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 NIjhRnJEgXSxdH;4bYMhSXO|YYm= NHXHTlU4OiCq NUOxO4dETE2VTx?= MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4PpcochWEl|S3HsdIhiKEV3NEXLJI12fGGwdDD3bZRpKEeLNUCgc4YhOC5yMECxOVgh|ryP MorvNlQ6ODB{Nk[=
DU145 MXfDfZRwfG:6aXOgRZN{[Xl? M4LzSlczKGh? M{nTN2ROW09? NU\oSIh3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN MnnaNlQ6ODB{Nk[=
A2780 MV;DfZRwfG:6aXOgRZN{[Xl? NWnvV2NFPzJiaB?= M2fqV2ROW09? NIrJeVZEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN NUnlboN2OjR7MECyOlY>
U87MG Mk\zR5l1d3SxeHnjJGF{e2G7 M13IcVczKGh? NHLUT5RFVVOR MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP M4DSW|I1QTByMk[2
A2780 NGjKOYRHfW6ldHnvckBCe3OjeR?= MoPSNUBp MU\EUXNQ M3n5PGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh|ryP NY\xR5Y3OjR7MECyOlY>
DU145 NF2zUJJHfW6ldHnvckBCe3OjeR?= M4S5clEhcA>? NUPhR24xTE2VTx?= MlHFTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? NGTYWJgzPDlyMEK2Oi=>
A2780 NYW4fm1TTnWwY4Tpc44hSXO|YYm= M2PkSFEhcA>? NUn2V2tQTE2VTx?= M1PJVGlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP NX3sbYQzOjR7MECyOlY>
MCF7 MWnGeY5kfGmxbjDBd5NigQ>? MUCxJIg> M4Drb2ROW09? MYrJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCHNUS1T{BufXSjboStcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMTFOwG0> NXXRTWtHOjR7MECyOlY>
U87MG M363O2Z2dmO2aX;uJGF{e2G7 MlTQNUBp MV;EUXNQ MUTJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iVUi3UWch[2WubIOge4l1cCCHQ{WwJI9nKDBwMUOg{txO NHjWNXEzPDlyMEK2Oi=>
A2780 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLrVY04OiCq NV;je2J7TE2VTx?= MlLLSWM2OD1yLkWyJO69VQ>? NX7BWZBFOjR7MECyOlY>
SKMES-1 MlLCR5l1d3SxeHnjJGF{e2G7 NH3wcVAyKM7:TR?= MkDvO|IhcA>? NG\JclVKdmS3Y3XzJINmdGxiZHXheIg> NHfHW2QzPjBzM{OxPC=>
H596 NILHRllHfW6ldHnvckBCe3OjeR?= NEPSUowyKM7:TR?= M{[yOWlueGGrcoOgZ4VtdCCvaXfyZZRqd25? MnvONlYxOTN|MUi=
HCC2450 MnTSSpVv[3Srb36gRZN{[Xl? MXmxJO69VQ>? NGTrfXlKdXCjaYLzJINmdGxiaX72ZZNqd25? NYXKeYdCOjZyMUOzNVg>
A549 NXK2e2tOTnWwY4Tpc44hSXO|YYm= MX[1NFAhdk1? MmnyOFghcA>? MlfTSG1UVw>? MlfqTY5pcWKrdIOgRYt1KGGldHn2ZZRqd25? NIHvfYIzPTl|N{K5PS=>
A549 M1O4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLUfWYyKM7:TR?= NGCwUIs4OiCq NWTWeHV7TE2VTx?= MUjJcohq[mm2czDj[YxtKGe{b4f0bC=> NVvS[FFROjV7M{eyPVk>
H522 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW3RlcyKM7:TR?= NFXsdII4OiCq NEL4PZZFVVOR NFe2bY5KdmirYnn0d{Bk\WyuIHfyc5d1cA>? M4O2RVI2QTN5Mkm5
LNCaP MlPMSpVv[3Srb36gRZN{[Xl? M4HDeVEh|ryP M{nYU3N2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NVvOXZh{OjV|NkC3PVk>
LNCaP95 NILhTJRHfW6ldHnvckBCe3OjeR?= MXqxJO69VQ>? Mn\rV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? NVLEfHp1OjV|NkC3PVk>
HCT-15 Mny3RZBwfG:|aYOgRZN{[Xl? NEfmSFQyOCEQvF2= NEj2U2k1QCCq M{[wU2ROW09? MoHaTY5lfWOnczDhdI9xfG:|aYOgbY4hUEOWLUG1JINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? M3TXXFI2OTV{MkS1
HCT-116 M{TlTGFxd3Sxc3nzJGF{e2G7 NXHsdWE{OTBizszN NFvkfIQ1QCCq MYXEUXNQ NVG0TIRTUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVEyPiClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u NYS0PJlpOjVzNUKyOFU>
NCI-H460 NFrCRXZCeG:2b4Ppd{BCe3OjeR?= NVLrOWJXOTBizszN MYO0PEBp NF:4[G1FVVOR MYDJcoR2[2W|IHHwc5B1d3OrczDpckBPS0lvSES2NEBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w M{\nelI2OTV{MkS1
SKOV-3 MYPBdI91d3OrczDBd5NigQ>? NWHjZ4VrOTBizszN NH;Qbnk1QCCq M{e0[WROW09? M1:1R2lv\HWlZYOgZZBweHSxc3nzJIlvKFONT2[tN{Bk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w MVKyOVE2OjJ2NR?=
BSY-1 NFLXdJVCeG:2b4Ppd{BCe3OjeR?= MorpNVAh|ryP NWLHelVrPDhiaB?= MXTEUXNQ NYG2OVBqUW6mdXPld{BieG:ydH;zbZMhcW5iQmPZMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M4HielI2OTV{MkS1
MKN-1 M{PzTWFxd3Sxc3nzJGF{e2G7 NGTRclMyOCEQvF2= NGHqPXM1QCCq Mo\HSG1UVw>? MYDJcoR2[2W|IHHwc5B1d3OrczDpckBOU05vMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NYG3O2FwOjVzNUKyOFU>
NCI-H522 Ml7uRZBwfG:|aYOgRZN{[Xl? NEPubpIyOCEQvF2= NGK5OIQ1QCCq M1G2XGROW09? NGjCcopKdmS3Y3XzJIFxd3C2b4Ppdy=> M1G3SlI2OTV{MkS1
OVCAR-3 MXvBdI91d3OrczDBd5NigQ>? MoTTNVAh|ryP MnfQOFghcA>? NVHsXmVYTE2VTx?= NYqzZmRwUW6mdXPld{BieG:ydH;zbZM> M37nNVI2OTV{MkS1
HBC-5 MX;BdI91d3OrczDBd5NigQ>? NH;nbG4yOCEQvF2= NWH6dpdLPDhiaB?= NUCx[WhXTE2VTx?= MoPXTY5lfWOnczDhdI9xfG:|aYO= MnnoNlUyPTJ{NEW=
RXF-631L MmHpRZBwfG:|aYOgRZN{[Xl? MUexNEDPxE1? NEDjfXU1QCCq Ml6ySG1UVw>? NYjPXFNiUW6mdXPld{BieG:ydH;zbZM> MWmyOVE2OjJ2NR?=
MKN-45 NEDoZ4JCeG:2b4Ppd{BCe3OjeR?= NVfGUFNCOTBizszN NYjFPFV2PDhiaB?= MkXWSG1UVw>? NHLIVpZKdmS3Y3XzJIFxd3C2b4Ppdy=> MnjmNlUyPTJ{NEW=
BON-1 NVrlRWw3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\pNmZ1PTByIH7N MXOxNEBl M3PPfWROW09? MVLJcohq[mm2czDj[YxtKGe{b4f0bC=> Ml:0NlUxOjZ{OUK=
BON-1 M4LIZ2Z2dmO2aX;uJGF{e2G7 NF7RcFA2ODBibl2= NGC1VIw1KGh? NWe2dFg4TE2VTx?= M1O2NWlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgWIhzOzB6IHHu[EBU\XJ2N{O= NWTBV3hpOjVyMk[yPVI>
QGP-1 Ml63SpVv[3Srb36gRZN{[Xl? NXO5XYxFPTByIH7N M3LhWFQhcA>? M1exZWROW09? NX;GXoFyUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> M3TOSlI2ODJ4Mkmy
Huh7 MVrGeY5kfGmxbjDBd5NigQ>? MVmxJO69VQ>? NUnzS3RXOSCq NHrPRlBFVVOR NELsfGdKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuWIHH0JHNmejR5NB?= M1K2eVI2ODB2NECz
BNL NW\vfVhtTnWwY4Tpc44hSXO|YYm= Ml7UNUDPxE1? M3XNPVEhcA>? NYfJ[o82TE2VTx?= MljJTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3 M3[5[FI2ODB2NECz
MDA-MB-175 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqxJO69VQ>? NXzUTHV3PSCm NUKzcnR7TE2VTx?= M1XIR2lEPTB:MTFOwG0> MWGyOFg4QTd7Nh?=
MDA-MB-134 M4P6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzROlQyKM7:TR?= NGL4OIM2KGR? NGDnNFJFVVOR M1\MZ2lEPTB:MTFOwG0> M1;r[lI1QDd7N{m2
HCC1500 M4mzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVixJO69VQ>? M2fVZVUh\A>? MkOxSG1UVw>? MUDJR|UxRDFizszN NITY[|kzPDh5OUe5Oi=>
EFM-19 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fnNlEh|ryP MX21JIQ> M1G0b2ROW09? Mn7tTWM2ODxzIN88US=> Mk\2NlQ5Pzl5OU[=
ZR-75-30 M4PMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHv3cpgyKM7:TR?= NEfxVXE2KGR? MnvwSG1UVw>? NUSwOnVOUUN3MEyxJO69VQ>? M17rWFI1QDd7N{m2
MDA-MB-361 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojzNUDPxE1? NVfXPFMxPSCm MmrwSG1UVw>? M{PTZmlEPTB:MTFOwG0> MVWyOFg4QTd7Nh?=
T-47D NF7LcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHqNUDPxE1? MVi1JIQ> NXvaPZNvTE2VTx?= M3rt[2lEPTB:MTFOwG0> M4PsdlI1QDd7N{m2
SK-BR-3 NV7QbYRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTpNUDPxE1? MVW1JIQ> Mk\zSG1UVw>? NVS2dGJKUUN3MEyxJO69VQ>? MlfCNlQ5Pzl5OU[=
UACC-732 NH7teVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVexJO69VQ>? NFLCO3k2KGR? MkSwSG1UVw>? NX;VUI5rUUN3MEyxJO69VQ>? NFi5SZIzPDh5OUe5Oi=>
BT-474 Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXUbGgyKM7:TR?= NGXkcmY2KGR? M2nObGROW09? NH;jT|JKSzVyPEGg{txO MVmyOFg4QTd7Nh?=
HCC202 MlXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ruOlEh|ryP M3TMVFUh\A>? NHTRV4hFVVOR MUPJR|UxRDFizszN NWLkRW5MOjR6N{m3PVY>
MCF7 M12wdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXVRlEyKM7:TR?= NWLqVYhWPSCm NEXWUVJFVVOR NVPzRZRNUUN3MEyxJO69VQ>? NHmz[ZgzPDh5OUe5Oi=>
MDA-MB-415 M1nVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LNSVEh|ryP M2XBfVUh\A>? NUTrUXUyTE2VTx?= MXLJR|UxRDFizszN MXOyOFg4QTd7Nh?=
MDA-MB-453 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;1NUDPxE1? M1zFeVUh\A>? NUGwb|J1TE2VTx?= NXTkdoxDUUN3MEyxJO69VQ>? MY[yOFg4QTd7Nh?=
ZR-75-1 NEK2ZoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\pXVEh|ryP NVT5[IlkPSCm M1nlVGROW09? NFHlTGdKSzVyPEGg{txO NHHFOmUzPDh5OUe5Oi=>
HCC38 M3nNe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmxJO69VQ>? M4L4NlUh\A>? NGHxS4FFVVOR NVzhc4R3UUN3MEyxJO69VQ>? M2nlZVI1QDd7N{m2
HCC1419 NH3EcIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOxJO69VQ>? MWW1JIQ> Ml\XSG1UVw>? NUW1W3U3UUN3MEyxJO69VQ>? MU[yOFg4QTd7Nh?=
UACC-812 MoTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELX[pUyKM7:TR?= NVrxS2JQPSCm MoDNSG1UVw>? M2XjV2lEPTB:MTFOwG0> M1LGeVI1QDd7N{m2
HCC1187 M3fWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCxJO69VQ>? MUG1JIQ> NHzLPGtFVVOR M2n5e2lEPTB:MTFOwG0> NIjxXVQzPDh5OUe5Oi=>
KPL-1 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHGRYwyKM7:TR?= MmjaOUBl NXHQUJE3TE2VTx?= NE\YdFhKSzVyPEGg{txO NHnQSZczPDh5OUe5Oi=>
SUM-225 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofONUDPxE1? NWjWOWpyPSCm MoT4SG1UVw>? NYO1dJpWUUN3MEyxJO69VQ>? MYGyOFg4QTd7Nh?=
EFM-192A NXKyfGV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmxJO69VQ>? M2j0ZlUh\A>? MmOySG1UVw>? MnSxTWM2ODxzIN88US=> NEj6OVAzPDh5OUe5Oi=>
JIMT-1 M121NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\EUFEh|ryP Mn3EOUBl NHTscFlFVVOR NGDvbmlKSzVyPEGg{txO MWGyOFg4QTd7Nh?=
HCC1143 MljJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLXdmFDOSEQvF2= NVLmXZhJPSCm NEPOe41FVVOR NXHPc4xoUUN3MEyxJO69VQ>? MnPzNlQ5Pzl5OU[=
HCC2218 NGL4UIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTwR5luOSEQvF2= MUm1JIQ> NFXwc5FFVVOR NHXkOYRKSzVyPEGg{txO MVGyOFg4QTd7Nh?=
MDA-MB-468 NUXTcpo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInHe4YyKM7:TR?= MVS1JIQ> MoTaSG1UVw>? MVHJR|UxRDFizszN M1jNb|I1QDd7N{m2
BT-20 NUTObGlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHmOIduOSEQvF2= NVXDRpBjPSCm NFjGU|dFVVOR NETCN2RKSzVyPEGg{txO M3;sfFI1QDd7N{m2
MDA-MB-435 Mn20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTMNUDPxE1? NGLCfI82KGR? NELh[IZFVVOR NF;iWWpKSzVyPEGg{txO NWLCUW15OjR6N{m3PVY>
BT-549 NWTU[|JpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxJO69VQ>? NIni[5Y2KGR? M1PCXmROW09? NV7UVGMyUUN3MEyxJO69VQ>? MWCyOFg4QTd7Nh?=
HCC1806 NXjwS4M{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHW[ngyKM7:TR?= NGDTcHc2KGR? NH\hN21FVVOR MnfaTWM2ODxzIN88US=> NIi0WnkzPDh5OUe5Oi=>
HCC1937 MoD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLONUDPxE1? M17YfFUh\A>? M4ewOGROW09? M1PifmlEPTB:MTFOwG0> MXqyOFg4QTd7Nh?=
Hs578T NWfOWW5GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mli0NUDPxE1? MkPjOUBl NYmxfnA5TE2VTx?= NYnZTmZDUUN3MEyxJO69VQ>? M2XtbVI1QDd7N{m2
LN18 M2e4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LJWFIxKM7:TR?= MWe3NkBp NUXaOlE5TE2VTx?= NH7TcIpKSzVyPEWg{txO NVvKXXVvOjR5NEGwO|Q>
LN229 NWfZd3FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrhUXYzOCEQvF2= M2XnTVczKGh? M3G2bWROW09? M3e0fmlEPTB:NTFOwG0> M1\WO|I1PzRzMEe0
LNZ308 M4m5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mof5NlAh|ryP Mlq4O|IhcA>? Mn3HSG1UVw>? MUjJR|UxRDVizszN NH\mT4MzPDd2MUC3OC=>
T98G NEDaTZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\WUVIxKM7:TR?= MkjmO|IhcA>? M{TZbGROW09? NGq5[|ZKSzVyPEWg{txO M1XxNVI1PzRzMEe0
U87 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCxW2JyOjBizszN NETB[Wg4OiCq NYjaXFF6TE2VTx?= MWDJR|UxRDVizszN NHXIcI0zPDd2MUC3OC=>
LN18 NETsSnJHfW6ldHnvckBCe3OjeR?= NFu5Z|g2KM7:TR?= MUSyOEBp MV;EUXNQ MYjJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV M1HNSlI1PzRzMEe0
LNZ308 NHLQZZpHfW6ldHnvckBCe3OjeR?= MmP0OUDPxE1? MUWyOEBp M3raUWROW09? M4e1WmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1R? NGXh[W8zPDd2MUC3OC=>
Saos-2 NU\6[G5wTnWwY4Tpc44hSXO|YYm= NVS2[XRZPTBizszN M{LERVQ5KGh? MUHJcohq[mm2czDj[YxtKGmwdnHzbY9v NUXTRoFOOjR5Mke2OlA>
MG-63 M{P6WmZ2dmO2aX;uJGF{e2G7 NVO0c3I1PTBizszN NFv5PXk1QCCq MYrJcohq[mm2czDj[YxtKGmwdnHzbY9v NXzvUYdROjR5Mke2OlA>
SJSA-1 MlLpSpVv[3Srb36gRZN{[Xl? NH7nRXA2OCEQvF2= NUTZXWVSPDhiaB?= Mk\LTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? NGfnWlEzPDd{N{[2NC=>
Saos-2 NF2zR45HfW6ldHnvckBCe3OjeR?= M{PEU|UxKM7:TR?= MUm0PEBp MVXJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u MViyOFczPzZ4MB?=
MG-63 MWHGeY5kfGmxbjDBd5NigQ>? MUK1NEDPxE1? M1ezbFQ5KGh? NYnmb3hLUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MYmyOFczPzZ4MB?=
SJSA-1 NEDjdYRHfW6ldHnvckBCe3OjeR?= M2LP[|UxKM7:TR?= MXq0PEBp NF3lV4NKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v M1H5cVI1PzJ5Nk[w
Saos-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYS1NEDPxE1? NXr4W5VPPDhiaB?= M{D2Z2lvcGmkaYTzJINmdGxidnnhZoltcXS7 MUGyOFczPzZ4MB?=
MG-63 M{jsNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnVdFM2OCEQvF2= MmTMOFghcA>? MlPRTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? NYXBSJpvOjR5Mke2OlA>
SJSA-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT4bHM2OCEQvF2= M{nsSlQ5KGh? NEjiUWdKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= M1G2dFI1PzJ5Nk[w
FaDu MXXGeY5kfGmxbjDBd5NigQ>? NFywWWk2KM7:TR?= MmnPNlQhcA>? M{LzSGROW09? MVLS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= Mm\QNlQ3OzFzNEe=
EMT6 NEDwRpNHfW6ldHnvckBCe3OjeR?= NUC4W3RJPSEQvF2= NVHqWXFPOjRiaB?= NWL5O3lXTE2VTx?= NGDmSGNT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> MV:yOFY{OTF2Nx?=
HCT116 Mmr2SpVv[3Srb36gRZN{[Xl? MXy1JO69VQ>? MmrENlQhcA>? NF62[XZFVVOR NGjEWmVT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NULVdJhwOjR4M{GxOFc>
U87 NEHtcI5HfW6ldHnvckBCe3OjeR?= NWXwSWljPSEQvF2= MYiyOEBp MnrWSG1UVw>? NXXIb3B{WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NFvBWmwzPDZ|MUG0Oy=>
GBM M{jDSGFxd3C2b4Ppd{BCe3OjeR?= NV;0OlFZOs7:TR?= NXrVU5Y3PDiq MmjQSG1UVw>? NYT5cGdycW6mdXPl[EBpcWeqZYKgcIV3\Wy|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>? MkHYNlQ2ODB2OUK=
BON MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmxMVXPxE1? NX7jTnpVPzKq NXzNU4Nk\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NGPORpIzPDR2M{WyNy=>
BON NX34bJJNSXCxcITvd4l{KEG|c3H5 MWKxMVXPxE1? MUWyOIg> NFHQPHVqdmO{ZXHz[ZMh[XCxcITvd4l{ MX2yOFQ1OzV{Mx?=
H1975 Ml7wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvpe4MxNjNvOT62{txO NYfO[2tTPzKq MlziSG1UVw>? NELrUYFKSzVyPUGuN|g2|ryP MYqyOFM{Pzh2Nh?=
H1975 M2\w[WFxd3C2b4Ppd{BCe3OjeR?= NGri[IMz|ryP MYSyOIg> MlL5SG1UVw>? M3fZb4lv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 NWrxZ3FpOjR|M{e4OFY>
T-ALL NGP2cWJCeG:ydH;zbZMhSXO|YYm= MYPi[ZR4\WWwIEGuOEBidmRiNT6zJI1OKGG2IEK0bEBidmRiMD65JIFv\CB3LkWgcW0h[XRiNEjoJIlvKGSrZn\ldoVvfCClZXzsJIxqdmV? M{\4[FI1KG:{IES4bC=> NGrJN41FVVOR M2DNPIFn\mWldIOgeIhmKFCLM1ugdIF1cHejeTDpckBVNUGOTDDj[YxtKGyrbnXz MlizNlQ{OTB5M{[=
BCR-ABL NGnVWWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\TO|AvOjVvMUFOwG0> M2\wblRl MVrzbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v MWOyOFI1PDZzMh?=
LC-1/SQSF NF3CbWpHfW6ldHnvckBCe3OjeR?= NFrKbnA{|ryP NGSyRW4zPGh? M1\iTGROW09? M1vDZYRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> NHv5coozOzl6MEC5Ny=>
Primary CLL cells MYnBdI9xfG:|aYOgRZN{[Xl? MmO3NU0yOM7:TR?= MmDvOFhp MljqbY5lfWOnczDhdI9xfG:|aYOgbY4hS0yOIHPlcIx{KGmwZHXw[Y5l\W62IH;mJJBzd2ewb4P0bYMhdWG{a3Xydy=> NE\oZZUzOzh3MEiwOy=>
Primary CLL cells Ml;iT4lv[XOnIFHzd4F6 NEL4UZgz|ryP NHfacmI{OG2rbh?= NUTwdVFY\GWlcnXhd4VlKFCLM1ugZYN1cX[rdIm= MV[yN|g2ODhyNx?=
Primary CLL cells Mn7XR5l1d3SxeHnjJGF{e2G7 M3TFOlLPxE1? NXywZ5VJOjSq M4r5SYlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MmTLNlM5PTB6MEe=
human NSCLC cell lines NH3jbJZCeG:ydH;zbZMhSXO|YYm= MVGwMlEzPS12zszN M{XGNFI1cA>? MmfsSG1UVw>? MlL2TWM2OHNicnHu[4V{KG[{b32gNE41NTMQvF2= NHPVN28zOzV4MkS3Ni=>
human HCC cell lines Mn[3R4VtdCC4aXHibYxqfHliYYPzZZk> NV;jS4ZrOC5yMEWtNe69VQ>? NF;NU241QGh? NY\zbYlyUUN3ME2x{txO MoHwNlM1QDl7OUm=
Huh7 Ml;PT4lv[XOnIFHzd4F6 M1noOVHPxE1? MXq0PIg> M4rtUJNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> M4PnN|I{PDh7OUm5
SK-HEP1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHmN5oyNTJyzszN NGDnNo04Omh? M4\0[WROW09? NEjF[2pKSzVy78{cNe69VQ>? M2\sXlI{PDd7MUO2
786-0 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXUNU0zOM7:TR?= MnXTO|Jp MmnZSG1UVw>? NIrVXXBKSzVy78{cNe69VQ>? MorsNlM1PzlzM{[=
JVM2 NV;OSFFpS3m2b4TvfIlkcXS7IHHzd4F6 NH3lNWIxNjJvMkFOwG0> M1TiOlczcA>? M37zUmROW09? NYrWUVYzUUN3ME2wMlnPxE1? MlrHNlMzOzh4M{m=
EHEB Ml73R5l1d3SxeHnjbZR6KGG|c3H5 MV6wMlIuOjEQvF2= MoPnO|Jp NFvwUHBFVVOR MlP0TWM2OD1yLkhOwG0> NYmxZ3hHOjN{M{i2N|k>
MEC2 M3;qV2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmTBNE4zNTJyzszN M{TVc|czcA>? NEPjdnhFVVOR M4LVVGlEPTB;MD63{txO MmT0NlMzOzh4M{m=
primary B-CLL lymphocytes MnPTRZBweHSxc3nzJGF{e2G7 Mny4TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? MX[yOIg> MUnEUXNQ NVnKTlZ7UUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? NGjTV|YzOzJ|OE[zPS=>
primary B-CLL lymphocytes MnTnT4lv[XOnIFHzd4F6 MmTtTWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? M3\1UFI1cA>? MVTpcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= NX3LemRCOjN{M{i2N|k>
human NSCLC NImyb|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKwMlUuOs7:TR?= MnW5O|Jp NFTZTYJKSzVyPUJOwG0> MlLBNlI4QDF|OUO=
human NSCLC MoG4T4lv[XOnIFHzd4F6 NVTXPFVFOc7:TR?= NH7lSmozPGh? M{G4cYlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= MmOxNlI4QDF|OUO=
Y1 cell line NVXr[JM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu1NE4y|ryPL{JOwG0> NV\HTm5tOjSq NWnXd|dSTE2VTx?= NVvwbphJcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= NFX5OIozOjZ7MkmwOC=>
PIK3CA-mutant MCF7 NInQbVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;kS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? MkjXO|Jp M4D3R2dKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P NHHk[JEzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 NXPQdGMyU2mwYYPlJGF{e2G7 NVrDO5ZsUUN3ME2xNVTDuTOwTR?= NFTme2c4Omh? MVXJR|UxRTFzNNMxN45OKGmwIILl[JVkcW6pIFHreEBxcG:|cHjvdplt[XSrb36gcIV3\Wy| MlH2NlI3PTN7Nke=
MCF7-myr-Akt MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TnSGdKPTB;Mkm5xtE3QG6P78{MUGQ2OO,:nkGwMFAxOG6P NHzxRm44Omh? NWTmOIlNT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= M4e4XFIzPjV|OU[3
colon cancer cell lines NFL5V3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;MSYUxNTFyzszN MnX3O|Jp M3ftT2ROW09? MkL3TWM2OD1zzszN NH;vcVIzOjV2M{i1Oy=>
gastric cancer cell lines M2nhNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuwMVEx|ryP Mn\1O|Jp MnPVSG1UVw>? MlTOTWM2OD1{LUZOwG0> MoDpNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 NFPyWHBCeG:ydH;zbZMhSXO|YYm= MknTNu69VQ>? MmnlOFhp NVjuVppre2irZoSgbY4hTzJicHjhd4U> MnfHNlI2PDN6NUe=
HT-29 and HCT-116 M1LRNWNie3Cjc3WgZZN{[Xl? M1PzOlXPxE1? NYrZNVZiOjSq MVjpcoR2[2W|IHPhd5Bie2ViYXP0bZZqfHl? NVfXXJc4OjJ3NEO4OVc>
MM cell lines MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPkZlFkOTEQvF2= NYfOPXhzOjSq NHX2RpZFVVOR M4ny[GlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? M1S4T|IzOjB5NEi1
ARP-1 M2X6c2Fxd3C2b4Ppd{BCe3OjeR?= M1LpVFEx|ryP M2HTZ|I1cA>? NFvJVZlFVVOR NYPX[o9rcW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> NYPOZlhwOjJ{MEe0PFU>
SNU-601 M2HBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfCO|Jp NUXjW45wTE2VTx?= NVXCUpdwUUN3ME2wMlgyPsLzMD6wOlPPxE1? NHGwPG8zOjF3OUixOC=>
SNU-1 NVfhd4xVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1iycVczcA>? NUHFVoR[TE2VTx?= NH\uUXFKSzVyPUGuNFgzyrFyLkCyPO69VQ>? MoLKNlIyPTl6MUS=
SNU-668 NG[xeIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jGN|czcA>? NHzPRXFFVVOR NXr1VY8yUUN3ME2xMlU4QcLzMD6wO|TPxE1? M3nSUFIzOTV7OEG0
AGS NHu3U2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[3Nog> MXzEUXNQ MlX2TWM2OD1zLkexOOKyOC5zMUhOwG0> M17BS|IzOTV7OEG0
SNU-216 NGXEbYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUK3Nog> MnjxSG1UVw>? MmXiTWM2OD1{Lk[5NuKyOC5yOENOwG0> NUD6VZBVOjJzNUm4NVQ>
SNU-5 NEexclNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHafI84Omh? NUPM[49jTE2VTx?= NGHSVIxKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? NGrIT4gzOjF3OUixOC=>
SNU-638 M{HOemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPWO|Jp MYnEUXNQ NHrNPXFKSzVyPUKuNlgzyrFyLkC1N:69VQ>? M2TsNFIzOTV7OEG0
SNU-16 NGDMZolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHm0bmw4Omh? NF\wb5ZFVVOR NWrGe2ZZUUN3ME2xMlU4O8LzMD6wNFHPxE1? NYfPUmFROjJzNUm4NVQ>
SNU-484 NX;zSFU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljuO|Jp MkjSSG1UVw>? MV\JR|UxRTFwN{K4xtExNjB2Nd88US=> Ml3iNlIyPTl6MUS=
SNU-620 NFH5OIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13aTVczcA>? NV3mOVR5TE2VTx?= NIfsUVVKSzVyPUKuPVM6yrFyLkCwNe69VQ>? NEDofmszOjF3OUixOC=>
SNU-719 NITGVWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzqO|Jp MkWxSG1UVw>? NIW5WmxKSzVyPUOuNFM4yrFyLkCzNu69VQ>? MWSyNlE2QThzNB?=
glioma cell lines MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXHVXg4Omh? NETFOYtKSzVyPUGtNu69VQ>? M37mclIzODZ3MEiw
U87 Mk[4RZBweHSxc3nzJGF{e2G7 NHHEfJkz|ryP NFfoRVY4Omh? MmrjbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= M{HvUlIzODZ3MEiw

... 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