdvce,ugXPhcpRtgSC{ZXT1Z4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= Mm\LNlM1QDl7OUm=
SK-HEP1 Mkj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:x[IR3OS1{MN88US=> NX[4O3dDPzKq Mnj4SG1UVw>? NVfvSGNRUUN3MP-8oFHPxE1? MlWwNlM1PzlzM{[=
786-0 NHPvRWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xMVIx|ryP NI\sUlM4Omh? NHX3WZdFVVOR MXXJR|Ux97zeMd88US=> NFrxWG4zOzR5OUGzOi=>
JVM2 NYP0dWhjS3m2b4TvfIlkcXS7IHHzd4F6 MUOwMlIuOjEQvF2= NFTXcJI4Omh? MXzEUXNQ NILPRXRKSzVyPUCuPe69VQ>? MlvFNlMzOzh4M{m=
EHEB NXzFR5Q{S3m2b4TvfIlkcXS7IHHzd4F6 M2jLbVAvOi1{MN88US=> M3jZdlczcA>? NXO4fIRDTE2VTx?= NEL5VXVKSzVyPUCuO:69VQ>? M2fRPFI{OjN6NkO5
MEC2 M37RNWN6fG:2b4jpZ4l1gSCjc4PhfS=> NInOV3YxNjJvMkFOwG0> M{DMbVczcA>? MXzEUXNQ MUXJR|UxRTBwN988US=> M165dlI{OjN6NkO5
primary B-CLL lymphocytes M164UWFxd3C2b4Ppd{BCe3OjeR?= MX\JR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m MlHRNlRp MYjEUXNQ MX7JR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz NVvzWGdZOjN{M{i2N|k>
primary B-CLL lymphocytes M37UPGtqdmG|ZTDBd5NigQ>? MVPJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m NF\heFMzPGh? M2Dhc4lvcGmkaYTzJJA4OFN4SzCmJFRGNUKSMTDlfJBz\XO|aX;u MVmyN|I{QDZ|OR?=
human NSCLC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrxcG8xNjVvMt88US=> MnXKO|Jp NWGx[5d2UUN3ME2x{txO MWCyNlc5OTN7Mx?=
human NSCLC MmmwT4lv[XOnIFHzd4F6 M1THR|HPxE1? NY\wfIVNOjSq MVPpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 NVHIeXk3OjJ5OEGzPVM>
Y1 cell line NX\ZXGhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HHTFAvOc7:TT:x{txO NHjHRYszPGh? NUnhSVg{TE2VTx?= M3X5U4lvcGmkaYTzJFYx97zHIHPlcIwhfmmjYnnsbZR6KGmwIF35Z{1U[3S{LYTyZY5{\mWldHXkJINmdGy| MV6yNlY6OjlyNB?=
PIK3CA-mutant MCF7 NFrIOWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? MoDKO|Jp NXn5NVExT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NFvMXW0zOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 NFTPV4pMcW6jc3WgRZN{[Xl? MUXJR|UxRTFzNNMxN45O MVS3Nog> MmPiTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= MVuyNlY2Ozl4Nx?=
MCF7-myr-Akt M1TjSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn0VVZIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= MV23Nog> NWDEVXNkT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= NFfYWVMzOjZ3M{m2Oy=>
colon cancer cell lines NH;Cd2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWwMVEx|ryP MWi3Nog> MUPEUXNQ MXjJR|UxRTIQvF2= MlLzNlI2PDN6NUe=
gastric cancer cell lines NGXvUW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q0XFAuOTEQvF2= NH:5UWs4Omh? NXi0SnZkTE2VTx?= NHnKUHBKSzVyPUKtOe69VQ>? M3voOVIzPTR|OEW3
HCT-116/HT-29/MKN-45 MnmyRZBweHSxc3nzJGF{e2G7 NYT2PIpLOs7:TR?= M4SydlQ5cA>? MXXzbIlnfCCrbjDHNkBxcGG|ZR?= NXnaOmZPOjJ3NEO4OVc>
HT-29 and HCT-116 NEDOWHpE[XOyYYPlJIF{e2G7 NVXXVIExPc7:TR?= M2\sfFI1cA>? MUnpcoR2[2W|IHPhd5Bie2ViYXP0bZZqfHl? M{HmWlIzPTR|OEW3
MM cell lines MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGxNO69VQ>? Mm[0NlRp NFq5NIhFVVOR MVXJR|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U> NGm2NJczOjJyN{S4OS=>
ARP-1 MmX3RZBweHSxc3nzJGF{e2G7 NILnfWoyOM7:TR?= NW\RbmtGOjSq MlzxSG1UVw>? NUjtU4hrcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> NYrBXlMyOjJ{MEe0PFU>
SNU-601 NEXPOJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjPXlk4Omh? MXHEUXNQ MXTJR|UxRTBwOEG2xtExNjB4M988US=> M{HrcFIzOTV7OEG0
SNU-1 NWfUdZJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\oUVJnPzKq MmqwSG1UVw>? NIrmTHRKSzVyPUGuNFgzyrFyLkCyPO69VQ>? MVKyNlE2QThzNB?=
SNU-668 M2OydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTIdmtIPzKq M4DkemROW09? NH\U[FRKSzVyPUGuOVc6yrFyLkC3OO69VQ>? Mle4NlIyPTl6MUS=
AGS MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPkWHU4Omh? NHnH[oRFVVOR NHrReZNKSzVyPUGuO|E1yrFyLkGxO:69VQ>? NYK2c2Z7OjJzNUm4NVQ>
SNU-216 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS3Nog> NH2z[oJFVVOR MmC1TWM2OD1{Lk[5NuKyOC5yOENOwG0> NVHNeoxCOjJzNUm4NVQ>
SNU-5 NIq0fmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[3Nog> NWrGV|RSTE2VTx?= NEW1WphKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? NFH4W5UzOjF3OUixOC=>
SNU-638 MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTZO|Jp NGrUR4ZFVVOR MlfHTWM2OD1{LkK4NuKyOC5yNUROwG0> NVjmPJN6OjJzNUm4NVQ>
SNU-16 NFvZ[WlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX5Z5VHPzKq M4fOZ2ROW09? MXLJR|UxRTFwNUezxtExNjByMd88US=> NX:xSVZzOjJzNUm4NVQ>
SNU-484 MmHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXKy[oVqPzKq MWTEUXNQ MWHJR|UxRTFwN{K4xtExNjB2Nd88US=> MnzUNlIyPTl6MUS=
SNU-620 NX[3SHRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\qRVczcA>? NFX1dlVFVVOR MlLnTWM2OD1{LkmzPeKyOC5yMEJOwG0> M{HsVVIzOTV7OEG0
SNU-719 NILVUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\ZUI9zPzKq MnzwSG1UVw>? Mn7UTWM2OD1|LkCzO:KyOC5yM{NOwG0> MUWyNlE2QThzNB?=
glioma cell lines NIrpeJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzuPIM4Omh? MVnJR|UxRTFvMt88US=> M1HwclIzODZ3MEiw
U87 NET0fpJCeG:ydH;zbZMhSXO|YYm= NVu1RoEyOs7:TR?= M3zJ[lczcA>? Mn7kbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= MXeyNlA3PTB6MB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT (T308) / p-AKT (S473) / AKT; 

PubMed: 27283525     


Left western blots showing levels of pAkt (T308), pAkt (S473) and total Akt in U87 cells exposed to buparlisib for 72 h. Right densitometric assessment of western blots, showing relative changes in phosphorylation.

p-FOXO3a (S253) / FOXO3a; 

PubMed: 28036259     


Cells were treated with 0.5 μM BKM120 for 24 h and cell lysates were immunoblotted with the indicated antibodies. Actin was used as the loading control.

Nuclear NF-κB p65 / NF-κB p65; 

PubMed: 26673665     


Western blots show BKM120 downregulating pAKT, nuclear NF-κB p65 and total NF-κB p65 in MDR and their parental cells. β-actin was used as a loading control for pAKT, AKT and total NF-κB p65. Lamin B was used as a loading control for nuclear NF-κB p65. 

p-ERK / ERK / LC3; 

PubMed: 27572309     


The indicated cell lines were exposed to different concentrations of BKM120 as indicated for 8 h A. or with 2 μM BKM120 for the indicated times B. The cells were then harvested for preparation of whole-cell protein lysates and subsequent Western blot analysis to detect the given proteins.

p-STAT3 / STAT3 / p-ERK / ERK / p-S6; 

PubMed: 29928341     


Western blot analysis of H460 and H2126 cell lysates using specific antibodies to phosphorylated or total proteins of STAT3, ERK1/2, AKT, S6 or GAPDH (loading control). The cells were treated with increasing concentrations of BKM120 for 24 h.

p-MET / MET; 

PubMed: 29928341     


The expression of phosphorylated or total forms of MET protein was analyzed by western blotting. 

27283525 28036259 26673665 27572309 29928341
Immunofluorescence
FOXO3a; 

PubMed: 28036259     


Cells were cultured on coverslips to approximately 60% confluency and then treated with 1 μM BKM120 for an additional 24 h. Immunofluorescence staining was performed using an anti-FOXO3a antibody and the nuclei were stained with DAPI. Scale bar, 20 μm.

28036259
Growth inhibition assay
Cell viability; 

PubMed: 26673665     


Dose-response curves were used to calculate the IC50 of BKM120 for MCs of MCF-7/A02 cells (upper) and CALDOX cells (lower).

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

Kinase Assay:[1]
- Collapse

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]
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  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: U87MG and A2780 xenografts are established in female nu/nu mice.
  • Dosages: ~60 mg/kg.
  • Administration: Dosed orally daily (q.d.).
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (199.8 mM)
Water Insoluble
Ethanol '2 mg/mL
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

* 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

Molecular Weight 410.39
Formula

C18H21F3N6O2

CAS No. 944396-07-0
Storage powder
in solvent
Synonyms NVP-BKM120
Smiles NC1=CC(=C(C=N1)C2=NC(=NC(=C2)N3CCOCC3)N4CCOCC4)C(F)(F)F

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    C2
    V2

* 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

  • 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

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04338399 Not yet recruiting Drug: Buparlisib & Paclitaxel Head and Neck Cancer Adlai Nortye Biopharma Co. Ltd. July 31 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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Related PI3K Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID