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
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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.. 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 NXi1[pg3S3m2b4TvfIlkKEG|c3H5 MkLiO|IhcA>? Mme0SG1UVw>? M37CemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2= NX74dpNxOjR7MECyOlY>
DU145 NH30R4REgXSxdH;4bYMhSXO|YYm= M{XjVVczKGh? NWrGdZJ7TE2VTx?= MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1? M{Ppb|I1QTByMk[2
A2780 NFS4UXZEgXSxdH;4bYMhSXO|YYm= NIe2Ono4OiCq NGnEZphFVVOR NYTjXYdQS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=> NFjwNIwzPDlyMEK2Oi=>
U87MG M2TiRmN6fG:2b4jpZ{BCe3OjeR?= MVu3NkBp NYT6XGRTTE2VTx?= NFe5bWpEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN M3PRV|I1QTByMk[2
A2780 M2TaW2Z2dmO2aX;uJGF{e2G7 MYSxJIg> M363TGROW09? NV;jbmNoUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlA2PSEQvF2= NYfF[GpiOjR7MECyOlY>
DU145 NEn3c45HfW6ldHnvckBCe3OjeR?= MXKxJIg> NUn2XVBiTE2VTx?= NF:3dpdKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR|UxKG:oIECuNFc{KM7:TR?= NV;Hb4NqOjR7MECyOlY>
A2780 NHjRToFHfW6ldHnvckBCe3OjeR?= NGTyRWwyKGh? MYHEUXNQ M3vT[2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP NIXKVVUzPDlyMEK2Oi=>
MCF7 NFrqcXhHfW6ldHnvckBCe3OjeR?= MXuxJIg> MknFSG1UVw>? Mor1TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO NEfZ[YMzPDlyMEK2Oi=>
U87MG NHnQV4pHfW6ldHnvckBCe3OjeR?= NYnXZ|B{OSCq NGjaTXVFVVOR NGf2PJVKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP NXizVlk5OjR7MECyOlY>
A2780 NWP6TYoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGf4[VU4OiCq MUXEUXNQ MYXFR|UxRTBwNUKg{txO NGrNXnYzPDlyMEK2Oi=>
SKMES-1 NITzWVZEgXSxdH;4bYMhSXO|YYm= MYKxJO69VQ>? MmG5O|IhcA>? M{jJemlv\HWlZYOgZ4VtdCCmZXH0bC=> NFn0dlEzPjBzM{OxPC=>
H596 NX\CUZNPTnWwY4Tpc44hSXO|YYm= NHXpOmgyKM7:TR?= MYjJcZBicXK|IHPlcIwhdWmpcnH0bY9v MnTwNlYxOTN|MUi=
HCC2450 Mly3SpVv[3Srb36gRZN{[Xl? MX:xJO69VQ>? M3X5[WlueGGrcoOgZ4VtdCCrbo\hd4lwdg>? MVeyOlAyOzNzOB?=
A549 M1XCN2Z2dmO2aX;uJGF{e2G7 MlfUOVAxKG6P NE\jO5A1QCCq NG\MOHpFVVOR NHSzR3dKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= NWPmOYlNOjV7M{eyPVk>
A549 MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfZXXgyKM7:TR?= MkOwO|IhcA>? NIrNZnlFVVOR MkL0TY5pcWKrdIOgZ4VtdCCpcn;3eIg> MoHsNlU6Ozd{OUm=
H522 NW\BN25YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvGNUDPxE1? MVO3NkBp Ml3TSG1UVw>? NFPucodKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NF7Qe|czPTl|N{K5PS=>
LNCaP NHnZV29HfW6ldHnvckBCe3OjeR?= MV[xJO69VQ>? NXvoVpdpW3WycILld5NmeyCyLVHLWEBt\X[nbIO= NFnxTIozPTN4MEe5PS=>
LNCaP95 MUXGeY5kfGmxbjDBd5NigQ>? NHjiRmIyKM7:TR?= MVnTeZBxemW|c3XzJJAuSUuWIHzleoVtew>? NVix[HBbOjV|NkC3PVk>
HCT-15 MYHBdI91d3OrczDBd5NigQ>? NHrkcWYyOCEQvF2= MkSxOFghcA>? NXm5[IttTE2VTx?= NV7MXI9uUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NVH6NFlqOjVzNUKyOFU>
HCT-116 MofDRZBwfG:|aYOgRZN{[Xl? M2H2UVExKM7:TR?= NH:xbng1QCCq MUTEUXNQ M2jHUWlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M4fmS|I2OTV{MkS1
NCI-H460 NVeyW4p[SXCxdH;zbZMhSXO|YYm= M1PjV|ExKM7:TR?= MmSxOFghcA>? MVzEUXNQ M{[1S2lv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= Mmn2NlUyPTJ{NEW=
SKOV-3 NUe1TVJtSXCxdH;zbZMhSXO|YYm= MV2xNEDPxE1? Mnm0OFghcA>? MYXEUXNQ NWHkPIxHUW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MlLRNlUyPTJ{NEW=
BSY-1 NXra[VBlSXCxdH;zbZMhSXO|YYm= MnP0NVAh|ryP MYK0PEBp NH;xSZRFVVOR Mln0TY5lfWOnczDhdI9xfG:|aYOgbY4hSlO\LUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MX:yOVE2OjJ2NR?=
MKN-1 NIjwb4dCeG:2b4Ppd{BCe3OjeR?= M4TMWVExKM7:TR?= MmDaOFghcA>? NVrZSm1{TE2VTx?= NHXyVXVKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCPS16tNUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MYWyOVE2OjJ2NR?=
NCI-H522 NFjhdJdCeG:2b4Ppd{BCe3OjeR?= NVP3[FBEOTBizszN MYG0PEBp NHfMRVBFVVOR MVXJcoR2[2W|IHHwc5B1d3Orcx?= NVrYTFhiOjVzNUKyOFU>
OVCAR-3 NVzDW|h2SXCxdH;zbZMhSXO|YYm= NEfYZmMyOCEQvF2= NHXMT4g1QCCq NUXsNllmTE2VTx?= NFjmOoZKdmS3Y3XzJIFxd3C2b4Ppdy=> MVWyOVE2OjJ2NR?=
HBC-5 MUjBdI91d3OrczDBd5NigQ>? MYSxNEDPxE1? Ml;iOFghcA>? NVXsemRqTE2VTx?= NG\n[YxKdmS3Y3XzJIFxd3C2b4Ppdy=> MnntNlUyPTJ{NEW=
RXF-631L M4HZTWFxd3Sxc3nzJGF{e2G7 M4DTelExKM7:TR?= NEfQN3E1QCCq MXzEUXNQ MkDhTY5lfWOnczDhdI9xfG:|aYO= NHHjdIQzPTF3MkK0OS=>
MKN-45 MUjBdI91d3OrczDBd5NigQ>? M4e5TFExKM7:TR?= NYXNZnl2PDhiaB?= NEXqSllFVVOR M1LxZWlv\HWlZYOgZZBweHSxc3nz MVSyOVE2OjJ2NR?=
BON-1 MlLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3Tb|Y2ODBibl2= M{DjflExKGR? MoLtSG1UVw>? MUXJcohq[mm2czDj[YxtKGe{b4f0bC=> MUSyOVAzPjJ7Mh?=
BON-1 M4rUR2Z2dmO2aX;uJGF{e2G7 NFjEOXM2ODBibl2= NH7OfJI1KGh? NHHNPGRFVVOR NHewWWlKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHRpejNyODDhcoQhW2W{NEez M1O3WVI2ODJ4Mkmy
QGP-1 M1e0OmZ2dmO2aX;uJGF{e2G7 NIDuXZI2ODBibl2= MUW0JIg> MXLEUXNQ NV7ERVltUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> NGrhfXYzPTB{NkK5Ni=>
Huh7 MVzGeY5kfGmxbjDBd5NigQ>? NWXydJhtOSEQvF2= M{XueVEhcA>? NVHqPHRiTE2VTx?= NVfCbXJJUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S= MYmyOVAxPDRyMx?=
BNL NYOyUlR5TnWwY4Tpc44hSXO|YYm= MnfENUDPxE1? MV[xJIg> NFPHV5pFVVOR Mn7tTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3 M33XXlI2ODB2NECz
MDA-MB-175 NWrCNWZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\kdIxQOSEQvF2= MkjnOUBl MYrEUXNQ M4LLSmlEPTB:MTFOwG0> NX3RVodIOjR6N{m3PVY>
MDA-MB-134 NXf0NGQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXqxJO69VQ>? NIfQN2w2KGR? M2[xN2ROW09? M2O1eGlEPTB:MTFOwG0> M2q0UFI1QDd7N{m2
HCC1500 NEjCVG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjBO2lNOSEQvF2= M1WyO|Uh\A>? Mn60SG1UVw>? NHXKenFKSzVyPEGg{txO Mnv4NlQ5Pzl5OU[=
EFM-19 NXXlVVN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnrNUDPxE1? NHTvV2o2KGR? MmLMSG1UVw>? MYDJR|UxRDFizszN NUDE[Jp6OjR6N{m3PVY>
ZR-75-30 M2PQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFznXlkyKM7:TR?= MmjGOUBl NWnXR4hPTE2VTx?= M{SxdGlEPTB:MTFOwG0> MnWwNlQ5Pzl5OU[=
MDA-MB-361 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSxJO69VQ>? MlK2OUBl MnP5SG1UVw>? NGPPbXBKSzVyPEGg{txO M3X2Z|I1QDd7N{m2
T-47D MnPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnrNUDPxE1? MWS1JIQ> MnjQSG1UVw>? NX7ESodOUUN3MEyxJO69VQ>? M3HIWVI1QDd7N{m2
SK-BR-3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLjb5EyKM7:TR?= Mo\sOUBl NVLtcW5NTE2VTx?= NX[4eVVWUUN3MEyxJO69VQ>? MortNlQ5Pzl5OU[=
UACC-732 MkTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxJO69VQ>? MWG1JIQ> MYnEUXNQ MkPkTWM2ODxzIN88US=> M3\qZlI1QDd7N{m2
BT-474 NWXscJl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPHNUDPxE1? M1\ZdVUh\A>? M4jJTGROW09? M3jBbGlEPTB:MTFOwG0> MlHrNlQ5Pzl5OU[=
HCC202 M{nlemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHGO2l{OSEQvF2= M4THOlUh\A>? NFH2dGlFVVOR MYXJR|UxRDFizszN NF3lZpAzPDh5OUe5Oi=>
MCF7 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWqxJO69VQ>? MoD0OUBl MWnEUXNQ MWPJR|UxRDFizszN NV\i[mlsOjR6N{m3PVY>
MDA-MB-415 NWL4bmVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVSwS5dZOSEQvF2= MoCxOUBl NEnmenJFVVOR MlHWTWM2ODxzIN88US=> NGO4PGgzPDh5OUe5Oi=>
MDA-MB-453 M{jxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWxJO69VQ>? NH:xUm02KGR? MXTEUXNQ NYrVb|NGUUN3MEyxJO69VQ>? NFfWOXAzPDh5OUe5Oi=>
ZR-75-1 NIXsbnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\mVGdUOSEQvF2= MWC1JIQ> NXnXc|NFTE2VTx?= Moj1TWM2ODxzIN88US=> NHLEbpUzPDh5OUe5Oi=>
HCC38 NITDTpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHznb4wyKM7:TR?= MnXFOUBl MYDEUXNQ M4jkS2lEPTB:MTFOwG0> M1HiSlI1QDd7N{m2
HCC1419 M2\GSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSxJO69VQ>? Mom5OUBl MWnEUXNQ NE\yZoxKSzVyPEGg{txO NF\VR5IzPDh5OUe5Oi=>
UACC-812 NHPsXIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGxJO69VQ>? NEHpUYw2KGR? NVjicWRJTE2VTx?= MYHJR|UxRDFizszN NVjLWmlXOjR6N{m3PVY>
HCC1187 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOxJO69VQ>? MVS1JIQ> NYPwfHB2TE2VTx?= NIPmUYtKSzVyPEGg{txO M2f1PFI1QDd7N{m2
KPL-1 MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnpTpYyKM7:TR?= M1H1NVUh\A>? MUXEUXNQ MYrJR|UxRDFizszN MoCyNlQ5Pzl5OU[=
SUM-225 M1jFZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XJdFEh|ryP MYi1JIQ> MmTVSG1UVw>? NGSzO4FKSzVyPEGg{txO NUjPeW5NOjR6N{m3PVY>
EFM-192A M4fEVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxJO69VQ>? NVnEWXgzPSCm NXrrXJhITE2VTx?= NVvlcpFXUUN3MEyxJO69VQ>? M3HkZlI1QDd7N{m2
JIMT-1 M1LuUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy5dIcyKM7:TR?= NU\qc|dpPSCm MX\EUXNQ NWjne2kyUUN3MEyxJO69VQ>? M33S[lI1QDd7N{m2
HCC1143 MkLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrQNUDPxE1? MnrjOUBl M3XKRWROW09? MVjJR|UxRDFizszN NFOxPIozPDh5OUe5Oi=>
HCC2218 NWLuZlc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[xJO69VQ>? Mm\VOUBl MXTEUXNQ NYfVfpJkUUN3MEyxJO69VQ>? Mne5NlQ5Pzl5OU[=
MDA-MB-468 MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGi2cmUyKM7:TR?= MmLLOUBl NXnUSHZuTE2VTx?= NFztfYlKSzVyPEGg{txO NEHHeZczPDh5OUe5Oi=>
BT-20 MmDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M32xNVEh|ryP M2\kbFUh\A>? NWjU[YdzTE2VTx?= MUXJR|UxRDFizszN NVf3d2tFOjR6N{m3PVY>
MDA-MB-435 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fsbFEh|ryP MUC1JIQ> NWfTO2tKTE2VTx?= NHftfmtKSzVyPEGg{txO NUHoc4NKOjR6N{m3PVY>
BT-549 NFjJU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULDNJpQOSEQvF2= NX:2[2JJPSCm NF;FPYxFVVOR NGPUeFZKSzVyPEGg{txO NVzvNWhKOjR6N{m3PVY>
HCC1806 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnHOI5MOSEQvF2= NULYdJUyPSCm M3\mXGROW09? Ml;WTWM2ODxzIN88US=> MlzlNlQ5Pzl5OU[=
HCC1937 NVrhWIFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFntc48yKM7:TR?= M4HOVFUh\A>? M{\RN2ROW09? NHny[ldKSzVyPEGg{txO M1:0eFI1QDd7N{m2
Hs578T MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TXPFEh|ryP MWC1JIQ> NWDSZ|hpTE2VTx?= M1X5[GlEPTB:MTFOwG0> MmnyNlQ5Pzl5OU[=
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MG-63 M165[mZ2dmO2aX;uJGF{e2G7 M17KblUxKM7:TR?= NWmzbVU3PDhiaB?= MUnJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NVXzZWxEOjR5Mke2OlA>
SJSA-1 NV\jd45{TnWwY4Tpc44hSXO|YYm= MYq1NEDPxE1? NFjrRmE1QCCq M3ftZ2lvcGmkaYTzJI1ifHKreDDt[ZRidGyxcILveIVqdmG|ZT2yJIV5eHKnc4Ppc44> Mo[zNlQ4Ojd4NkC=
Saos-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHO4cYY2OCEQvF2= MlTROFghcA>? MXPJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? NFfidGozPDd{N{[2NC=>
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SJSA-1 M4f6V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnmcIp6PTBizszN NIPPdGo1QCCq MXjJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? NWLOd|BlOjR5Mke2OlA>
FaDu NEH6UWZHfW6ldHnvckBCe3OjeR?= NEL1PYg2KM7:TR?= M{nXdVI1KGh? NHzjWpZFVVOR M2f4e3Jm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u MX2yOFY{OTF2Nx?=
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HCT116 MYjGeY5kfGmxbjDBd5NigQ>? MnvGOUDPxE1? NWHaOZNIOjRiaB?= MWnEUXNQ NFn2U4dT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NFfDSFUzPDZ|MUG0Oy=>
U87 NVW0OG5uTnWwY4Tpc44hSXO|YYm= M4rp[FUh|ryP NFjweGIzPCCq MYPEUXNQ MkTCVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= M4\UO|I1PjNzMUS3
GBM NYi2Z|NuSXCxcITvd4l{KEG|c3H5 M4TCNlLPxE1? M2O3[FQ5cA>? NGrQcmtFVVOR MWnpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 NVzEOWhMOjR3MEC0PVI>
BON NYjubZA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nF[FEuPc7:TR?= MYm3Nog> MmTz[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NHG1ZpIzPDR2M{WyNy=>
BON NEizRYhCeG:ydH;zbZMhSXO|YYm= NEfoXpUyNTYQvF2= M4DLVVI1cA>? NX;5RXRVcW6lcnXhd4V{KGGyb4D0c5Nqew>? MUmyOFQ1OzV{Mx?=
H1975 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HOTlAvOy17LkdOwG0> M3m0eFczcA>? NUHI[HBGTE2VTx?= M{jzW2lEPTB;MT6zPFXPxE1? MV[yOFM{Pzh2Nh?=
H1975 MVzBdI9xfG:|aYOgRZN{[Xl? NEjNR4Qz|ryP M13pW|I1cA>? NXnoTGZLTE2VTx?= NYKzfXJucW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl? NXXrRpl1OjR|M{e4OFY>
T-ALL NIT4UGVCeG:ydH;zbZMhSXO|YYm= NF\vUGZj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW= NXjkS4pvOjRib4KgOFhp M3jCXmROW09? MX7h[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= NYjTdoZTOjR|MUC3N|Y>
BCR-ABL MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fXTlAvOjVvMUFOwG0> NEDpNIU1\A>? NVTNNHZEe2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= NEnCOWszPDJ2NE[xNi=>
LC-1/SQSF MVXGeY5kfGmxbjDBd5NigQ>? MlX6N:69VQ>? NHjs[pIzPGh? MmPoSG1UVw>? NWfHXG9S\GWlcnXhd4UhVlKIMjDwdo91\WmwIHzleoVt MYSyN|k5ODB7Mx?=
Primary CLL cells M3;4PWFxd3C2b4Ppd{BCe3OjeR?= MYOxMVEx|ryP MUi0PIg> MXjpcoR2[2W|IHHwc5B1d3OrczDpckBEVExiY3XscJMhcW6mZYDlcoRmdnRib3[gdJJw\26xc4TpZ{Bu[XKtZYLz MUeyN|g2ODhyNx?=
Primary CLL cells Mln4T4lv[XOnIFHzd4F6 Mo[5Nu69VQ>? MmLSN|BucW5? MVrk[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>? MnLWNlM5PTB6MEe=
Primary CLL cells MXnDfZRwfG:6aXOgRZN{[Xl? NVy4N4Q2Os7:TR?= MYeyOIg> M1PkVolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MViyN|g2ODhyNx?=
human NSCLC cell lines NXe3c|ZtSXCxcITvd4l{KEG|c3H5 MnTYNE4yOjVvNN88US=> NG\4fo8zPGh? Ml;wSG1UVw>? M{XXc2lEPTC|IILhcodmeyCocn;tJFAvPC1{zszN NWjH[mpjOjN3NkK0O|I>
human HCC cell lines MUDD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M{SxO|AvODB3LUJOwG0> NF\qXog1QGh? NVr2O2tUUUN3ME2x{txO NFLEfHEzOzR6OUm5PS=>
Huh7 MV7LbY5ie2ViQYPzZZk> MnHvNe69VQ>? M2K5flQ5cA>? NFuxcGp{cWewaf-shYNidnSueTDy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MmXINlM1QDl7OUm=
SK-HEP1 MmLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLucnoyNTJyzszN NHu1XJQ4Omh? NHXlWZFFVVOR NWLsOG9[UUN3MP-8oFHPxE1? M1XwbFI{PDd7MUO2
786-0 NYjG[IZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n6OVEuOjEQvF2= M2P2blczcA>? MlnwSG1UVw>? NXLp[mdyUUN3MP-8oFHPxE1? MlTMNlM1PzlzM{[=
JVM2 NEfpT5ZEgXSxdH;4bYNqfHliYYPzZZk> NFXlO5oxNjJvMkFOwG0> M1;xOlczcA>? MmmwSG1UVw>? MkK5TWM2OD1yLkpOwG0> Mmj0NlMzOzh4M{m=
EHEB NYTJRXl6S3m2b4TvfIlkcXS7IHHzd4F6 MmHLNE4zNTJyzszN NUS4VFQ3PzKq MXHEUXNQ NGixWFhKSzVyPUCuO:69VQ>? MnHQNlMzOzh4M{m=
MEC2 NG\iRlhEgXSxdH;4bYNqfHliYYPzZZk> NGnrcVMxNjJvMkFOwG0> M1nSTFczcA>? NHPwO2lFVVOR M4nrOmlEPTB;MD63{txO NFjnRoIzOzJ|OE[zPS=>
primary B-CLL lymphocytes MWHBdI9xfG:|aYOgRZN{[Xl? MVHJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m Moe1NlRp MmH1SG1UVw>? MYDJR|Ux97zeM988UUBnd3JiYXzsJJBifGmnboTz MoPHNlMzOzh4M{m=
primary B-CLL lymphocytes MU\LbY5ie2ViQYPzZZk> MVvJR|UxKG[xcjDlZYNpKHC{aX3hdpkh[2WubDDsbY5m M4XqbVI1cA>? NIjuRVRqdmirYnn0d{BxPzCVNlugKkA1TS2EUEGg[ZhxemW|c3nvci=> MWGyN|I{QDZ|OR?=
human NSCLC MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXm5b|doOC53LUNOwG0> MVy3Nog> M1[2VGlEPTB;Md88US=> NX\rOZhiOjJ5OEGzPVM>
human NSCLC NWrReWlEU2mwYYPlJGF{e2G7 MljoNe69VQ>? NIfy[mozPGh? NFHjcGJqdmirYnn0d{B1cGViQXv0M41VV1Jic3nncoFtcW6pIIDheIh4[XliYYSgN4gh[W[2ZYKgeJJm[XSvZX70 Mon4NlI4QDF|OUO=
Y1 cell line MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PiVVAvOc7:TT:x{txO M37rfFI1cA>? NG\sWmVFVVOR MVPpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>? MnTyNlI3QTJ7MES=
PIK3CA-mutant MCF7 NGXh[21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLHTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? NYrhdI1ZPzKq MX7HTVUxRTF4MNMxPVFvVe,:jFzEOVA:QThywsGyO|NvVQ>? NWHJO2c{OjJ4NUO5Olc>
PIK3CA-mutant MCF7 NFvWdmdMcW6jc3WgRZN{[Xl? Mli1TWM2OD1zMUVCtVNvVQ>? M2fFU|czcA>? Mn3PTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= M1r0WFIzPjV|OU[3
MCF7-myr-Akt MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? NWP3SJd3PzKq MojFS2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? NXGyZnloOjJ4NUO5Olc>
colon cancer cell lines M1PG[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrONE0yOM7:TR?= MWW3Nog> M13RXGROW09? MmK5TWM2OD1zzszN M37qRlIzPTR|OEW3
gastric cancer cell lines MmeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke3NE0yOM7:TR?= M3fhXFczcA>? MWfEUXNQ NYXN[lhEUUN3ME2yMVXPxE1? MlvJNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 M122SWFxd3C2b4Ppd{BCe3OjeR?= MWey{txO Ml;HOFhp NHe1b3J{cGmodDDpckBIOiCyaHHz[S=> MkXuNlI2PDN6NUe=
HT-29 and HCT-116 Mn3uR4F{eGG|ZTDhd5NigQ>? NEXUOJQ2|ryP MWiyOIg> NVXXRnp6cW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5 M3W3eFIzPTR|OEW3
MM cell lines NEjWcZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIn2e|gyOM7:TR?= NUjOTYVyOjSq NFjoPFRFVVOR NFS3T4NKSzVyII\hdolmeyCjbX;u[{BlcW[oZYLlcpQh[2WubDDsbY5meyCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVv[2V? NGnCS4czOjJyN{S4OS=>
ARP-1 NFjYbJZCeG:ydH;zbZMhSXO|YYm= NH7ue2cyOM7:TR?= MUOyOIg> NVXT[FBxTE2VTx?= NUi5PGhDcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> NVLBWYhzOjJ{MEe0PFU>
SNU-601 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO3Nog> M4\QPGROW09? NUS5WFlsUUN3ME2wMlgyPsLzMD6wOlPPxE1? NFXzPIYzOjF3OUixOC=>
SNU-1 Mn3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlraO|Jp MYrEUXNQ MV;JR|UxRTFwMEiyxtExNjB{ON88US=> MnrWNlIyPTl6MUS=
SNU-668 NILhN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULtPFVPPzKq MnK0SG1UVw>? M2XkSWlEPTB;MT61O|nDuTBwMEe0{txO MkHkNlIyPTl6MUS=
AGS NX36RY1xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK3Nog> MWLEUXNQ MUTJR|UxRTFwN{G0xtExNjFzN988US=> NGHtWoozOjF3OUixOC=>
SNU-216 MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUW3Nog> NVz6TmdGTE2VTx?= M{XhWWlEPTB;Mj62PVLDuTBwMEiy{txO NITwb4czOjF3OUixOC=>
SNU-5 NX\5NXBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LQblczcA>? MVrEUXNQ NX\iellKUUN3ME2xMlM2OcLzMD6wPVHPxE1? NGjZUoUzOjF3OUixOC=>
SNU-638 Mmj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfHO2FOPzKq NYezZ2k6TE2VTx?= MVvJR|UxRTJwMkiyxtExNjB3M988US=> M3fYVVIzOTV7OEG0
SNU-16 MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfQO|Jp NIj3e45FVVOR M13mWGlEPTB;MT61O|PDuTBwMECx{txO NXPX[oRKOjJzNUm4NVQ>
SNU-484 MlizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF73NYk4Omh? MYrEUXNQ MX\JR|UxRTFwN{K4xtExNjB2Nd88US=> NYHhcmNmOjJzNUm4NVQ>
SNU-620 M3fzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXS3Nog> M1fJZ2ROW09? NEnPSmZKSzVyPUKuPVM6yrFyLkCwNe69VQ>? MVuyNlE2QThzNB?=
SNU-719 MnrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX23Nog> MU\EUXNQ M3LYdmlEPTB;Mz6wN|fDuTBwMEOy{txO NV7Q[mFJOjJzNUm4NVQ>
glioma cell lines NW\QdGVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vvclczcA>? MlPVTWM2OD1zLUNOwG0> M4jhWlIzODZ3MEiw
U87 NGOxNoxCeG:ydH;zbZMhSXO|YYm= NXXseW4zOs7:TR?= MlXTO|Jp NYTwdW9icW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> MmnKNlIxPjVyOEC=

... 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:
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
Synonyms N/A

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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