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 NXfVO5pkS3m2b4TvfIlkKEG|c3H5 NYT4[2RnPzJiaB?= MlTrSG1UVw>? M4O4PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh\XiycnXzd4lv\yCSSUPLZYxxcGFiRUW0OWshdXW2YX70JJdqfGhiR1m1NEBw\iByLkCwNFE2QCEQvF2= NWXOS4gzOjR7MECyOlY>
DU145 M1Hh[WN6fG:2b4jpZ{BCe3OjeR?= MlPTO|IhcA>? M{j3SmROW09? MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1? M2TEV|I1QTByMk[2
A2780 NYn4OYJqS3m2b4TvfIlkKEG|c3H5 M{jTe|czKGh? NISzW2tFVVOR NH\PU4ZEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN NETlWGkzPDlyMEK2Oi=>
U87MG NVj2dGdkS3m2b4TvfIlkKEG|c3H5 MUK3NkBp MXHEUXNQ NV;mSZpvS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjl6IN88US=> NUfENnoyOjR7MECyOlY>
A2780 NYPYdZJtTnWwY4Tpc44hSXO|YYm= NHXjO2oyKGh? NGDIO|JFVVOR NUHkbnlqUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlA2PSEQvF2= NHvuWI8zPDlyMEK2Oi=>
DU145 M2\IemZ2dmO2aX;uJGF{e2G7 NHnVVFkyKGh? MmriSG1UVw>? NVLZbIgzUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKESXMUS1JINmdGy|IHjhdoJwemmwZzDMT2IyKG23dHH0bY9vKHerdHigSWM2OCCxZjCwMlA4OyEQvF2= NEnLWoszPDlyMEK2Oi=>
A2780 MVnGeY5kfGmxbjDBd5NigQ>? MXixJIg> NV2yfFRzTE2VTx?= NWTSVW1{UW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2= MoTCNlQ6ODB{Nk[=
MCF7 NEK4TnNHfW6ldHnvckBCe3OjeR?= NIjqXXQyKGh? MWnEUXNQ NVvwV2NMUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP MkXrNlQ6ODB{Nk[=
U87MG M4i0NGZ2dmO2aX;uJGF{e2G7 NWPjWXE{OSCq MVTEUXNQ MUPJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO NFfs[3kzPDlyMEK2Oi=>
A2780 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXq3NkBp NYXSfVdKTE2VTx?= MV\FR|UxRTBwNUKg{txO NFvGWJQzPDlyMEK2Oi=>
SKMES-1 NIjofnREgXSxdH;4bYMhSXO|YYm= Mn\PNUDPxE1? NFO1S3k4OiCq MYLJcoR2[2W|IHPlcIwh\GWjdHi= NGfLT5IzPjBzM{OxPC=>
H596 NYW3R4FRTnWwY4Tpc44hSXO|YYm= NFHoS3cyKM7:TR?= NHLOVm9KdXCjaYLzJINmdGxibXnndoF1cW:w NUfUeopqOjZyMUOzNVg>
HCC2450 M2rqZmZ2dmO2aX;uJGF{e2G7 MUKxJO69VQ>? MUfJcZBicXK|IHPlcIwhcW64YYPpc44> M4HSXlI3ODF|M{G4
A549 NE[zSFJHfW6ldHnvckBCe3OjeR?= MUO1NFAhdk1? MXm0PEBp NFLIe41FVVOR MlO3TY5pcWKrdIOgRYt1KGGldHn2ZZRqd25? Mn64NlU6Ozd{OUm=
A549 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13hOFEh|ryP NGr3dG04OiCq MkPVSG1UVw>? MUHJcohq[mm2czDj[YxtKGe{b4f0bC=> NWKxeJpvOjV7M{eyPVk>
H522 M3vzUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXtb5NTOSEQvF2= Mo\iO|IhcA>? M3nufmROW09? NVzwVldpUW6qaXLpeJMh[2WubDDndo94fGh? Mki2NlU6Ozd{OUm=
LNCaP NYS4dW1WTnWwY4Tpc44hSXO|YYm= M1PMZVEh|ryP NUnmVpp[W3WycILld5NmeyCyLVHLWEBt\X[nbIO= M2XpNFI2OzZyN{m5
LNCaP95 MXLGeY5kfGmxbjDBd5NigQ>? MmfVNUDPxE1? NHWxOnlUfXCycnXzd4V{KHBvQVvUJIxmfmWucx?= MnLGNlU{PjB5OUm=
HCT-15 NXmwb2pMSXCxdH;zbZMhSXO|YYm= MYGxNEDPxE1? MWW0PEBp MnTySG1UVw>? NIPZ[I1KdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVUh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M33BSlI2OTV{MkS1
HCT-116 MV\BdI91d3OrczDBd5NigQ>? MX[xNEDPxE1? M1iz[FQ5KGh? M4m5XGROW09? NXrVW49NUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVEyPiClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u NHjJNoIzPTF3MkK0OS=>
NCI-H460 M4X4eWFxd3Sxc3nzJGF{e2G7 NGCzbm0yOCEQvF2= MWq0PEBp NU\GcW9NTE2VTx?= NUG4Wm9qUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=> Mmm4NlUyPTJ{NEW=
SKOV-3 Mn35RZBwfG:|aYOgRZN{[Xl? NWOybmJlOTBizszN MlK3OFghcA>? NWTBV3dZTE2VTx?= MYHJcoR2[2W|IHHwc5B1d3OrczDpckBUU0:YLUOgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NYnvb5pPOjVzNUKyOFU>
BSY-1 NF[xeVBCeG:2b4Ppd{BCe3OjeR?= NX31dIg{OTBizszN MojSOFghcA>? NUOwXVlVTE2VTx?= M1\vNmlv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M1rpdVI2OTV{MkS1
MKN-1 NGrGUndCeG:2b4Ppd{BCe3OjeR?= M{XHOVExKM7:TR?= MljHOFghcA>? Ml6xSG1UVw>? MnnrTY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? M{LGelI2OTV{MkS1
NCI-H522 M{P2S2Fxd3Sxc3nzJGF{e2G7 NVjWfWFSOTBizszN NEHhb5Y1QCCq NEjwWpFFVVOR M4ju[Wlv\HWlZYOgZZBweHSxc3nz NVX1UFRFOjVzNUKyOFU>
OVCAR-3 MXfBdI91d3OrczDBd5NigQ>? MUmxNEDPxE1? M12zSFQ5KGh? NXzCPHhLTE2VTx?= M{X0ZWlv\HWlZYOgZZBweHSxc3nz NUnCSXh4OjVzNUKyOFU>
HBC-5 NFT4VmNCeG:2b4Ppd{BCe3OjeR?= MX2xNEDPxE1? MVy0PEBp NVj2[JVJTE2VTx?= M3vaOmlv\HWlZYOgZZBweHSxc3nz NXvtUWVOOjVzNUKyOFU>
RXF-631L M4fSOWFxd3Sxc3nzJGF{e2G7 MoDzNVAh|ryP NV7hZ5ExPDhiaB?= M2\ROGROW09? MW\JcoR2[2W|IHHwc5B1d3Orcx?= NWnsZ3hGOjVzNUKyOFU>
MKN-45 NILBeJlCeG:2b4Ppd{BCe3OjeR?= NHPEbXQyOCEQvF2= NVTwU49WPDhiaB?= MnTGSG1UVw>? NXX4OHBZUW6mdXPld{BieG:ydH;zbZM> MoPPNlUyPTJ{NEW=
BON-1 MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTqUHc2ODBibl2= NF3tSHEyOCCm NFu1cpVFVVOR NIjvVXNKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHLMPWEzPTB{NkK5Ni=>
BON-1 NUjkfWRRTnWwY4Tpc44hSXO|YYm= NX:xVGs4PTByIH7N MoHvOEBp M2S4fGROW09? M{e0cmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= NFO0[ogzPTB{NkK5Ni=>
QGP-1 NYXw[HRITnWwY4Tpc44hSXO|YYm= NXviWWdHPTByIH7N NITScpY1KGh? NYW5SFUyTE2VTx?= MlTqTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= MVyyOVAzPjJ7Mh?=
Huh7 M1rGWWZ2dmO2aX;uJGF{e2G7 MYGxJO69VQ>? M1nneVEhcA>? MYXEUXNQ MULJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGPldlQ4PA>? NHnON2wzPTByNESwNy=>
BNL NHnhSHVHfW6ldHnvckBCe3OjeR?= MXixJO69VQ>? NVrtUok3OSCq MlTjSG1UVw>? NUewWlFIUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKFN4 NUjINWcyOjVyMES0NFM>
MDA-MB-175 MmXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\0NUDPxE1? NFzQW3E2KGR? NUjzTG9xTE2VTx?= M{jDW2lEPTB:MTFOwG0> Mn\zNlQ5Pzl5OU[=
MDA-MB-134 NWHQVZZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG3XlUyKM7:TR?= MXm1JIQ> NWnwXZU3TE2VTx?= NH;iT4RKSzVyPEGg{txO NVnNfoVHOjR6N{m3PVY>
HCC1500 NHTrUXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqxJO69VQ>? M37ucVUh\A>? MWTEUXNQ M3fremlEPTB:MTFOwG0> NV;BeHNIOjR6N{m3PVY>
EFM-19 NHjJUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWji[GZVOSEQvF2= NHjnXFU2KGR? M4rHOGROW09? MVLJR|UxRDFizszN NF\6TVEzPDh5OUe5Oi=>
ZR-75-30 M{LseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS1NUDPxE1? M4Cx[VUh\A>? NGrHUXRFVVOR MlHYTWM2ODxzIN88US=> NI[zfYMzPDh5OUe5Oi=>
MDA-MB-361 NXT1UopCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfPc3EyKM7:TR?= MljaOUBl MUjEUXNQ NEK5SJNKSzVyPEGg{txO MUOyOFg4QTd7Nh?=
T-47D NGXzOJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF6zSlkyKM7:TR?= NHXS[mY2KGR? NYXYXo5UTE2VTx?= NECzcHFKSzVyPEGg{txO NWLFR3AyOjR6N{m3PVY>
SK-BR-3 MnK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTZNUDPxE1? MmHHOUBl MnHhSG1UVw>? Mn\RTWM2ODxzIN88US=> NVno[FNwOjR6N{m3PVY>
UACC-732 NV7SfGxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPVNUDPxE1? MXG1JIQ> MVHEUXNQ M4H6SWlEPTB:MTFOwG0> MYWyOFg4QTd7Nh?=
BT-474 NHq3dFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLKNUDPxE1? NF2wOZk2KGR? M2LqWmROW09? MYrJR|UxRDFizszN M1TQ[lI1QDd7N{m2
HCC202 M37pXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\XNm4yKM7:TR?= MkS2OUBl NUL3dlh1TE2VTx?= NFLEclRKSzVyPEGg{txO NXK4Z2E3OjR6N{m3PVY>
MCF7 M1HHOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvONUDPxE1? NIf6SII2KGR? NFTJU|RFVVOR MX;JR|UxRDFizszN M4DKO|I1QDd7N{m2
MDA-MB-415 MoTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInhSGMyKM7:TR?= NF3aT4Q2KGR? MojOSG1UVw>? NWHwWVczUUN3MEyxJO69VQ>? NX3sUGdDOjR6N{m3PVY>
MDA-MB-453 NXzueIJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHVXW4yKM7:TR?= MWm1JIQ> NILmOnJFVVOR NITDdFlKSzVyPEGg{txO Ml[xNlQ5Pzl5OU[=
ZR-75-1 M1yyPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojRNUDPxE1? NYjLc2FuPSCm M{TBcWROW09? M4naeGlEPTB:MTFOwG0> NUDXV4M5OjR6N{m3PVY>
HCC38 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXyxJO69VQ>? NGPwSII2KGR? M1fCT2ROW09? MnL1TWM2ODxzIN88US=> MlGyNlQ5Pzl5OU[=
HCC1419 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuxJO69VQ>? NFXy[|Y2KGR? NHzWZXFFVVOR MYPJR|UxRDFizszN NXW4WHJ7OjR6N{m3PVY>
UACC-812 NFvufVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\3PGYyKM7:TR?= NIS4Nng2KGR? NGTFU2VFVVOR MnriTWM2ODxzIN88US=> Mm\yNlQ5Pzl5OU[=
HCC1187 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDrSVNoOSEQvF2= NWDG[2FZPSCm MWXEUXNQ NF\yfmRKSzVyPEGg{txO M2HU[|I1QDd7N{m2
KPL-1 M2DVTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWxJO69VQ>? NH;MXZE2KGR? M3\EO2ROW09? NXPzcVJXUUN3MEyxJO69VQ>? NUnTfmQxOjR6N{m3PVY>
SUM-225 M4Kwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn3TVMyKM7:TR?= NYPl[G1nPSCm NHjJb|JFVVOR MVjJR|UxRDFizszN Ml72NlQ5Pzl5OU[=
EFM-192A NHGzbHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnjWWYyKM7:TR?= MX21JIQ> NH3OOZJFVVOR MoPHTWM2ODxzIN88US=> NHTBWXozPDh5OUe5Oi=>
JIMT-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK0UpEyKM7:TR?= NHWyU282KGR? NXH4V4lrTE2VTx?= MWDJR|UxRDFizszN NHPkbHkzPDh5OUe5Oi=>
HCC1143 M4rtOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjmVGhjOSEQvF2= NYrVUnZDPSCm NYnkWHhqTE2VTx?= MnKwTWM2ODxzIN88US=> MXyyOFg4QTd7Nh?=
HCC2218 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrVXJhjOSEQvF2= MorjOUBl NVzCO41ETE2VTx?= Mm\BTWM2ODxzIN88US=> NFvNUW8zPDh5OUe5Oi=>
MDA-MB-468 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfmNUDPxE1? M4rVWVUh\A>? NWq2T|JzTE2VTx?= MWHJR|UxRDFizszN NV6yXJdjOjR6N{m3PVY>
BT-20 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX34UVBDOSEQvF2= Mn7lOUBl M3jiS2ROW09? MoG4TWM2ODxzIN88US=> NYPDVHlTOjR6N{m3PVY>
MDA-MB-435 Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHGNUDPxE1? MkD1OUBl NFjwe3NFVVOR MnvWTWM2ODxzIN88US=> NYLCTW1YOjR6N{m3PVY>
BT-549 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTBd4YyKM7:TR?= M1jzXVUh\A>? NU\WV2huTE2VTx?= Mn30TWM2ODxzIN88US=> M2PxcVI1QDd7N{m2
HCC1806 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGxJO69VQ>? MoSyOUBl MonsSG1UVw>? NYruZ|BSUUN3MEyxJO69VQ>? MWKyOFg4QTd7Nh?=
HCC1937 M{n0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSxJO69VQ>? M1jSVFUh\A>? M1ziPWROW09? MX7JR|UxRDFizszN M2DaNlI1QDd7N{m2
Hs578T NU\tWpg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFu2[5AyKM7:TR?= MWK1JIQ> NIfM[IpFVVOR MWHJR|UxRDFizszN M3;IPVI1QDd7N{m2
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LN229 M2Wzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf4U5E3OjBizszN NEX2[XU4OiCq NYTN[2Z6TE2VTx?= MluwTWM2ODx3IN88US=> Mn\RNlQ4PDFyN{S=
LNZ308 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLqNlAh|ryP NFm3S5I4OiCq M1[4VmROW09? MnPlTWM2ODx3IN88US=> NIPIZ2EzPDd2MUC3OC=>
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U87 MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuyNEDPxE1? NEfne5Q4OiCq MW\EUXNQ NH7hcXVKSzVyPEWg{txO MnrQNlQ4PDFyN{S=
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MG-63 M2LjXGZ2dmO2aX;uJGF{e2G7 M2[3clUxKM7:TR?= MmC1OFghcA>? MofUTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? NHntWoczPDd{N{[2NC=>
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MG-63 MVfGeY5kfGmxbjDBd5NigQ>? NGnLbXY2OCEQvF2= MmTMOFghcA>? MkPSTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> NXHvcG9JOjR5Mke2OlA>
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SJSA-1 NULjfZFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPYWIE2OCEQvF2= MoLCOFghcA>? NV:4RWNsUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= M2HKWVI1PzJ5Nk[w
FaDu MoPZSpVv[3Srb36gRZN{[Xl? M{ntXFUh|ryP NF[zWoszPCCq MV3EUXNQ Mn3QVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= MlPtNlQ3OzFzNEe=
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HCT116 NID5[GZHfW6ldHnvckBCe3OjeR?= NXjPTHMzPSEQvF2= MVeyOEBp NVHVU29QTE2VTx?= MYPS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= M2\zPFI1PjNzMUS3
U87 NIj3NGVHfW6ldHnvckBCe3OjeR?= NVfzVHRQPSEQvF2= NID2ZnIzPCCq M2KwdGROW09? MnTqVoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= NFm2U3AzPDZ|MUG0Oy=>
GBM M1jhVGFxd3C2b4Ppd{BCe3OjeR?= NHPDc2Ez|ryP NFTUUG01QGh? Mlv1SG1UVw>? MmezbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> NXnCelduOjR3MEC0PVI>
BON NH7CeVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rsTFEuPc7:TR?= M4S5W|czcA>? M1n4V4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> M33jTVI1PDR|NUKz
BON NV7LN49ZSXCxcITvd4l{KEG|c3H5 M2jTUVEuPc7:TR?= MlW1NlRp MnS5bY5kemWjc3XzJIFxd3C2b4Ppdy=> MX6yOFQ1OzV{Mx?=
H1975 NVrWU|N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X3T|AvOy17LkdOwG0> M13YdlczcA>? MVTEUXNQ NXXSdodmUUN3ME2xMlM5Pc7:TR?= MUeyOFM{Pzh2Nh?=
H1975 M1Xt[2Fxd3C2b4Ppd{BCe3OjeR?= MUmy{txO NEjuTHozPGh? NVLSV2xlTE2VTx?= NXnVfpBPcW6lcnXhd4V{KGGyb4D0c5NqeyC{YYTlJJNq\26rZnnjZY51dHl? M4XQelI1OzN5OES2
T-ALL MmTBRZBweHSxc3nzJGF{e2G7 NEDwc21j\XS5ZXXuJFEvPCCjbnSgOU4{KG2PIHH0JFI1cCCjbnSgNE46KGGwZDC1MlUhdU1iYYSgOFhpKGmwIHTp[oZmemWwdDDj[YxtKGyrbnW= NVr1PJdOOjRib4KgOFhp MmWwSG1UVw>? NEfXbJFi\m[nY4TzJJRp\SCSSUPLJJBifGi5YYmgbY4hXC2DTFygZ4VtdCCuaX7ldy=> NWDnPGdLOjR|MUC3N|Y>
BCR-ABL M4fpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;XZVAvOjVvMUFOwG0> MXS0[C=> MlThd4lodmmoaXPhcpRtgSCrbnjpZol1KGOnbHygdJJwdGmoZYLheIlwdg>? NWnncoNiOjR{NES2NVI>
LC-1/SQSF MmfBSpVv[3Srb36gRZN{[Xl? NFnpOGM{|ryP NHTZZWQzPGh? M{fPNGROW09? NGfSRXFl\WO{ZXHz[UBPWkZ{IIDyc5RmcW5ibHX2[Yw> NInJeYczOzl6MEC5Ny=>
Primary CLL cells MVrBdI9xfG:|aYOgRZN{[Xl? MXmxMVEx|ryP Mnf0OFhp M3ztNYlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> NVqwcIRWOjN6NUC4NFc>
Primary CLL cells MnXHT4lv[XOnIFHzd4F6 NFLXNpcz|ryP NFj4V48{OG2rbh?= NEDoSWRl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= MlnkNlM5PTB6MEe=
Primary CLL cells MVjDfZRwfG:6aXOgRZN{[Xl? NHXNUnYz|ryP M2f1UFI1cA>? NXTEc|hicW6mdXPld{Bk\WyuIHP5eI91d3irY3n0fS=> M{HQU|I{QDVyOEC3
human NSCLC cell lines MVLBdI9xfG:|aYOgRZN{[Xl? MmD1NE4yOjVvNN88US=> NV6yfYE4OjSq M3;LWmROW09? NX;KOIZmUUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> NUS5VJdqOjN3NkK0O|I>
human HCC cell lines M{[zXGNmdGxidnnhZoltcXS7IHHzd4F6 NYXzOZhkOC5yMEWtNe69VQ>? NXHvUnN4PDiq NUn6TotkUUN3ME2x{txO NVj0[JRkOjN2OEm5PVk>
Huh7 Ml;4T4lv[XOnIFHzd4F6 M37W[lHPxE1? M4Pq[VQ5cA>? M3PXVZNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M2TkPFI{PDh7OUm5
SK-HEP1 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPGNVIyNTJyzszN M{jwU|czcA>? NXvifFVMTE2VTx?= NU\ER5plUUN3MP-8oFHPxE1? NWnrPZZiOjN2N{mxN|Y>
786-0 M4Tlc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxMVIx|ryP MV63Nog> NXrzU3FXTE2VTx?= Ml23TWM2OO,:nEJOwG0> M1i5[|I{PDd7MUO2
JVM2 NFq5fZpEgXSxdH;4bYNqfHliYYPzZZk> MV6wMlIuOjEQvF2= NYnjO5lOPzKq MXHEUXNQ M{n6V2lEPTB;MD65{txO NW\sWpZtOjN{M{i2N|k>
EHEB MnuzR5l1d3SxeHnjbZR6KGG|c3H5 NWDDNppVOC5{LUKw{txO NEXuVlQ4Omh? NYrJVYRtTE2VTx?= M4rvPGlEPTB;MD63{txO MnfsNlMzOzh4M{m=
MEC2 MmrSR5l1d3SxeHnjbZR6KGG|c3H5 NXfOOVRLOC5{LUKw{txO NVXEb3dDPzKq MUDEUXNQ Mke0TWM2OD1yLkhOwG0> MoLjNlMzOzh4M{m=
primary B-CLL lymphocytes NU[5e3Q{SXCxcITvd4l{KEG|c3H5 MoX0TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MWCyOIg> NXy2TVJNTE2VTx?= MlH1TWM2OO,:nEROwG0h\m:{IHHscEBx[XSrZX70dy=> NXjRWmlDOjN{M{i2N|k>
primary B-CLL lymphocytes Mly0T4lv[XOnIFHzd4F6 MkjkTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MlzJNlRp MW\pcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= MofWNlMzOzh4M{m=
human NSCLC NUPlPJZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzEVYMxNjVvMt88US=> MoT4O|Jp M3nDeGlEPTB;Md88US=> NEDJWG4zOjd6MUO5Ny=>
human NSCLC NYHoS|l7U2mwYYPlJGF{e2G7 NXzFdopmOc7:TR?= M1zLWlI1cA>? M1\DSolvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= MnXwNlI4QDF|OUO=
Y1 cell line Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWqwMlHPxE1xMd88US=> MYmyOIg> MXfEUXNQ NIHaU4JqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= NYHLNW9IOjJ4OUK5NFQ>
PIK3CA-mutant MCF7 MoXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojrS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MVG3Nog> NXrLN5AyT0l3ME2xOlDDuTlzbl5vwKxNTDVyPUm4NOKyOjd|bl2= NWHmSY1qOjJ4NUO5Olc>
PIK3CA-mutant MCF7 M4nlc2tqdmG|ZTDBd5NigQ>? M1rNTmlEPTB;MUG0xtE{dk1? M4\2dVczcA>? MYfJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| M1fYNFIzPjV|OU[3
MCF7-myr-Akt MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HEbmdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P NVnj[lB1PzKq M1fpWGdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P MVqyNlY2Ozl4Nx?=
colon cancer cell lines MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly5NE0yOM7:TR?= MnnrO|Jp MWfEUXNQ NG\4cZpKSzVyPUJOwG0> M1PvR|IzPTR|OEW3
gastric cancer cell lines MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvrUYI2OC1zMN88US=> NUDp[HRlPzKq MlXwSG1UVw>? M2TDbGlEPTB;Mj21{txO NILPXmEzOjV2M{i1Oy=>
HCT-116/HT-29/MKN-45 M{Xjd2Fxd3C2b4Ppd{BCe3OjeR?= NULDSZFZOs7:TR?= MV60PIg> MYfzbIlnfCCrbjDHNkBxcGG|ZR?= MYmyNlU1Ozh3Nx?=
HT-29 and HCT-116 NIi5ZXFE[XOyYYPlJIF{e2G7 NX71VllFPc7:TR?= MkjwNlRp NH;zO|BqdmS3Y3XzJINie3Cjc3WgZYN1cX[rdIm= NFn5SJMzOjV2M{i1Oy=>
MM cell lines MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGGyO3EyOM7:TR?= NEn5OJIzPGh? M1v1NWROW09? MoWyTWM2OCC4YYLp[ZMh[W2xbneg[Iln\mW{ZX70JINmdGxibHnu[ZMhcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcoNm MlryNlIzODd2OEW=
ARP-1 NIjjc|NCeG:ydH;zbZMhSXO|YYm= MlTSNVDPxE1? M3nwNlI1cA>? NGW5VYNFVVOR MVzpcoR2[2W|IF3NJINmdGxiYYDvdJRwe2m|IITodo92\2hiY3HzdIF{\SCjY4TpeoF1cW:w NILEVnIzOjJyN{S4OS=>
SNU-601 NGHrUW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVi3Nog> Mo[zSG1UVw>? M1iwWGlEPTB;MD64NVbDuTBwME[z{txO NXXL[4VpOjJzNUm4NVQ>
SNU-1 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCwTm1MPzKq NIHZOpRFVVOR Mom2TWM2OD1zLkC4NuKyOC5yMklOwG0> NXPYe2p5OjJzNUm4NVQ>
SNU-668 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[3Nog> MXPEUXNQ MV3JR|UxRTFwNUe5xtExNjB5NN88US=> M3WzUFIzOTV7OEG0
AGS MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX63Nog> MkXISG1UVw>? NInFTGlKSzVyPUGuO|E1yrFyLkGxO:69VQ>? NX\rXGdyOjJzNUm4NVQ>
SNU-216 NFLBW|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHhO|Jp M1XXTGROW09? MmK2TWM2OD1{Lk[5NuKyOC5yOENOwG0> M4CyUVIzOTV7OEG0
SNU-5 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13le|czcA>? NE\OVmhFVVOR NVLkNm03UUN3ME2xMlM2OcLzMD6wPVHPxE1? MWCyNlE2QThzNB?=
SNU-638 M2q0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[3Nog> MmWwSG1UVw>? MXHJR|UxRTJwMkiyxtExNjB3M988US=> NV\3dIg3OjJzNUm4NVQ>
SNU-16 Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G4e|czcA>? NEjmWI1FVVOR Moq2TWM2OD1zLkW3N:KyOC5yMEJOwG0> NULMXXJKOjJzNUm4NVQ>
SNU-484 NH;nS41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjze244Omh? M4q5fWROW09? MUTJR|UxRTFwN{K4xtExNjB2Nd88US=> MkTiNlIyPTl6MUS=
SNU-620 NFnH[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInyd3E4Omh? NEf3ZYhFVVOR NH7iVlRKSzVyPUKuPVM6yrFyLkCwNe69VQ>? M2W2RVIzOTV7OEG0
SNU-719 NFX5ZmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXW3Nog> MWrEUXNQ NEXZS5BKSzVyPUOuNFM4yrFyLkCzNu69VQ>? M3HJZlIzOTV7OEG0
glioma cell lines MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\ROlczcA>? MmTWTWM2OD1zLUNOwG0> MVSyNlA3PTB6MB?=
U87 MUnBdI9xfG:|aYOgRZN{[Xl? NVrafFkzOs7:TR?= M33DPFczcA>? M2\YZYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiYX7kJINt\WG4ZXSgVGFTWCCjbnSgZ4F{eGG|ZT2z MVOyNlA3PTB6MB?=

... 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
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