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 MmL4R5l1d3SxeHnjJGF{e2G7 MmmwO|IhcA>? NIXFbldFVVOR NEC4XJlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGW6cILld5NqdmdiUFmzT4FteGijIFW1OFVMKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFAyPThizszN NG[wemQzPDlyMEK2Oi=>
DU145 MX\DfZRwfG:6aXOgRZN{[Xl? NIC5WFU4OiCq MX3EUXNQ NV3TblhSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiZYjwdoV{e2mwZzDMT2IyKG23dHHueEB4cXSqIFfJOVAhd2ZiMD6wNFA1OzVizszN NYjrSohYOjR7MECyOlY>
A2780 NFvTSJhEgXSxdH;4bYMhSXO|YYm= MkfSO|IhcA>? NYK0NYNrTE2VTx?= NXXkR3FRS3m2b4TvfIlkcXS7IHHnZYlve3RiUGTFUk1l\W[rY3nlcpQhcHWvYX6gRVI4QDBiY3XscJMhf2m2aDDHTVUxKG:oIECuNFAxPjN3IN88US=> M3LTWFI1QTByMk[2
U87MG MWnDfZRwfG:6aXOgRZN{[Xl? NXfOdFhPPzJiaB?= MoLySG1UVw>? M2XKTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY6QCEQvF2= NVzC[5pGOjR7MECyOlY>
A2780 MUXGeY5kfGmxbjDBd5NigQ>? M1r4SFEhcA>? MV\EUXNQ MUTJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36ge4l1cCCHQ{WwJI9nKDBwMEW1JO69VQ>? M1TzS|I1QTByMk[2
DU145 NE\Z[mZHfW6ldHnvckBCe3OjeR?= NU[4UnJsOSCq NVrTTXZkTE2VTx?= NFexTmlKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR|UxKG:oIECuNFc{KM7:TR?= NUnHS2JROjR7MECyOlY>
A2780 NWDXVIlSTnWwY4Tpc44hSXO|YYm= MlTlNUBp M1TWSWROW09? NUTnbHhYUW6qaXLpeIlwdiCxZjDQTVNMNW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGmwIGDUSW4u\GWoaXPp[Y51KGi3bXHuJGEzPzhyIHPlcIx{KHerdHigSWM2OCCxZjCwMlA4PCEQvF2= NHmzO3ozPDlyMEK2Oi=>
MCF7 M{TtN2Z2dmO2aX;uJGF{e2G7 M3\ENFEhcA>? NYDUdJU3TE2VTx?= Mnj5TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiRUW0OWshdXW2YX70MY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkGg{txO NWSzOXpwOjR7MECyOlY>
U87MG NW\nc2pzTnWwY4Tpc44hSXO|YYm= M2no[FEhcA>? MX3EUXNQ NIe4cmdKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP MYeyOFkxODJ4Nh?=
A2780 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHhO|IhcA>? MX3EUXNQ MUfFR|UxRTBwNUKg{txO MWmyOFkxODJ4Nh?=
SKMES-1 NV\wWJR{S3m2b4TvfIlkKEG|c3H5 MWOxJO69VQ>? M3;KfFczKGh? NHnxRZFKdmS3Y3XzJINmdGxiZHXheIg> MlK4NlYxOTN|MUi=
H596 NVrje452TnWwY4Tpc44hSXO|YYm= NETPb4wyKM7:TR?= MWXJcZBicXK|IHPlcIwhdWmpcnH0bY9v MlzNNlYxOTN|MUi=
HCC2450 M4XFSmZ2dmO2aX;uJGF{e2G7 MWexJO69VQ>? M1zRWWlueGGrcoOgZ4VtdCCrbo\hd4lwdg>? NFvl[nkzPjBzM{OxPC=>
A549 NIfMdIlHfW6ldHnvckBCe3OjeR?= NHHSdGU2ODBibl2= M2\jclQ5KGh? MXfEUXNQ MYnJcohq[mm2czDBb5Qh[WO2aY\heIlwdg>? NIKzPWwzPTl|N{K5PS=>
A549 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTxclI2OSEQvF2= M3jrcVczKGh? Mn;3SG1UVw>? NU\rR3drUW6qaXLpeJMh[2WubDDndo94fGh? M3\Z[FI2QTN5Mkm5
H522 MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH32e|UyKM7:TR?= MoTCO|IhcA>? M2rjRWROW09? NIL0UoZKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NVfXdVBEOjV7M{eyPVk>
LNCaP M1\MRWZ2dmO2aX;uJGF{e2G7 MknkNUDPxE1? MoC0V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? NEjLbHkzPTN4MEe5PS=>
LNCaP95 MnjFSpVv[3Srb36gRZN{[Xl? MWSxJO69VQ>? MmjxV5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? MXSyOVM3ODd7OR?=
HCT-15 MmT4RZBwfG:|aYOgRZN{[Xl? NUjH[plROTBizszN NIDDfmg1QCCq M1npdGROW09? NHWwc2pKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVUh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= MVKyOVE2OjJ2NR?=
HCT-116 NX\EbG1KSXCxdH;zbZMhSXO|YYm= MYOxNEDPxE1? MofWOFghcA>? NV3lZVAxTE2VTx?= NFn4S4dKdmS3Y3XzJIFxd3C2b4Ppd{BqdiCKQ2StNVE3KGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NV\QflJoOjVzNUKyOFU>
NCI-H460 M4\NdWFxd3Sxc3nzJGF{e2G7 MVWxNEDPxE1? MXm0PEBp MWjEUXNQ NXjVSXhpUW6mdXPld{BieG:ydH;zbZMhcW5iTlPJMWg1PjBiY3XscJMhcGG{Yn;1dolv\yCSSVuzR2EhcG:2c4DveEBufXSjdHnvci=> NF3XSY4zPTF3MkK0OS=>
SKOV-3 NYjkW|VJSXCxdH;zbZMhSXO|YYm= M{D3OVExKM7:TR?= NUW4RpZtPDhiaB?= MUTEUXNQ M1e3d2lv\HWlZYOgZZBweHSxc3nzJIlvKFONT2[tN{Bk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NHfaNVUzPTF3MkK0OS=>
BSY-1 MlW0RZBwfG:|aYOgRZN{[Xl? NXzSTnBVOTBizszN M4W4S|Q5KGh? NF3PeHZFVVOR MU\JcoR2[2W|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NITmeVczPTF3MkK0OS=>
MKN-1 NWnkUJhsSXCxdH;zbZMhSXO|YYm= MYGxNEDPxE1? MkToOFghcA>? M2nwNGROW09? MonaTY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NVXMO4h6OjVzNUKyOFU>
NCI-H522 Ml3HRZBwfG:|aYOgRZN{[Xl? MXqxNEDPxE1? M3;aOVQ5KGh? NV;y[YRDTE2VTx?= MXXJcoR2[2W|IHHwc5B1d3Orcx?= NGfNPHkzPTF3MkK0OS=>
OVCAR-3 MXTBdI91d3OrczDBd5NigQ>? MmDGNVAh|ryP NV6xOJc1PDhiaB?= M33ydGROW09? MnLrTY5lfWOnczDhdI9xfG:|aYO= MUOyOVE2OjJ2NR?=
HBC-5 NIn5clhCeG:2b4Ppd{BCe3OjeR?= MX:xNEDPxE1? MVG0PEBp MVPEUXNQ NFnS[m1KdmS3Y3XzJIFxd3C2b4Ppdy=> MV[yOVE2OjJ2NR?=
RXF-631L NELhNWVCeG:2b4Ppd{BCe3OjeR?= MoTmNVAh|ryP M2\YOFQ5KGh? MX7EUXNQ M4LjW2lv\HWlZYOgZZBweHSxc3nz NU\G[3BtOjVzNUKyOFU>
MKN-45 NVnvXHhCSXCxdH;zbZMhSXO|YYm= NVXL[nU{OTBizszN NUi0OJFWPDhiaB?= NG\O[olFVVOR MWfJcoR2[2W|IHHwc5B1d3Orcx?= Mn2wNlUyPTJ{NEW=
BON-1 Mmq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nDT|UxOCCwTR?= NV7jZZB4OTBiZB?= MUPEUXNQ Ml3tTY5pcWKrdIOgZ4VtdCCpcn;3eIg> NX\LeVc3OjVyMk[yPVI>
BON-1 MlPjSpVv[3Srb36gRZN{[Xl? NXPmNXJiPTByIH7N MlnUOEBp M{XXbGROW09? MnjjTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= MVqyOVAzPjJ7Mh?=
QGP-1 Mly5SpVv[3Srb36gRZN{[Xl? NXzPcI44PTByIH7N NGjjcog1KGh? NFjzW2JFVVOR MWXJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtVKGG2IGTodlMxQCCjbnSgV4VzPDd| M1nxVFI2ODJ4Mkmy
Huh7 MXfGeY5kfGmxbjDBd5NigQ>? Mn3xNUDPxE1? NHXZeYUyKGh? NWPN[2dHTE2VTx?= NWPUNFF4UW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBU\XJ2N{S= NXj0dIs5OjVyMES0NFM>
BNL Mm\TSpVv[3Srb36gRZN{[Xl? NVPXWG5tOSEQvF2= MnG2NUBp NVvZZpJmTE2VTx?= MnHBTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJHM3 NFT0RngzPTByNESwNy=>
MDA-MB-175 NInReI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjiZW17OSEQvF2= Mn3VOUBl NWHKPIJyTE2VTx?= Mn7rTWM2ODxzIN88US=> NYToSXNyOjR6N{m3PVY>
MDA-MB-134 NVPG[XZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;t[FEh|ryP MWq1JIQ> MWXEUXNQ M3jaOWlEPTB:MTFOwG0> NWHtSINLOjR6N{m3PVY>
HCC1500 NUizVGtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVKxJO69VQ>? NWPGW|VVPSCm MYjEUXNQ NUn1N2pOUUN3MEyxJO69VQ>? MmnRNlQ5Pzl5OU[=
EFM-19 NUfBT4doT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HWd|Eh|ryP NEPQR3A2KGR? NX7QUmlVTE2VTx?= MUnJR|UxRDFizszN NIiyVHEzPDh5OUe5Oi=>
ZR-75-30 M3Kzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjTXnpIOSEQvF2= M3jtT|Uh\A>? NUeybmVnTE2VTx?= NXPCSYk3UUN3MEyxJO69VQ>? M3fmdVI1QDd7N{m2
MDA-MB-361 M4jKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjDXYIyKM7:TR?= NWj3b2FMPSCm M4TyfmROW09? MmDZTWM2ODxzIN88US=> NED2fnAzPDh5OUe5Oi=>
T-47D MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUexJO69VQ>? MUS1JIQ> NH3TWGpFVVOR NFH0NIFKSzVyPEGg{txO NITxdIMzPDh5OUe5Oi=>
SK-BR-3 NInlelZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mke4NUDPxE1? MYK1JIQ> MYXEUXNQ MkjJTWM2ODxzIN88US=> NHLVdoozPDh5OUe5Oi=>
UACC-732 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn74NUDPxE1? MWe1JIQ> MVfEUXNQ NYLiUI5{UUN3MEyxJO69VQ>? MYSyOFg4QTd7Nh?=
BT-474 NH7vUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2xJO69VQ>? MUS1JIQ> MlKwSG1UVw>? NUX4Rpl5UUN3MEyxJO69VQ>? MlrRNlQ5Pzl5OU[=
HCC202 M2TDTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGOxOpIyKM7:TR?= NYHkVXZtPSCm MmnMSG1UVw>? NUfsXJZKUUN3MEyxJO69VQ>? NXTofJVkOjR6N{m3PVY>
MCF7 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXLNUDPxE1? NFK3dno2KGR? NF\oZ5FFVVOR M4riVGlEPTB:MTFOwG0> M2fHd|I1QDd7N{m2
MDA-MB-415 M3rWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTnRYwyKM7:TR?= M3TWelUh\A>? NY\IUlNITE2VTx?= MUXJR|UxRDFizszN M3XTWFI1QDd7N{m2
MDA-MB-453 M2nhN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2W3W|Eh|ryP M3nYbVUh\A>? MWDEUXNQ M4fCSmlEPTB:MTFOwG0> NUGwNXVzOjR6N{m3PVY>
ZR-75-1 Mn\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ixVlEh|ryP NFXPPYo2KGR? NGrLXXVFVVOR NUPSbGdRUUN3MEyxJO69VQ>? M3THdFI1QDd7N{m2
HCC38 NGDEc2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\zVVEh|ryP NVPYdXJ[PSCm NXTxfXFnTE2VTx?= NXrsSYNbUUN3MEyxJO69VQ>? MmmwNlQ5Pzl5OU[=
HCC1419 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzhb4E6OSEQvF2= MUi1JIQ> NYfQWZRRTE2VTx?= NWWybllEUUN3MEyxJO69VQ>? NI[3[o4zPDh5OUe5Oi=>
UACC-812 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzPNUDPxE1? MU[1JIQ> MmntSG1UVw>? NW\Jc2NzUUN3MEyxJO69VQ>? NYW2b2VIOjR6N{m3PVY>
HCC1187 M{[2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFL3fZkyKM7:TR?= MYK1JIQ> NEXwe2JFVVOR MojlTWM2ODxzIN88US=> M1uxXlI1QDd7N{m2
KPL-1 M3K5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfPSZRLOSEQvF2= M{H4OVUh\A>? NIm0SYZFVVOR MojpTWM2ODxzIN88US=> NHj1VYozPDh5OUe5Oi=>
SUM-225 MlHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jXNFEh|ryP NXHyU5ZQPSCm MW\EUXNQ NInrO2RKSzVyPEGg{txO MVyyOFg4QTd7Nh?=
EFM-192A Mo\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[1e|Eh|ryP M{[xVlUh\A>? NVXY[2FqTE2VTx?= NHGxcG1KSzVyPEGg{txO NE\w[o0zPDh5OUe5Oi=>
JIMT-1 M1\rT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxJO69VQ>? M3S0eFUh\A>? NV[xN5ZlTE2VTx?= M3;wTWlEPTB:MTFOwG0> M1v4WlI1QDd7N{m2
HCC1143 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPMeY9[OSEQvF2= M3:4ZlUh\A>? MoPBSG1UVw>? M{f4fWlEPTB:MTFOwG0> M1PvclI1QDd7N{m2
HCC2218 NYfWXYs2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HaNFEh|ryP M3TLbFUh\A>? M{PnW2ROW09? MkGxTWM2ODxzIN88US=> MXWyOFg4QTd7Nh?=
MDA-MB-468 NHTQ[HBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnZ[G1xOSEQvF2= NV;Te|lvPSCm MmftSG1UVw>? NVzsd5dQUUN3MEyxJO69VQ>? MXyyOFg4QTd7Nh?=
BT-20 MorjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnQNUDPxE1? NEHOVos2KGR? NHzGN25FVVOR NH3oU41KSzVyPEGg{txO NGfvVJAzPDh5OUe5Oi=>
MDA-MB-435 MlvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XnflEh|ryP NWL4Wm1iPSCm MnPTSG1UVw>? M2rCOGlEPTB:MTFOwG0> NHLNb3EzPDh5OUe5Oi=>
BT-549 M37mTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LSOFEh|ryP MXO1JIQ> NWC3SohMTE2VTx?= MnHoTWM2ODxzIN88US=> NWX4TmU5OjR6N{m3PVY>
HCC1806 NUjldnJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\S[|Eh|ryP MlvlOUBl NV7h[VRNTE2VTx?= MkDxTWM2ODxzIN88US=> NETEeWszPDh5OUe5Oi=>
HCC1937 NEfDR5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUD6cotLOSEQvF2= MYe1JIQ> M1PBNGROW09? NIXtOItKSzVyPEGg{txO M4D1NVI1QDd7N{m2
Hs578T MmLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe0T2kyKM7:TR?= MYq1JIQ> NVyyRlJMTE2VTx?= NGXxfJBKSzVyPEGg{txO M2C5eVI1QDd7N{m2
LN18 NFHYPWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\ENlAh|ryP NVPlUGZFPzJiaB?= NIm2bGxFVVOR MXXJR|UxRDVizszN NV3yU|FGOjR5NEGwO|Q>
LN229 NEW0OYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvUd4IzOCEQvF2= M3fxZ|czKGh? MWjEUXNQ Mn3GTWM2ODx3IN88US=> MkXwNlQ4PDFyN{S=
LNZ308 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml6xNlAh|ryP MWq3NkBp MU\EUXNQ M3\6T2lEPTB:NTFOwG0> NF;3cngzPDd2MUC3OC=>
T98G NILQSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjs[HhvOjBizszN NIi1OIQ4OiCq NULSXWNyTE2VTx?= MkjlTWM2ODx3IN88US=> M4iz[|I1PzRzMEe0
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MG-63 NVjHN21NTnWwY4Tpc44hSXO|YYm= Ml73OVAh|ryP NWW4O3A4PDhiaB?= NVHWcJI1UW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MoLNNlQ4Ojd4NkC=
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Saos-2 NFzuZ|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TXXlUxKM7:TR?= NWTDbpNDPDhiaB?= MoXHTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? NHmwUXUzPDd{N{[2NC=>
MG-63 NHS4OYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXyeG1xPTBizszN Mn3wOFghcA>? NHfzUnpKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= MV6yOFczPzZ4MB?=
SJSA-1 NH;FR3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHUOIVtPTBizszN MV20PEBp M3\5NmlvcGmkaYTzJINmdGxidnnhZoltcXS7 MUKyOFczPzZ4MB?=
FaDu Mof2SpVv[3Srb36gRZN{[Xl? NUPtTlJHPSEQvF2= NIfFZXYzPCCq MlnJSG1UVw>? MUfS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MWKyOFY{OTF2Nx?=
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HCT116 NFf1Wm1HfW6ldHnvckBCe3OjeR?= NIXCfG42KM7:TR?= NH7INYUzPCCq MX7EUXNQ MYnS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= MlP2NlQ3OzFzNEe=
U87 MnTrSpVv[3Srb36gRZN{[Xl? NXr6VW5KPSEQvF2= M{TOUVI1KGh? MnHhSG1UVw>? NVn2OYdnWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NEjHPVQzPDZ|MUG0Oy=>
GBM Mn\pRZBweHSxc3nzJGF{e2G7 M2G2bFLPxE1? M3WzbFQ5cA>? NX3OW3FUTE2VTx?= NYrWbYFXcW6mdXPl[EBpcWeqZYKgcIV3\Wy|IH;mJIFxd3C2b4Ppd{wh[W6mIHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gQ>? M4rOdlI1PTByNEmy
BON NFLidGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDoXpptOS13zszN MUK3Nog> MYfk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u NWfafm9POjR2NEO1NlM>
BON MljhRZBweHSxc3nzJGF{e2G7 MlHDNU02|ryP MXKyOIg> MkXTbY5kemWjc3XzJIFxd3C2b4Ppdy=> NV7kWmNYOjR2NEO1NlM>
H1975 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPXR2MxNjNvOT62{txO M4LyO|czcA>? MYjEUXNQ NV:4U5ZrUUN3ME2xMlM5Pc7:TR?= NETrTWgzPDN|N{i0Oi=>
H1975 Mn7ZRZBweHSxc3nzJGF{e2G7 NEXnc44z|ryP M3H6TFI1cA>? MWnEUXNQ M1Lq[Ylv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 M3XKWVI1OzN5OES2
T-ALL MYLBdI9xfG:|aYOgRZN{[Xl? NX3Fe2VP[mW2d3XlckAyNjRiYX7kJFUvOyCvTTDheEAzPGhiYX7kJFAvQSCjbnSgOU42KG2PIHH0JFQ5cCCrbjDkbYZn\XKnboSgZ4VtdCCuaX7l MYSyOEBweiB2OHi= MojpSG1UVw>? MUjh[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= Mk\wNlQ{OTB5M{[=
BCR-ABL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS1bVJGOC5{NT2xNO69VQ>? NGWyVnI1\A>? NV3ON5VQe2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= M3LaR|I1OjR2NkGy
LC-1/SQSF NXHqXZlVTnWwY4Tpc44hSXO|YYm= NEm4c4g{|ryP NYDZOmxQOjSq NUnl[4dHTE2VTx?= M2DGb4Rm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> MViyN|k5ODB7Mx?=
Primary CLL cells NHj3U2FCeG:ydH;zbZMhSXO|YYm= NVfWSY5EOS1zMN88US=> NXv1cG9MPDiq NXLOPHBbcW6mdXPld{BieG:ydH;zbZMhcW5iQ1zMJINmdGy|IHnu[IVx\W6mZX70JI9nKHC{b3fuc5N1cWNibXHyb4Vzew>? NVHHPYJxOjN6NUC4NFc>
Primary CLL cells NV73fYR3U2mwYYPlJGF{e2G7 NXfVXY45Os7:TR?= MnzvN|BucW5? MVvk[YNz\WG|ZXSgVGk{UyCjY4Tpeol1gQ>? M1vIXlI{QDVyOEC3
Primary CLL cells NFL0cHhEgXSxdH;4bYMhSXO|YYm= NFXndXcz|ryP MkCzNlRp M4r3Volv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= NF7rfJQzOzh3MEiwOy=>
human NSCLC cell lines NGjyXY1CeG:ydH;zbZMhSXO|YYm= NYS1fHk{OC5zMkWtOO69VQ>? M2T4blI1cA>? NUn0eXhjTE2VTx?= NF7BdoRKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> NFfnUpUzOzV4MkS3Ni=>
human HCC cell lines NYHMb2tqS2WubDD2bYFjcWyrdImgZZN{[Xl? M2fpdlAvODB3LUJOwG0> MmC3OFhp M{XY[GlEPTB;Md88US=> NEjnUpgzOzR6OUm5PS=>
Huh7 M1\2XWtqdmG|ZTDBd5NigQ>? NH7IWnAy|ryP NIXLUnY1QGh? MYHzbYdvce,ugXPhcpRtgSC{ZXT1Z4V{KHCqb4PwbI9zgWyjdHnvckBw\iCDa4S= NYraOXR4OjN2OEm5PVk>
SK-HEP1 NYTNSXl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxMVIx|ryP NFP2NIk4Omh? NED5cmNFVVOR M2C3TWlEPTExvKyx{txO NHH6U|MzOzR5OUGzOi=>
786-0 NWKyZ5lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjnOpkyNTJyzszN M1KzNlczcA>? M{DCVWROW09? MkW1TWM2OO,:nEJOwG0> M3[zXFI{PDd7MUO2
JVM2 M1fOSGN6fG:2b4jpZ4l1gSCjc4PhfS=> NYnyOnplOC5{LUKw{txO MlLFO|Jp MlWySG1UVw>? MkXNTWM2OD1yLkpOwG0> NIfjVlMzOzJ|OE[zPS=>
EHEB MXHDfZRwfG:6aXPpeJkh[XO|YYm= M{f5NFAvOi1{MN88US=> NF22OJE4Omh? MV\EUXNQ MU\JR|UxRTBwN988US=> NWHkfVNwOjN{M{i2N|k>
MEC2 MYDDfZRwfG:6aXPpeJkh[XO|YYm= MVKwMlIuOjEQvF2= M1HDb|czcA>? NH7BflVFVVOR NV;nfYJlUUN3ME2wMlfPxE1? M{jHblI{OjN6NkO5
primary B-CLL lymphocytes M3;HO2Fxd3C2b4Ppd{BCe3OjeR?= NHPHVGRKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n Mm[4NlRp NVOzWmZ5TE2VTx?= NUDuV2JmUUN3MP-8oFPPxE1iZn;yJIFtdCCyYYTp[Y51ew>? MY[yN|I{QDZ|OR?=
primary B-CLL lymphocytes MWfLbY5ie2ViQYPzZZk> NEjKRYpKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n MVmyOIg> MYTpcohq[mm2czDwO|BUPktiJjC0SU1DWDFiZYjwdoV{e2mxbh?= NV36b41pOjN{M{i2N|k>
human NSCLC NGPiUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHCNE42NTMQvF2= NXvReIFNPzKq M3Xzb2lEPTB;Md88US=> NXzxcI5IOjJ5OEGzPVM>
human NSCLC NVvWW|g5U2mwYYPlJGF{e2G7 NYi1eG9vOc7:TR?= MoHJNlRp NUnaPG9TcW6qaXLpeJMhfGinIFHreE9uXE:UIIPp[45idGmwZzDwZZRpf2G7IHH0JFNpKGGodHXyJJRz\WG2bXXueC=> MlfSNlI4QDF|OUO=
Y1 cell line MonPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\5PFAvOc7:TT:x{txO MV6yOIg> MlzBSG1UVw>? NV[zTlhHcW6qaXLpeJMhPjExvJWgZ4VtdCC4aXHibYxqfHliaX6gUZlkNVOldIKteJJidnOoZXP0[YQh[2WubIO= MlrmNlI3QTJ7MES=
PIK3CA-mutant MCF7 MmX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3uwOGdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P MkPtO|Jp MkPZS2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? NHixO2kzOjZ3M{m2Oy=>
PIK3CA-mutant MCF7 NV7PN2VnU2mwYYPlJGF{e2G7 NHezd|BKSzVyPUGxOOKyO26P MYC3Nog> NYG4b3BWUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=> M3TGVlIzPjV|OU[3
MCF7-myr-Akt M1rucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHPVFJIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= M{LoNVczcA>? NYq2WJlYT0l3ME2yPVnDuTZ6bl5vwKxNTDVy78{eNVAtODBybl2= MXKyNlY2Ozl4Nx?=
colon cancer cell lines MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTjNE0yOM7:TR?= NWPubHk1PzKq MlP5SG1UVw>? MYXJR|UxRTIQvF2= MXKyNlU1Ozh3Nx?=
gastric cancer cell lines MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfhUmV[OC1zMN88US=> M3m1[|czcA>? NY[4XoM5TE2VTx?= NHH0dIZKSzVyPUKtOe69VQ>? MmDRNlI2PDN6NUe=
HCT-116/HT-29/MKN-45 NUPQV5oySXCxcITvd4l{KEG|c3H5 Ml7lNu69VQ>? NYrBN3dUPDiq MVzzbIlnfCCrbjDHNkBxcGG|ZR?= NFjLdm0zOjV2M{i1Oy=>
HT-29 and HCT-116 MkToR4F{eGG|ZTDhd5NigQ>? MlnkOe69VQ>? NELSTJAzPGh? M4Lldolv\HWlZYOgZ4F{eGG|ZTDhZ5Rqfmm2eR?= NGDGSoEzOjV2M{i1Oy=>
MM cell lines MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPxNVDPxE1? MUeyOIg> Mn7MSG1UVw>? M3LBRmlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? NGLQboczOjJyN{S4OS=>
ARP-1 NWLhSnNSSXCxcITvd4l{KEG|c3H5 MnLsNVDPxE1? Mn;ONlRp MVjEUXNQ NXPxZ5d1cW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> Mkm0NlIzODd2OEW=
SNU-601 MmHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XUWlczcA>? MnWxSG1UVw>? NI\JfnVKSzVyPUCuPFE3yrFyLkC2N:69VQ>? NVrZcnY6OjJzNUm4NVQ>
SNU-1 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfIO|Jp NGTQXXhFVVOR NWfLSXlKUUN3ME2xMlA5OsLzMD6wNljPxE1? M2jNfFIzOTV7OEG0
SNU-668 NVy1Zm9OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXCO|Jp NVjwUIlvTE2VTx?= MlvGTWM2OD1zLkW3PeKyOC5yN{VOwG0> NHfKOY8zOjF3OUixOC=>
AGS NFXucJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fQN|czcA>? MYHEUXNQ NFrSeG5KSzVyPUGuO|E1yrFyLkGxO:69VQ>? MVmyNlE2QThzNB?=
SNU-216 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS5O|Jp NYXOSo9pTE2VTx?= NXjUOm9lUUN3ME2yMlY6OsLzMD6wPFLPxE1? NXf2R|dQOjJzNUm4NVQ>
SNU-5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXIO|Jp NUm4[HZ2TE2VTx?= NF\2c2pKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? NHLhfo8zOjF3OUixOC=>
SNU-638 M4jsNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fEelczcA>? NEjoVFdFVVOR NFznUG9KSzVyPUKuNlgzyrFyLkC1N:69VQ>? M4CzbVIzOTV7OEG0
SNU-16 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\qO|Jp M1LlemROW09? NUCzc45[UUN3ME2xMlU4O8LzMD6wNFHPxE1? MX6yNlE2QThzNB?=
SNU-484 NVLafYxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHYO|Jp NYXTUFAzTE2VTx?= NIrvU4xKSzVyPUGuO|I5yrFyLkC0Oe69VQ>? NHzwVWMzOjF3OUixOC=>
SNU-620 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn3Xo84Omh? MkLCSG1UVw>? MoXRTWM2OD1{LkmzPeKyOC5yMEJOwG0> NUPRdXVHOjJzNUm4NVQ>
SNU-719 NH3CVnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml23O|Jp MlHLSG1UVw>? NEi3N|hKSzVyPUOuNFM4yrFyLkCzNu69VQ>? MUOyNlE2QThzNB?=
glioma cell lines M1nnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HqZ|czcA>? MWTJR|UxRTFvMt88US=> MV:yNlA3PTB6MB?=
U87 MkDBRZBweHSxc3nzJGF{e2G7 NIrt[XMz|ryP MkH0O|Jp MoDEbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCjbnSgZ4xm[X[nZDDQRXJRKGGwZDDjZZNx[XOnLUO= M4S2fVIzODZ3MEiw

... 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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID