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 37 Publications

5 Customer Reviews

  • 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 NILreW9EgXSxdH;4bYMhSXO|YYm= NIXuVXU4OiCq NITmUYlFVVOR Ml\OR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BmgHC{ZYPzbY5oKFCLM1vhcJBp[SCHNUS1T{BufXSjboSge4l1cCCJSUWwJI9nKDBwMECwNVU5KM7:TR?= M17HflI1QTByMk[2
DU145 MnTWR5l1d3SxeHnjJGF{e2G7 NXvuXnF{PzJiaB?= NEDyfHBFVVOR NIPZSm9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCneIDy[ZN{cW6pIFzLRlEhdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFQ{PSEQvF2= M1rYblI1QTByMk[2
A2780 MU\DfZRwfG:6aXOgRZN{[Xl? NV3OR|JKPzJiaB?= MlHQSG1UVw>? NXvIN5FpS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=> NGLOdoUzPDlyMEK2Oi=>
U87MG M37ZdWN6fG:2b4jpZ{BCe3OjeR?= NV3ESXNWPzJiaB?= M1rYdGROW09? NELxdFJEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDVPFdOTyClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3QThizszN M4nue|I1QTByMk[2
A2780 Ml;NSpVv[3Srb36gRZN{[Xl? NEGwSnAyKGh? NEDZVHZFVVOR MXfJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? NGDid|MzPDlyMEK2Oi=>
DU145 MYjGeY5kfGmxbjDBd5NigQ>? MXyxJIg> M3HqVmROW09? MUjJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gSHUyPDViY3XscJMhcGG{Yn;ybY5oKEyNQkGgcZV1[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEezJO69VQ>? NVi3[pJJOjR7MECyOlY>
A2780 MonqSpVv[3Srb36gRZN{[Xl? MYKxJIg> M37kSmROW09? M1nzbWlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP NUnOfI5lOjR7MECyOlY>
MCF7 Mny1SpVv[3Srb36gRZN{[Xl? NXXsSXcxOSCq MYXEUXNQ NHXJOnRKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hf2m2aDDFR|UxKG:oIECuNUDPxE1? NFLDXI8zPDlyMEK2Oi=>
U87MG MVvGeY5kfGmxbjDBd5NigQ>? NVXuWnhLOSCq NGraO2tFVVOR MYXJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO NYPscohnOjR7MECyOlY>
A2780 MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm2S2o4OiCq MkX2SG1UVw>? NGHHd|lGSzVyPUCuOVIh|ryP MVKyOFkxODJ4Nh?=
SKMES-1 NHfZeVBEgXSxdH;4bYMhSXO|YYm= M1L4eVEh|ryP NWPIS|RJPzJiaB?= NF;qS3BKdmS3Y3XzJINmdGxiZHXheIg> MlzKNlYxOTN|MUi=
H596 M1n0VWZ2dmO2aX;uJGF{e2G7 M3[zUVEh|ryP MUHJcZBicXK|IHPlcIwhdWmpcnH0bY9v M4K2N|I3ODF|M{G4
HCC2450 M2fPPWZ2dmO2aX;uJGF{e2G7 NW\4[FFUOSEQvF2= MVzJcZBicXK|IHPlcIwhcW64YYPpc44> Ml;rNlYxOTN|MUi=
A549 MkG4SpVv[3Srb36gRZN{[Xl? M3fVVlUxOCCwTR?= MnPSOFghcA>? NETyT3dFVVOR M3TEPGlvcGmkaYTzJGFsfCCjY4TpeoF1cW:w NFmye2IzPTl|N{K5PS=>
A549 M324emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\PNUDPxE1? NWL0UIg4PzJiaB?= NHn1eINFVVOR MkfxTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MYWyOVk{PzJ7OR?=
H522 NYnCRmRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37lTFEh|ryP NXPSb5BtPzJiaB?= MkDoSG1UVw>? MmrzTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX:yOVk{PzJ7OR?=
LNCaP NF;KRXpHfW6ldHnvckBCe3OjeR?= M2q3flEh|ryP M3HhZXN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| MnzENlU{PjB5OUm=
LNCaP95 MY\GeY5kfGmxbjDBd5NigQ>? M1nP[VEh|ryP NUDodGQ5W3WycILld5NmeyCyLVHLWEBt\X[nbIO= MYWyOVM3ODd7OR?=
HCT-15 MmnrRZBwfG:|aYOgRZN{[Xl? MoLINVAh|ryP NHXIW3o1QCCq MWLEUXNQ NWm1cpFuUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVE2KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MWqyOVE2OjJ2NR?=
HCT-116 M4P0d2Fxd3Sxc3nzJGF{e2G7 M4foO|ExKM7:TR?= M2HnWFQ5KGh? M1HlPWROW09? MUHJcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUG2JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M3[2XlI2OTV{MkS1
NCI-H460 NHiwTXRCeG:2b4Ppd{BCe3OjeR?= Ml\qNVAh|ryP NE\Jb4Y1QCCq MoXtSG1UVw>? M1vMT2lv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NHnab3MzPTF3MkK0OS=>
SKOV-3 NGXWWY5CeG:2b4Ppd{BCe3OjeR?= NVrHNXRNOTBizszN NF72SIw1QCCq MUPEUXNQ NVuz[pY6UW6mdXPld{BieG:ydH;zbZMhcW5iU1vPWk0{KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= MorSNlUyPTJ{NEW=
BSY-1 NVz6TpBjSXCxdH;zbZMhSXO|YYm= MYKxNEDPxE1? M2W1T|Q5KGh? MVjEUXNQ NVKwTopNUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NF2xd4ozPTF3MkK0OS=>
MKN-1 NXfxfJRzSXCxdH;zbZMhSXO|YYm= MoXtNVAh|ryP MYG0PEBp MYXEUXNQ MmDuTY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? M{XSUlI2OTV{MkS1
NCI-H522 MlvQRZBwfG:|aYOgRZN{[Xl? NVfJPXBCOTBizszN NIXIR5U1QCCq MV7EUXNQ MUHJcoR2[2W|IHHwc5B1d3Orcx?= Mm\sNlUyPTJ{NEW=
OVCAR-3 NUnmV3VvSXCxdH;zbZMhSXO|YYm= NXm3dowyOTBizszN Mli1OFghcA>? MWXEUXNQ NY\OcHlrUW6mdXPld{BieG:ydH;zbZM> MXmyOVE2OjJ2NR?=
HBC-5 MWDBdI91d3OrczDBd5NigQ>? NXzDUnVYOTBizszN NUnuNmRxPDhiaB?= NEPy[VZFVVOR NFvTcVFKdmS3Y3XzJIFxd3C2b4Ppdy=> MWOyOVE2OjJ2NR?=
RXF-631L M4K2d2Fxd3Sxc3nzJGF{e2G7 MYqxNEDPxE1? MlLKOFghcA>? M13S[2ROW09? NFXRPWpKdmS3Y3XzJIFxd3C2b4Ppdy=> NELi[|QzPTF3MkK0OS=>
MKN-45 M1rvcmFxd3Sxc3nzJGF{e2G7 NYfB[plYOTBizszN NGL4[5Q1QCCq NHmydnBFVVOR NXniUWpYUW6mdXPld{BieG:ydH;zbZM> MoXjNlUyPTJ{NEW=
BON-1 NYHGd2N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjsPGM2ODBibl2= NGnrSJQyOCCm NH;C[mFFVVOR MkfDTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MorKNlUxOjZ{OUK=
BON-1 MXTGeY5kfGmxbjDBd5NigQ>? NFnB[nc2ODBibl2= NFXZNoI1KGh? MlvuSG1UVw>? NUK4VlVmUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> M3jFe|I2ODJ4Mkmy
QGP-1 NXr6VJUzTnWwY4Tpc44hSXO|YYm= NIPi[Xk2ODBibl2= MV60JIg> NVrJdFVLTE2VTx?= MYHJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| NXnVeJV4OjVyMk[yPVI>
Huh7 NH3rOJBHfW6ldHnvckBCe3OjeR?= M1S3XFEh|ryP NGm5fYQyKGh? Mn;6SG1UVw>? M{fqSmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgV4VzPDd2 M2\2SVI2ODB2NECz
BNL NVfuNpJlTnWwY4Tpc44hSXO|YYm= M2\HfVEh|ryP NX7KTId7OSCq M1f2OGROW09? NIi5OYJKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? MmrnNlUxODR2MEO=
MDA-MB-175 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX6xJO69VQ>? M4fVfVUh\A>? NIX5OmpFVVOR NXnqUYtsUUN3MEyxJO69VQ>? NHHLTHozPDh5OUe5Oi=>
MDA-MB-134 NYrsZ4oxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTQNUDPxE1? M3X6c|Uh\A>? NFT3b2tFVVOR MX7JR|UxRDFizszN NGj3O5czPDh5OUe5Oi=>
HCC1500 M2PmOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxJO69VQ>? NVexblJjPSCm M4rTc2ROW09? NYmy[nlbUUN3MEyxJO69VQ>? NWjWco5yOjR6N{m3PVY>
EFM-19 Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGniXZYyKM7:TR?= M2TqblUh\A>? NHrxfm1FVVOR MXHJR|UxRDFizszN Mk[zNlQ5Pzl5OU[=
ZR-75-30 M3S1bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkX5NUDPxE1? MkTmOUBl MnPHSG1UVw>? NEDrZXNKSzVyPEGg{txO MX2yOFg4QTd7Nh?=
MDA-MB-361 M4DjWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[0W2EyKM7:TR?= MoTyOUBl MUPEUXNQ MlniTWM2ODxzIN88US=> MoPTNlQ5Pzl5OU[=
T-47D NW\ibVJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHDUGcyKM7:TR?= NYTaOFZjPSCm NFK3dnZFVVOR NWrENYlJUUN3MEyxJO69VQ>? MWCyOFg4QTd7Nh?=
SK-BR-3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zNZ|Eh|ryP MVO1JIQ> M1:zfmROW09? NV\jVmJjUUN3MEyxJO69VQ>? NXzHXXg2OjR6N{m3PVY>
UACC-732 NUXiWXJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\6UXlSOSEQvF2= MUW1JIQ> NHHhbmdFVVOR NVLlcVFrUUN3MEyxJO69VQ>? MXSyOFg4QTd7Nh?=
BT-474 M3XVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\WRZJtOSEQvF2= M1zQWVUh\A>? NH70UHVFVVOR MXvJR|UxRDFizszN NHPlOXMzPDh5OUe5Oi=>
HCC202 NHvpNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fVT|Eh|ryP NH\aVXI2KGR? MmnUSG1UVw>? M4WwXWlEPTB:MTFOwG0> MUCyOFg4QTd7Nh?=
MCF7 NYrtR2tmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOxJO69VQ>? MXm1JIQ> NXrzPYQ4TE2VTx?= M{i4XGlEPTB:MTFOwG0> NF;pem4zPDh5OUe5Oi=>
MDA-MB-415 NVPqbXBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnjNUDPxE1? NHL5dIw2KGR? M4PMUWROW09? M3zZb2lEPTB:MTFOwG0> NIXON4kzPDh5OUe5Oi=>
MDA-MB-453 Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUCzZoNROSEQvF2= NWTTWoFrPSCm NWKzS|lHTE2VTx?= NXvlTpRFUUN3MEyxJO69VQ>? NHjYb2UzPDh5OUe5Oi=>
ZR-75-1 NIfu[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3O5VlEh|ryP MnfhOUBl MoHCSG1UVw>? M3nYUmlEPTB:MTFOwG0> MU[yOFg4QTd7Nh?=
HCC38 M{n1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzEbWQyKM7:TR?= MVi1JIQ> MWHEUXNQ M3njdWlEPTB:MTFOwG0> NELwSGEzPDh5OUe5Oi=>
HCC1419 NV3lb5oyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;v[HUyKM7:TR?= NHL0fnk2KGR? NXvoZ45TTE2VTx?= NWi2W4JPUUN3MEyxJO69VQ>? NEnlXWozPDh5OUe5Oi=>
UACC-812 NX\xeIl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2xJO69VQ>? NXnsbWlmPSCm MorXSG1UVw>? NEPzSoRKSzVyPEGg{txO MX2yOFg4QTd7Nh?=
HCC1187 NEG5NXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCxJO69VQ>? M1jCdFUh\A>? MmLOSG1UVw>? NX[4TZFsUUN3MEyxJO69VQ>? M4jtWVI1QDd7N{m2
KPL-1 NIDvZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzldW0yKM7:TR?= NFTKW3A2KGR? M2Tnc2ROW09? Mle5TWM2ODxzIN88US=> MoHKNlQ5Pzl5OU[=
SUM-225 NF;qSnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYK1TnNwOSEQvF2= MmHwOUBl NEHJOYRFVVOR NY\2N2FuUUN3MEyxJO69VQ>? NIfaOZUzPDh5OUe5Oi=>
EFM-192A MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:2NUDPxE1? MUG1JIQ> NXy3ZXFpTE2VTx?= MnPjTWM2ODxzIN88US=> NIfM[GIzPDh5OUe5Oi=>
JIMT-1 NVfV[nQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm2d4x5OSEQvF2= NXvpPFY3PSCm NH\YcFJFVVOR NWHCXVRwUUN3MEyxJO69VQ>? MlO4NlQ5Pzl5OU[=
HCC1143 NFnkV4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjDS5MyKM7:TR?= NW\qSYZ1PSCm NYHuNXBGTE2VTx?= MojSTWM2ODxzIN88US=> NYi4SJJKOjR6N{m3PVY>
HCC2218 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX6NUDPxE1? M17IRlUh\A>? MWTEUXNQ M1WxZWlEPTB:MTFOwG0> MkiwNlQ5Pzl5OU[=
MDA-MB-468 M2G1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\3OXIyKM7:TR?= MV:1JIQ> NXv4ZVJsTE2VTx?= MlPnTWM2ODxzIN88US=> NYG0VoR6OjR6N{m3PVY>
BT-20 NGDmVotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWxJO69VQ>? NICxUZk2KGR? NVz3bmd2TE2VTx?= NF7FSWJKSzVyPEGg{txO MkP5NlQ5Pzl5OU[=
MDA-MB-435 NVX5[3J5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL4N2cyKM7:TR?= MmnLOUBl M3HHfGROW09? NIDpXldKSzVyPEGg{txO NUTyO412OjR6N{m3PVY>
BT-549 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxJO69VQ>? NFLQSJU2KGR? NYfhdnQ3TE2VTx?= NUjFSJFRUUN3MEyxJO69VQ>? MlXBNlQ5Pzl5OU[=
HCC1806 NUHQW5E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV31OWx3OSEQvF2= M3TsbVUh\A>? NXPjSoVETE2VTx?= NVjwNFNUUUN3MEyxJO69VQ>? NWHz[HlNOjR6N{m3PVY>
HCC1937 NFjQXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrYWGEyKM7:TR?= MnnIOUBl NIjkTWdFVVOR M4LLNmlEPTB:MTFOwG0> NWHCNnB5OjR6N{m3PVY>
Hs578T M{GzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCxJO69VQ>? MUm1JIQ> MXXEUXNQ NX70R5BUUUN3MEyxJO69VQ>? MXyyOFg4QTd7Nh?=
LN18 MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfxT3AzOCEQvF2= M4rzcVczKGh? MVvEUXNQ MojmTWM2ODx3IN88US=> MXOyOFc1OTB5NB?=
LN229 NWnpN4o6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3H2TFIxKM7:TR?= NYP6No1uPzJiaB?= NV;DOZNDTE2VTx?= MY\JR|UxRDVizszN M{\5SVI1PzRzMEe0
LNZ308 M2nTcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjsW|kzOCEQvF2= MluyO|IhcA>? NUSwOohbTE2VTx?= NEXzfoNKSzVyPEWg{txO NV3MbGVSOjR5NEGwO|Q>
T98G MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[5PIh5OjBizszN MkDQO|IhcA>? Mn\oSG1UVw>? MUDJR|UxRDVizszN NGDsWWkzPDd2MUC3OC=>
U87 MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrLNlAh|ryP M2r4OFczKGh? M33BdWROW09? Mn;MTWM2ODx3IN88US=> NFn2VlgzPDd2MUC3OC=>
LN18 NU\XeXdNTnWwY4Tpc44hSXO|YYm= NHLwenM2KM7:TR?= NV3hNIlkOjRiaB?= MVjEUXNQ NWf5WmU5UW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NHLiXYYzPDd2MUC3OC=>
LNZ308 NHW0[W9HfW6ldHnvckBCe3OjeR?= NWf6SmJ7PSEQvF2= MmTGNlQhcA>? MknoSG1UVw>? M4e3N2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? MkLqNlQ4PDFyN{S=
Saos-2 NIDwSG5HfW6ldHnvckBCe3OjeR?= MmTVOVAh|ryP MnH4OFghcA>? MWHJcohq[mm2czDj[YxtKGmwdnHzbY9v NXXZclJTOjR5Mke2OlA>
MG-63 MkLwSpVv[3Srb36gRZN{[Xl? MlTNOVAh|ryP NHrDU3A1QCCq NFT3bXJKdmirYnn0d{Bk\WyuIHnueoF{cW:w NXjSZYxLOjR5Mke2OlA>
SJSA-1 MnzVSpVv[3Srb36gRZN{[Xl? NV3UV4hoPTBizszN NFvsTlk1QCCq M{DrNmlvcGmkaYTzJINmdGxiaX72ZZNqd25? M3jwUVI1PzJ5Nk[w
Saos-2 M4\XSmZ2dmO2aX;uJGF{e2G7 NI[5PYM2OCEQvF2= NIjm[FI1QCCq MX;Jcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NGmySWozPDd{N{[2NC=>
MG-63 NUTWflR4TnWwY4Tpc44hSXO|YYm= MV61NEDPxE1? NX\N[ZprPDhiaB?= MULJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u M3THXVI1PzJ5Nk[w
SJSA-1 M1vpOWZ2dmO2aX;uJGF{e2G7 M1vy[|UxKM7:TR?= MmPFOFghcA>? NGfDXYlKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v NXW0bW53OjR5Mke2OlA>
Saos-2 M3TpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWO1NEDPxE1? MVy0PEBp M3LxcmlvcGmkaYTzJINmdGxidnnhZoltcXS7 NYnzVHExOjR5Mke2OlA>
MG-63 NVH5eWR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVm1NEDPxE1? NEPOWm01QCCq NIXtNXBKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= M1Tt[|I1PzJ5Nk[w
SJSA-1 NIPVbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HBOVUxKM7:TR?= MYG0PEBp MoLqTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? M3\rOFI1PzJ5Nk[w
FaDu NX:4e|hYTnWwY4Tpc44hSXO|YYm= MnvkOUDPxE1? NULs[mFJOjRiaB?= NWflTJZsTE2VTx?= NYH3OWVnWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MonHNlQ3OzFzNEe=
EMT6 NH;ZTIJHfW6ldHnvckBCe3OjeR?= Ml7nOUDPxE1? NX3JeWtoOjRiaB?= MoH1SG1UVw>? MXfS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NWXjV25iOjR4M{GxOFc>
HCT116 MVLGeY5kfGmxbjDBd5NigQ>? Mkj0OUDPxE1? NHrhTlQzPCCq Ml3LSG1UVw>? M1LZPXJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u MoCxNlQ3OzFzNEe=
U87 MmnTSpVv[3Srb36gRZN{[Xl? MVu1JO69VQ>? MXuyOEBp MkTFSG1UVw>? MWPS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= M4TBVVI1PjNzMUS3
GBM NGfSS5BCeG:ydH;zbZMhSXO|YYm= MYGy{txO NV;ySZQ6PDiq NWTrNYdjTE2VTx?= MVPpcoR2[2WmIHjp[4hmeiCuZY\lcJMhd2ZiYYDvdJRwe2m|LDDhcoQh\GWlcnXhd4VlKGOnbHygeoli[mmuaYT5 MnfwNlQ2ODB2OUK=
BON NYTXTW1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\0dJUyNTYQvF2= NXfOcIk5PzKq M3T3c4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MoPXNlQ1PDN3MkO=
BON M3\LU2Fxd3C2b4Ppd{BCe3OjeR?= MUWxMVXPxE1? MXiyOIg> MXXpcoNz\WG|ZYOgZZBweHSxc3nz MXWyOFQ1OzV{Mx?=
H1975 NUjYdHlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLwNE4{NTlwNt88US=> MkPlO|Jp M1GyVWROW09? M4DyZ2lEPTB;MT6zPFXPxE1? NF[yPXEzPDN|N{i0Oi=>
H1975 NXraem85SXCxcITvd4l{KEG|c3H5 MWSy{txO M2T5e|I1cA>? MlGwSG1UVw>? MXPpcoNz\WG|ZYOgZZBweHSxc3nzJJJifGVic3nncolncWOjboTsfS=> NH;GUGUzPDN|N{i0Oi=>
T-ALL MnO5RZBweHSxc3nzJGF{e2G7 NGLCSZJj\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW= NF61clczPCCxcjC0PIg> NW[2[XpzTE2VTx?= M2fJR4Fn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz M3[5UlI1OzFyN{O2
BCR-ABL NXfwbWxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj6VWxMOC5{NT2xNO69VQ>? Mn7vOIQ> NH7tWJJ{cWewaX\pZ4FvfGy7IHnubIljcXRiY3XscEBxem:uaX\ldoF1cW:w M2r6SVI1OjR2NkGy
LC-1/SQSF MWDGeY5kfGmxbjDBd5NigQ>? MkLzN:69VQ>? MmrFNlRp NYnseHZvTE2VTx?= NHLoXI1l\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> M{TvUlI{QThyMEmz
Primary CLL cells MWfBdI9xfG:|aYOgRZN{[Xl? M2LVNlEuOTEQvF2= NWLKeINxPDiq M1[zVYlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> NXnaNlZUOjN6NUC4NFc>
Primary CLL cells MUTLbY5ie2ViQYPzZZk> M{nFZlLPxE1? NWT3bGFiOzCvaX6= MYjk[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>? NVTsPI5rOjN6NUC4NFc>
Primary CLL cells NXjXXnhZS3m2b4TvfIlkKEG|c3H5 NVPnbZRCOs7:TR?= MVSyOIg> M3W3PIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MYqyN|g2ODhyNx?=
human NSCLC cell lines NVro[Zl7SXCxcITvd4l{KEG|c3H5 NGXsNogxNjF{NT20{txO NXfjPFl2OjSq NGn3d2RFVVOR MUjJR|UxeyC{YX7n[ZMh\nKxbTCwMlQuOs7:TR?= NH;sbVIzOzV4MkS3Ni=>
human HCC cell lines MXLD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NVq4UYdxOC5yMEWtNe69VQ>? MVK0PIg> MUjJR|UxRTIQvF2= M{DjfFI{PDh7OUm5
Huh7 NX23[VNxU2mwYYPlJGF{e2G7 MXKx{txO NWS3d3VIPDiq NFTtO3d{cWewaf-shYNidnSueTDy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDBb5Q> MXKyN|Q5QTl7OR?=
SK-HEP1 NVXyUGxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvjUoMyNTJyzszN NETROY04Omh? NHThbHlFVVOR NGD2fodKSzVy78{cNe69VQ>? M{DSfVI{PDd7MUO2
786-0 M4TP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:xMVIx|ryP M4\BSFczcA>? MVHEUXNQ NIX5S4hKSzVy78{cNe69VQ>? MlruNlM1PzlzM{[=
JVM2 NV\0NHpvS3m2b4TvfIlkcXS7IHHzd4F6 M3S3dFAvOi1{MN88US=> M1n4elczcA>? M3v1XGROW09? M334XmlEPTB;MD65{txO MlvNNlMzOzh4M{m=
EHEB M1;KbGN6fG:2b4jpZ4l1gSCjc4PhfS=> MViwMlIuOjEQvF2= Ml24O|Jp NXTwS2RZTE2VTx?= M4P3O2lEPTB;MD63{txO M4j6ZlI{OjN6NkO5
MEC2 MYjDfZRwfG:6aXPpeJkh[XO|YYm= M4LzcVAvOi1{MN88US=> M1S2dFczcA>? NGizPIJFVVOR Ml7QTWM2OD1yLkhOwG0> NFHJNXMzOzJ|OE[zPS=>
primary B-CLL lymphocytes MVjBdI9xfG:|aYOgRZN{[Xl? NVPQPFhmUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= NFjZWlEzPGh? NWXBV2ZOTE2VTx?= M{TsbWlEPTExvKyz{txOKG[xcjDhcIwheGG2aXXueJM> MoDINlMzOzh4M{m=
primary B-CLL lymphocytes M1\0S2tqdmG|ZTDBd5NigQ>? NWSwU3BDUUN3MDDmc5Ih\WGlaDDwdolu[XK7IHPlcIwhdGmwZR?= NY\NWXFxOjSq Moj0bY5pcWKrdIOgdFcxWz[NID[gOGUuSlBzIHX4dJJme3Orb36= MmHaNlMzOzh4M{m=
human NSCLC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fZNlAvPS1{zszN M1;DPFczcA>? NHPPZZhKSzVyPUJOwG0> NXG2V4FkOjJ5OEGzPVM>
human NSCLC M37SdGtqdmG|ZTDBd5NigQ>? NIKyXnYy|ryP MYSyOIg> MVfpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 MWiyNlc5OTN7Mx?=
Y1 cell line MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3GcY0xNjIQvF2vNe69VQ>? NUHybopvOjSq NXHSTWlWTE2VTx?= NWLJOIxucW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= M1LETlIzPjl{OUC0
PIK3CA-mutant MCF7 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPTS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MXS3Nog> MoHiS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? M1Oze|IzPjV|OU[3
PIK3CA-mutant MCF7 NFf1W5NMcW6jc3WgRZN{[Xl? MXzJR|UxRTFzNNMxN45O M{exWFczcA>? NXHBc2NJUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=> NWTVbIlnOjJ4NUO5Olc>
MCF7-myr-Akt M{TZfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;qOGhIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= M3jUSFczcA>? M{K1ZWdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P M2\q[FIzPjV|OU[3
colon cancer cell lines MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvWU2UxNTFyzszN M{fkcFczcA>? MlXKSG1UVw>? NFLEd|dKSzVyPUJOwG0> Ml\CNlI2PDN6NUe=
gastric cancer cell lines M1vMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGwMVEx|ryP M1:5elczcA>? MYPEUXNQ MluzTWM2OD1{LUZOwG0> NIXPTZIzOjV2M{i1Oy=>
HCT-116/HT-29/MKN-45 M4q2TGFxd3C2b4Ppd{BCe3OjeR?= Ml:3Nu69VQ>? NWPMTYh4PDiq NX;5Z2hOe2irZoSgbY4hTzJicHjhd4U> M{nkPVIzPTR|OEW3
HT-29 and HCT-116 M{nCb2Nie3Cjc3WgZZN{[Xl? NVXp[VJzPc7:TR?= NVjQSpVDOjSq MmexbY5lfWOnczDjZZNx[XOnIHHjeIl3cXS7 M2D6V|IzPTR|OEW3
MM cell lines M1HTUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HUVlEx|ryP NXzFe3lmOjSq MVvEUXNQ M4XYV2lEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? NVTGN5VsOjJ{MEe0PFU>
ARP-1 Mn\3RZBweHSxc3nzJGF{e2G7 MVqxNO69VQ>? NY\ZRlRtOjSq M2ixRmROW09? NVrjRo1{cW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> MXSyNlIxPzR6NR?=
SNU-601 NXzqN5ZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe3Nog> MYXEUXNQ NWP3W4xqUUN3ME2wMlgyPsLzMD6wOlPPxE1? MkHPNlIyPTl6MUS=
SNU-1 NH\aW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrNbIU4Omh? MojOSG1UVw>? M2rGbmlEPTB;MT6wPFLDuTBwMEK4{txO NHHkZ3YzOjF3OUixOC=>
SNU-668 NYr4O|diT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofCO|Jp M17ld2ROW09? M4Wyd2lEPTB;MT61O|nDuTBwMEe0{txO NVHJVHpzOjJzNUm4NVQ>
AGS M2TBPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nBV|czcA>? Mn\pSG1UVw>? MV7JR|UxRTFwN{G0xtExNjFzN988US=> MYWyNlE2QThzNB?=
SNU-216 NXLHV5h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHBPVA4Omh? M{\1ZWROW09? Mn7XTWM2OD1{Lk[5NuKyOC5yOENOwG0> NVu3Vo9COjJzNUm4NVQ>
SNU-5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XrXlczcA>? NYPIbFZPTE2VTx?= M3TjcmlEPTB;MT6zOVHDuTBwMEmx{txO NVnxUW9{OjJzNUm4NVQ>
SNU-638 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPJfJJ7PzKq M1r6OmROW09? Mlj0TWM2OD1{LkK4NuKyOC5yNUROwG0> MXKyNlE2QThzNB?=
SNU-16 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHKSnQ4Omh? NFzXRlFFVVOR MnnHTWM2OD1zLkW3N:KyOC5yMEJOwG0> M{\PbVIzOTV7OEG0
SNU-484 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\HO|Jp NIXtN2JFVVOR NIDoVmtKSzVyPUGuO|I5yrFyLkC0Oe69VQ>? NIC1N2czOjF3OUixOC=>
SNU-620 NV\SUppoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K4cFczcA>? NUXGU2lMTE2VTx?= MWPJR|UxRTJwOUO5xtExNjByMd88US=> MnzCNlIyPTl6MUS=
SNU-719 NVfTRo1xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUO3Nog> NIS5XFhFVVOR M3;oXWlEPTB;Mz6wN|fDuTBwMEOy{txO NHjWUFgzOjF3OUixOC=>
glioma cell lines MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnVc204Omh? MojaTWM2OD1zLUNOwG0> MVKyNlA3PTB6MB?=
U87 MUDBdI9xfG:|aYOgRZN{[Xl? NXjuXVQ2Os7:TR?= M2jEflczcA>? NX\4e|lCcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDhcoQh[2ynYY\l[EBRSVKSIHHu[EBk[XOyYYPlMVM> MVqyNlA3PTB6MB?=

... 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 individually and in order:
5% DMSO+30% PEG 300+ddH2O		 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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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

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID