Buparlisib (BKM120, NVP-BKM120)

Catalog No.S2247

Buparlisib (BKM120, NVP-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. Phase 2.

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In DMSO USD 272 In stock
USD 170 In stock
USD 320 In stock
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Cited by 38 Publications

6 Customer Reviews

  • NLGN3 mRNA expression in SU-pcGBM2 cells after 12 hr exposure to vehicle, 50 nM NLGN3, 100 nM BKM120, or 50 nM NLGN3 + 100 nM BKM120.

    Cell, 2017, 161(4):803-16. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

    Western blot analysis of cleaved caspase 3 in T cell-enriched PBMCs.

    J Hematol Oncol, 2016, 9(1):113. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

  • AN3CA (A) and JHUEM2 (B) cells were treated for the indicated times with DMSO, 0.3 μM BGJ398 (BGJ), 0.3 μM GDC-0941 (GDC), 0.6 μM BYL719 (BYL) and 0.6 μM BKM120 (BKM) alone or in combination. Cell lysates were immunoblotted with antibodies for phospho-AKT (Ser473), total AKT, phospho-ERK (Thr202/Tyr204), ERK2, phospho-S6 (Ser240/244), total S6, phospho-4EBP1 (Thr37/46), total 4EBP1, total PARP and cleaved PARP. Tubulin was detected as the loading control. Western blot analysis of AN3CA and JHUEM2.

    Mol Cancer Ther, 2017, 16(4):637-648. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

    After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of BKM120 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

  • One customer. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

    Dr. Pilar Eroles of INCLIVA Biomedical Research Institute.. Buparlisib (BKM120, NVP-BKM120) purchased from Selleck.

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. 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 Mo\ZR5l1d3SxeHnjJGF{e2G7 NUfr[|ZwPzJiaB?= MmjJSG1UVw>? MoL1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?= MkW2NlQ6ODB{Nk[=
DU145 M1rlS2N6fG:2b4jpZ{BCe3OjeR?= NEPYUWE4OiCq M4[4XGROW09? Mm\kR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh\XiycnXzd4lv\yCOS1KxJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMEC0N|Uh|ryP NUfkfnBYOjR7MECyOlY>
A2780 NH7GN4NEgXSxdH;4bYMhSXO|YYm= MXW3NkBp NHPFXVJFVVOR NHT2TYVEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN MXeyOFkxODJ4Nh?=
U87MG MmHOR5l1d3SxeHnjJGF{e2G7 Ml3qO|IhcA>? NEHjXFdFVVOR NET2NJNEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN NXTXS45JOjR7MECyOlY>
A2780 NX7ldnM2TnWwY4Tpc44hSXO|YYm= M3Pve|EhcA>? MlLKSG1UVw>? MWXJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? MUGyOFkxODJ4Nh?=
DU145 NVvlPHZVTnWwY4Tpc44hSXO|YYm= NEDZcIQyKGh? NFfRfWpFVVOR NVTONmxGUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKESXMUS1JINmdGy|IHjhdoJwemmwZzDMT2IyKG23dHH0bY9vKHerdHigSWM2OCCxZjCwMlA4OyEQvF2= Mn\tNlQ6ODB{Nk[=
A2780 NWLwc|d1TnWwY4Tpc44hSXO|YYm= M4DucVEhcA>? Mo\PSG1UVw>? MWDJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>? M2DGSlI1QTByMk[2
MCF7 MnfFSpVv[3Srb36gRZN{[Xl? M3XuO|EhcA>? NV;nNnltTE2VTx?= MnrrTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO NEnpOIEzPDlyMEK2Oi=>
U87MG NXq3c2R{TnWwY4Tpc44hSXO|YYm= NIG3R|AyKGh? Ml35SG1UVw>? Mn3rTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiRVO1NEBw\iByLkGzJO69VQ>? M{X1eFI1QTByMk[2
A2780 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljlO|IhcA>? M1vB[2ROW09? NVq5[ZBITUN3ME2wMlUzKM7:TR?= M3vnZVI1QTByMk[2
SKMES-1 NVP2WmJYS3m2b4TvfIlkKEG|c3H5 M{TIc|Eh|ryP MlvQO|IhcA>? MVzJcoR2[2W|IHPlcIwh\GWjdHi= M2XqRlI3ODF|M{G4
H596 MUnGeY5kfGmxbjDBd5NigQ>? MlHHNUDPxE1? NGTieFRKdXCjaYLzJINmdGxibXnndoF1cW:w NID1bmkzPjBzM{OxPC=>
HCC2450 M2LwRWZ2dmO2aX;uJGF{e2G7 M2nxcVEh|ryP NUX1Sok1UW2yYXnyd{Bk\WyuIHnueoF{cW:w Mm\4NlYxOTN|MUi=
A549 Mnn3SpVv[3Srb36gRZN{[Xl? NGj0NZI2ODBibl2= NYnaXJpDPDhiaB?= MkHxSG1UVw>? NHyxTldKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= MUWyOVk{PzJ7OR?=
A549 NGfreFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3j3cVEh|ryP M4jhTVczKGh? NUDhdHhuTE2VTx?= NH7JVJZKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NYTzR2VlOjV7M{eyPVk>
H522 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTL[VgyKM7:TR?= MVO3NkBp NWnlUmJDTE2VTx?= MWXJcohq[mm2czDj[YxtKGe{b4f0bC=> NGjBbJczPTl|N{K5PS=>
LNCaP MnvBSpVv[3Srb36gRZN{[Xl? MWOxJO69VQ>? MVXTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? M4D3[|I2OzZyN{m5
LNCaP95 Mn31SpVv[3Srb36gRZN{[Xl? NUjoVpQ1OSEQvF2= MmP4V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MUSyOVM3ODd7OR?=
HCT-15 NH\NXFdCeG:2b4Ppd{BCe3OjeR?= NHrtNYMyOCEQvF2= MWK0PEBp NF3WWlBFVVOR M{DQNWlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xOUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MYCyOVE2OjJ2NR?=
HCT-116 MUDBdI91d3OrczDBd5NigQ>? NH\YXXoyOCEQvF2= MlXhOFghcA>? MnLQSG1UVw>? MV;JcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MWOyOVE2OjJ2NR?=
NCI-H460 MXrBdI91d3OrczDBd5NigQ>? MWCxNEDPxE1? MYK0PEBp NVjQW5hWTE2VTx?= M{TxdWlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NEHvNXAzPTF3MkK0OS=>
SKOV-3 MkDJRZBwfG:|aYOgRZN{[Xl? NUfjVJpoOTBizszN MUW0PEBp M1\5d2ROW09? NV\zR2ZmUW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= Mn3FNlUyPTJ{NEW=
BSY-1 MmnpRZBwfG:|aYOgRZN{[Xl? MlT4NVAh|ryP NYPWbXRqPDhiaB?= NWXjcYk1TE2VTx?= NI\ZWZdKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCEU2mtNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MnPaNlUyPTJ{NEW=
MKN-1 NGHZSpRCeG:2b4Ppd{BCe3OjeR?= NXjFNG92OTBizszN M1HLdFQ5KGh? NF62TYRFVVOR MWHJcoR2[2W|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NIDvTFYzPTF3MkK0OS=>
NCI-H522 M1rKOGFxd3Sxc3nzJGF{e2G7 M2nGSFExKM7:TR?= MYi0PEBp NFHMTYZFVVOR MlfsTY5lfWOnczDhdI9xfG:|aYO= NYHacm5QOjVzNUKyOFU>
OVCAR-3 Ml33RZBwfG:|aYOgRZN{[Xl? NV\uOZh6OTBizszN MVO0PEBp NH;iPFdFVVOR NX3W[oM2UW6mdXPld{BieG:ydH;zbZM> NHLRNmYzPTF3MkK0OS=>
HBC-5 MnTWRZBwfG:|aYOgRZN{[Xl? MXOxNEDPxE1? M37QcFQ5KGh? M3z4dGROW09? NVjR[Zh6UW6mdXPld{BieG:ydH;zbZM> M4faOFI2OTV{MkS1
RXF-631L Mn;vRZBwfG:|aYOgRZN{[Xl? NXLEUphDOTBizszN MmfyOFghcA>? NGnxOJJFVVOR MonTTY5lfWOnczDhdI9xfG:|aYO= NHjWWm8zPTF3MkK0OS=>
MKN-45 NWe2UJVSSXCxdH;zbZMhSXO|YYm= MXSxNEDPxE1? M1zIcVQ5KGh? MnfXSG1UVw>? NH;2OpdKdmS3Y3XzJIFxd3C2b4Ppdy=> M1PneFI2OTV{MkS1
BON-1 NFy2dFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW1NFAhdk1? MYSxNEBl Mn3ySG1UVw>? MljQTY5pcWKrdIOgZ4VtdCCpcn;3eIg> NHnHdXIzPTB{NkK5Ni=>
BON-1 NHXtSplHfW6ldHnvckBCe3OjeR?= NXjadmx1PTByIH7N MlL6OEBp NVnrWYZkTE2VTx?= MWPJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NV;NfXJyOjVyMk[yPVI>
QGP-1 M2HnSmZ2dmO2aX;uJGF{e2G7 MlvWOVAxKG6P M1i0NVQhcA>? NX;DRVM4TE2VTx?= NX7HcHFoUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> NFrW[4EzPTB{NkK5Ni=>
Huh7 NE\aZY1HfW6ldHnvckBCe3OjeR?= Mm\PNUDPxE1? MWCxJIg> M1T0OmROW09? MmSzTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? MoPTNlUxODR2MEO=
BNL M4Pa[GZ2dmO2aX;uJGF{e2G7 NI\z[XEyKM7:TR?= NFPCOZUyKGh? MVrEUXNQ Mny3TY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3 MYqyOVAxPDRyMx?=
MDA-MB-175 M1vZSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XnT|Eh|ryP MYm1JIQ> M4fKNWROW09? MX;JR|UxRDFizszN MXuyOFg4QTd7Nh?=
MDA-MB-134 MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPkNUDPxE1? M{\ZbFUh\A>? NHja[lNFVVOR M4\hbGlEPTB:MTFOwG0> NXjv[m1ZOjR6N{m3PVY>
HCC1500 NWfBdoFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2xJO69VQ>? MmTiOUBl MVzEUXNQ NIHMNXBKSzVyPEGg{txO MUOyOFg4QTd7Nh?=
EFM-19 M2Tr[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H4XlEh|ryP MlXSOUBl Mmn5SG1UVw>? NG[1c41KSzVyPEGg{txO MkLNNlQ5Pzl5OU[=
ZR-75-30 NGCzPXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO4NUDPxE1? NUHKO2hkPSCm NF;UfFBFVVOR M1qxcWlEPTB:MTFOwG0> MljHNlQ5Pzl5OU[=
MDA-MB-361 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIqyfmQyKM7:TR?= NXi3cI5KPSCm MmLTSG1UVw>? M1TRTWlEPTB:MTFOwG0> MoWxNlQ5Pzl5OU[=
T-47D MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonLNUDPxE1? Mkm2OUBl NGXwZ2VFVVOR NIPSV4xKSzVyPEGg{txO M{K1NVI1QDd7N{m2
SK-BR-3 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfWc2dlOSEQvF2= NELqWGU2KGR? MVzEUXNQ MkLJTWM2ODxzIN88US=> MlvSNlQ5Pzl5OU[=
UACC-732 NXHY[5NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[xJO69VQ>? NEX6fHU2KGR? NYjnUGhYTE2VTx?= NVu0b3JQUUN3MEyxJO69VQ>? NFXwbHgzPDh5OUe5Oi=>
BT-474 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSxJO69VQ>? M3zLWlUh\A>? M17FWmROW09? NIXO[pZKSzVyPEGg{txO M2jPdlI1QDd7N{m2
HCC202 M2jiVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLPNUDPxE1? M3fyVVUh\A>? M{TkTGROW09? NXewTWliUUN3MEyxJO69VQ>? MknENlQ5Pzl5OU[=
MCF7 MmLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnVOldsOSEQvF2= MXe1JIQ> NYD4W|lxTE2VTx?= NH[wN5ZKSzVyPEGg{txO MkjuNlQ5Pzl5OU[=
MDA-MB-415 NHnlc5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC1dIVTOSEQvF2= MoLjOUBl MXrEUXNQ MorDTWM2ODxzIN88US=> NIHHUWozPDh5OUe5Oi=>
MDA-MB-453 MlPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHKeI8yKM7:TR?= Mnm4OUBl M17iT2ROW09? MXPJR|UxRDFizszN NFGxeZkzPDh5OUe5Oi=>
ZR-75-1 M3rvW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHtNUDPxE1? MnfWOUBl MW\EUXNQ M4m2UGlEPTB:MTFOwG0> MlnmNlQ5Pzl5OU[=
HCC38 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[xJO69VQ>? NVS3TZNxPSCm MYrEUXNQ MVjJR|UxRDFizszN NHHNOWgzPDh5OUe5Oi=>
HCC1419 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvUZ4oyKM7:TR?= MVW1JIQ> Mor6SG1UVw>? NX74fHZNUUN3MEyxJO69VQ>? NHHZd5QzPDh5OUe5Oi=>
UACC-812 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX2[lM6OSEQvF2= NFm1RW42KGR? M3zGNmROW09? MmL1TWM2ODxzIN88US=> NUDtdI9IOjR6N{m3PVY>
HCC1187 M1TBc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPkVokyKM7:TR?= M3y3TFUh\A>? M{\LdmROW09? MWTJR|UxRDFizszN Ml3aNlQ5Pzl5OU[=
KPL-1 Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{W3R|Eh|ryP M1nnWVUh\A>? MWjEUXNQ NFHmOJRKSzVyPEGg{txO NWj5XHo1OjR6N{m3PVY>
SUM-225 NEP4No1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TiWVEh|ryP M{\CNVUh\A>? MUHEUXNQ M3zyPGlEPTB:MTFOwG0> MmfVNlQ5Pzl5OU[=
EFM-192A M4L4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvQR25pOSEQvF2= NF;EcG42KGR? NH7FPWdFVVOR MlHFTWM2ODxzIN88US=> MUWyOFg4QTd7Nh?=
JIMT-1 M{LxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWSzSFl1OSEQvF2= M37RV|Uh\A>? NWX0V4RrTE2VTx?= NGHSbVdKSzVyPEGg{txO MXmyOFg4QTd7Nh?=
HCC1143 NX[z[XZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfBcIdOOSEQvF2= M2O5flUh\A>? NETRPVBFVVOR Mkf3TWM2ODxzIN88US=> MojENlQ5Pzl5OU[=
HCC2218 NYjmWmtMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrDNUDPxE1? MmDEOUBl MnXZSG1UVw>? NFLzflRKSzVyPEGg{txO NHnEcVkzPDh5OUe5Oi=>
MDA-MB-468 NXH3XHFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLYZWZUOSEQvF2= MXi1JIQ> MXjEUXNQ NFjpbIlKSzVyPEGg{txO MYCyOFg4QTd7Nh?=
BT-20 NVL2XHpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrRNUDPxE1? NIPub442KGR? NHXid3VFVVOR NFXSZndKSzVyPEGg{txO NHW2dmIzPDh5OUe5Oi=>
MDA-MB-435 NHLodVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVKxJO69VQ>? Mkn1OUBl MXPEUXNQ MV7JR|UxRDFizszN NFSxU3YzPDh5OUe5Oi=>
BT-549 NYL1PZJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSxJO69VQ>? NX\5fnN[PSCm M4PZe2ROW09? NGXuTYJKSzVyPEGg{txO MYeyOFg4QTd7Nh?=
HCC1806 NFjiTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVixJO69VQ>? Mof1OUBl NYjSb4RKTE2VTx?= NWTjbph{UUN3MEyxJO69VQ>? MYKyOFg4QTd7Nh?=
HCC1937 NXrafHhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfxZnNGOSEQvF2= MnrEOUBl MVXEUXNQ NV3tRlE1UUN3MEyxJO69VQ>? M{HaZ|I1QDd7N{m2
Hs578T M2HHeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PlflEh|ryP NUXzXldGPSCm NVqwcXlTTE2VTx?= M{TMUmlEPTB:MTFOwG0> NXHEXHlkOjR6N{m3PVY>
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MG-63 MlL5SpVv[3Srb36gRZN{[Xl? MWC1NEDPxE1? M4PsblQ5KGh? NYTTcItCUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MkLTNlQ4Ojd4NkC=
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SJSA-1 M2n1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPqOVAh|ryP M3[wPFQ5KGh? NH;3WVZKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MoPtNlQ4Ojd4NkC=
FaDu MVzGeY5kfGmxbjDBd5NigQ>? M2fNOlUh|ryP MX[yOEBp M4jIeWROW09? NHXoU4xT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MljINlQ3OzFzNEe=
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HCT116 MXnGeY5kfGmxbjDBd5NigQ>? NUTEZ29WPSEQvF2= M3rDO|I1KGh? NU\OV5VRTE2VTx?= NG\1SGlT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MUeyOFY{OTF2Nx?=
U87 MYTGeY5kfGmxbjDBd5NigQ>? MlTFOUDPxE1? M{PjeVI1KGh? MX\EUXNQ NUnVPW1PWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MVmyOFY{OTF2Nx?=
GBM MY\BdI9xfG:|aYOgRZN{[Xl? MmLkNu69VQ>? MXK0PIg> MkHYSG1UVw>? NETDfm5qdmS3Y3XkJIhq\2incjDs[ZZmdHNib3[gZZBweHSxc3nzMEBidmRiZHXjdoVie2WmIHPlcIwhfmmjYnnsbZR6 M4faU|I1PTByNEmy
BON NYTZcJZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\INU02|ryP NYLvZppJPzKq MoTr[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NEj1[lczPDR2M{WyNy=>
BON M4nyVmFxd3C2b4Ppd{BCe3OjeR?= MWWxMVXPxE1? MlrvNlRp NWD0To9ycW6lcnXhd4V{KGGyb4D0c5Nqew>? MXyyOFQ1OzV{Mx?=
H1975 NWXlW|FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlOyNE4{NTlwNt88US=> M2HNSFczcA>? MlXKSG1UVw>? NHvxN4VKSzVyPUGuN|g2|ryP NYrodGU1OjR|M{e4OFY>
H1975 M{XCfGFxd3C2b4Ppd{BCe3OjeR?= MmHqNu69VQ>? Mon3NlRp NFrwcHVFVVOR NVLzTZRGcW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl? MY[yOFM{Pzh2Nh?=
T-ALL NX75XJRxSXCxcITvd4l{KEG|c3H5 NFLoSZFj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW= NWGzcmdKOjRib4KgOFhp Ml\CSG1UVw>? M3TuUYFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz MVKyOFMyODd|Nh?=
BCR-ABL MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PlZ|AvOjVvMUFOwG0> NX3aRlBPPGR? M3HBdpNq\26rZnnjZY51dHliaX7obYJqfCClZXzsJJBzd2yrZnXyZZRqd25? NHu4[WUzPDJ2NE[xNi=>
LC-1/SQSF MoPHSpVv[3Srb36gRZN{[Xl? NVjMcnRiO87:TR?= Mk\GNlRp NGPkPGNFVVOR MVnk[YNz\WG|ZTDOVmYzKHC{b4TlbY4hdGW4ZXy= MonaNlM6QDByOUO=
Primary CLL cells NGTxRldCeG:ydH;zbZMhSXO|YYm= MmDxNU0yOM7:TR?= NGLxUpU1QGh? M4\uW4lv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> M{LLbVI{QDVyOEC3
Primary CLL cells NXG5ZoZSU2mwYYPlJGF{e2G7 M3\XOFLPxE1? M{j2WlMxdWmw NXLQeYE{\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm= NIXzNHozOzh3MEiwOy=>
Primary CLL cells NX[wcodzS3m2b4TvfIlkKEG|c3H5 M2TKZ|LPxE1? NX7oOY9ZOjSq M1P2Rolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= Mm[xNlM5PTB6MEe=
human NSCLC cell lines NVWzbYdKSXCxcITvd4l{KEG|c3H5 M1HONFAvOTJ3LUVOwG0> MkTRNlRp MULEUXNQ NHnqXHdKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> M1PKOlI{PTZ{NEey
human HCC cell lines MYnD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MmHFNE4xODVvMd88US=> NIPHW|k1QGh? M4PYSGlEPTB;Md88US=> NWjLfYoyOjN2OEm5PVk>
Huh7 Mk\oT4lv[XOnIFHzd4F6 M{LZW|HPxE1? MUC0PIg> M2DJNpNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M3\jelI{PDh7OUm5
SK-HEP1 NHfJPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnSNU0zOM7:TR?= NF\wbY44Omh? NVXTZXltTE2VTx?= NFe1ZYNKSzVy78{cNe69VQ>? MXSyN|Q4QTF|Nh?=
786-0 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELtVlcyNTJyzszN NH;uOJo4Omh? NHi5NpRFVVOR Mlj5TWM2OO,:nEJOwG0> NV3vbJBSOjN2N{mxN|Y>
JVM2 M3;z[2N6fG:2b4jpZ4l1gSCjc4PhfS=> M2HF[lAvOi1{MN88US=> M4DEbFczcA>? NGnTeWxFVVOR MXjJR|UxRTBwOd88US=> M{DBVVI{OjN6NkO5
EHEB NWj4SHllS3m2b4TvfIlkcXS7IHHzd4F6 MV:wMlIuOjEQvF2= M{[zd|czcA>? NX\HN5Q6TE2VTx?= M{PZ[GlEPTB;MD63{txO MV6yN|I{QDZ|OR?=
MEC2 M3j5cGN6fG:2b4jpZ4l1gSCjc4PhfS=> M3rUSFAvOi1{MN88US=> M17UdFczcA>? NUPHNmVUTE2VTx?= MYnJR|UxRTBwN988US=> Mn\jNlMzOzh4M{m=
primary B-CLL lymphocytes M2LjbWFxd3C2b4Ppd{BCe3OjeR?= MYXJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m NHvYW28zPGh? NGLpXHRFVVOR M2\4TGlEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> MUiyN|I{QDZ|OR?=
primary B-CLL lymphocytes MYjLbY5ie2ViQYPzZZk> NVXMWlZjUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= M2Lab|I1cA>? MUHpcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= MXOyN|I{QDZ|OR?=
human NSCLC NH\ZS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSwMlUuOs7:TR?= M1HTO|czcA>? Mnu3TWM2OD1zzszN NEPENGczOjd6MUO5Ny=>
human NSCLC NILPOVlMcW6jc3WgRZN{[Xl? MV[x{txO M3rXNFI1cA>? M1f4[YlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= M2PLSVIzPzhzM{mz
Y1 cell line MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMlHPxE1xMd88US=> NV;Ld5RuOjSq NH\yUYZFVVOR Mn;mbY5pcWKrdIOgOlDwxIViY3XscEB3cWGkaXzpeJkhcW5iTYnjMXNkfHJvdILhcpNn\WO2ZXSgZ4VtdHN? NXvpW|JvOjJ4OUK5NFQ>
PIK3CA-mutant MCF7 NF70d2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\HTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? M2Dt[VczcA>? M3PsNWdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P M2rkPFIzPjV|OU[3
PIK3CA-mutant MCF7 M4DJVWtqdmG|ZTDBd5NigQ>? MmP0TWM2OD1zMUVCtVNvVQ>? MUi3Nog> NV2yW|J2UUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=> M3\me|IzPjV|OU[3
MCF7-myr-Akt MnjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF6ySmJIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= MmTMO|Jp NFznbXBIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= NUG3VHAyOjJ4NUO5Olc>
colon cancer cell lines NEXzeWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\pXXhmOC1zMN88US=> M4T3c|czcA>? MYjEUXNQ NEW4bZlKSzVyPUJOwG0> M2PLW|IzPTR|OEW3
gastric cancer cell lines MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMVEx|ryP NVjxT|BqPzKq MWPEUXNQ NIeycVBKSzVyPUKtOe69VQ>? NVjlRlB4OjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 M2HyUGFxd3C2b4Ppd{BCe3OjeR?= M1;YTFLPxE1? M2raTFQ5cA>? MkGzd4hq\nRiaX6gS|IheGijc3W= M4TGXFIzPTR|OEW3
HT-29 and HCT-116 MWnDZZNx[XOnIHHzd4F6 M{nGc|XPxE1? MV[yOIg> M4Hxbolv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= MUWyNlU1Ozh3Nx?=
MM cell lines MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWGxNO69VQ>? Ml7zNlRp MlvWSG1UVw>? MX3JR|UxKH[jcnnld{BidW:wZzDkbYZn\XKnboSgZ4VtdCCuaX7ld{BqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXuZ4U> NH;nTVAzOjJyN{S4OS=>
ARP-1 NEDxfm9CeG:ydH;zbZMhSXO|YYm= M{\N[VEx|ryP NXfhZYROOjSq NFPS[WRFVVOR NGeyV45qdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG|ZTDhZ5RqfmG2aX;u MV6yNlIxPzR6NR?=
SNU-601 NHfsSHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfOO|Jp M4LRbWROW09? MnKyTWM2OD1yLkixOuKyOC5yNkROwG0> NV3DSJRTOjJzNUm4NVQ>
SNU-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4n2N|czcA>? NYnjbIcxTE2VTx?= M3fBPGlEPTB;MT6wPFLDuTBwMEK4{txO NV\CXJhVOjJzNUm4NVQ>
SNU-668 M4XSb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjiO|Jp NUCxVGVWTE2VTx?= NVvGPINpUUN3ME2xMlU4QcLzMD6wO|TPxE1? NITB[ngzOjF3OUixOC=>
AGS M4TsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPJO|Jp Ml7QSG1UVw>? MVjJR|UxRTFwN{G0xtExNjFzN988US=> M3\0c|IzOTV7OEG0
SNU-216 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe3Nog> NF3DUYZFVVOR MXvJR|UxRTJwNkmyxtExNjB6Mt88US=> M3LEXVIzOTV7OEG0
SNU-5 M{nnTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWi3Nog> MVHEUXNQ MXTJR|UxRTFwM{WxxtExNjB7Md88US=> MknONlIyPTl6MUS=
SNU-638 M{H3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnTb5lYPzKq NYT1PWlYTE2VTx?= M3ezUWlEPTB;Mj6yPFLDuTBwMEWz{txO NYD0e4liOjJzNUm4NVQ>
SNU-16 NIGy[3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ZO|Jp Mn71SG1UVw>? MYHJR|UxRTFwNUezxtExNjByMd88US=> M4HTb|IzOTV7OEG0
SNU-484 NITYZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXpU4FTPzKq NI\aVmhFVVOR M2mzd2lEPTB;MT63NljDuTBwMES1{txO M4TSNFIzOTV7OEG0
SNU-620 NHjUV|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPPO|Jp NUHQeW5wTE2VTx?= MX7JR|UxRTJwOUO5xtExNjByMd88US=> MX6yNlE2QThzNB?=
SNU-719 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO3Nog> NV;EO4U6TE2VTx?= NWWwWI1TUUN3ME2zMlA{P8LzMD6wN|LPxE1? MXqyNlE2QThzNB?=
glioma cell lines MkXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIj1SnU4Omh? Ml3hTWM2OD1zLUNOwG0> NGrHeJIzOjB4NUC4NC=>
U87 MlLiRZBweHSxc3nzJGF{e2G7 NVfEeppXOs7:TR?= NVzYdmFZPzKq NHPGb5VqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHHu[EBkdGWjdnXkJHBCWlBiYX7kJINie3Cjc3WtNy=> NV:yXmVFOjJyNkWwPFA>

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: U87MG and A2780 xenografts are established in female nu/nu mice.
  • Formulation: In 15% Captisol.
  • 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)
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

* 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 N/A

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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 Conditions Sponsor/Collaborators Start Date Phases
NCT01870726 Completed c-MET Inhibitor; PI3K Inhibitor, PTEN Mutations, Homozygous Del. of PTEN or PTEN Neg. by IHC, c-Met Ampli. by FISH, INC280, BKM120, Buparlisib; Recurrent GBM Novartis Pharmaceuticals|Novartis January 9, 2014 Phase 1|Phase 2
NCT01473901 Active, not recruiting Glioblastoma Novartis Pharmaceuticals|Novartis December 30, 2011 Phase 1
NCT01633060 Active, not recruiting Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis October 3, 2012 Phase 3
NCT02756247 Recruiting Lymphoma|Mantle Cell Lymphoma|Follicular Lymphoma|Diffuse Large B Cell Lymphoma Memorial Sloan Kettering Cancer Center|Janssen Scientific Affairs, LLC|Novartis Pharmaceuticals May 2016 Phase 1
NCT02614508 Active, not recruiting 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 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

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID