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 41 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 Mn7RR5l1d3SxeHnjJGF{e2G7 NUnkfVN[PzJiaB?= MY\EUXNQ NUj6Vpl2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=> NFnEUJAzPDlyMEK2Oi=>
DU145 MWLDfZRwfG:6aXOgRZN{[Xl? MmDDO|IhcA>? NXTifYVFTE2VTx?= MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BmgHC{ZYPzbY5oKEyNQkGgcZV1[W62IIfpeIghT0l3MDDv[kAxNjByMESzOUDPxE1? MXeyOFkxODJ4Nh?=
A2780 MnHER5l1d3SxeHnjJGF{e2G7 NHr5N4E4OiCq NFXXb|RFVVOR M{DpdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIFGyO|gxKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY{PSEQvF2= M{fCO|I1QTByMk[2
U87MG M{LtRmN6fG:2b4jpZ{BCe3OjeR?= NV7IPZJoPzJiaB?= NWq3boVTTE2VTx?= MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBRXEWQLXTl[olkcWWwdDDoeY1idiCXOEfNS{Bk\WyuczD3bZRpKEeLNUCgc4YhOC5yMEC2PVgh|ryP NXziT3RkOjR7MECyOlY>
A2780 NVq5SWpwTnWwY4Tpc44hSXO|YYm= M1PZOFEhcA>? NFnENWVFVVOR M4fhcmlvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFXDOVAhd2ZiMD6wOVUh|ryP NGfLTpUzPDlyMEK2Oi=>
DU145 NI\DXZNHfW6ldHnvckBCe3OjeR?= M3;WXlEhcA>? M{fPW2ROW09? MofPTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGRWOTR3IHPlcIx{KGijcnLvdolv\yCOS1KxJI12fGG2aX;uJJdqfGhiRVO1NEBw\iByLkC3N{DPxE1? MmHlNlQ6ODB{Nk[=
A2780 MVLGeY5kfGmxbjDBd5NigQ>? NHX1epcyKGh? NGHrR|BFVVOR MUfJcohq[mm2aX;uJI9nKFCLM1utcYVlcWG2ZXSgRWtVKFOnckS3N{BxcG:|cHjvdplt[XSrb36gbY4hWFSHTj3k[YZq[2mnboSgbJVu[W5iQUK3PFAh[2WubIOge4l1cCCHQ{WwJI9nKDBwMEe0JO69VQ>? Mn:4NlQ6ODB{Nk[=
MCF7 MV7GeY5kfGmxbjDBd5NigQ>? NHnTSpYyKGh? NU\XT|hLTE2VTx?= NXHPUnhjUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP NHLhbZYzPDlyMEK2Oi=>
U87MG MYTGeY5kfGmxbjDBd5NigQ>? M3vu[|EhcA>? MkfxSG1UVw>? MmjGTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIlvKFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiRVO1NEBw\iByLkGzJO69VQ>? M1rnWVI1QTByMk[2
A2780 NEfYRXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe3NkBp M4noRmROW09? MYjFR|UxRTBwNUKg{txO MYqyOFkxODJ4Nh?=
SKMES-1 NULIO|JCS3m2b4TvfIlkKEG|c3H5 Mn\0NUDPxE1? Mkf0O|IhcA>? NGHPOGZKdmS3Y3XzJINmdGxiZHXheIg> M2iyRlI3ODF|M{G4
H596 M{TyfmZ2dmO2aX;uJGF{e2G7 MXixJO69VQ>? NGXhV4lKdXCjaYLzJINmdGxibXnndoF1cW:w NFy5W3QzPjBzM{OxPC=>
HCC2450 NUjtN21RTnWwY4Tpc44hSXO|YYm= Mn;vNUDPxE1? NHX6e3VKdXCjaYLzJINmdGxiaX72ZZNqd25? MUGyOlAyOzNzOB?=
A549 MYPGeY5kfGmxbjDBd5NigQ>? MmjpOVAxKG6P M2TtXlQ5KGh? NHXzdm1FVVOR MlzMTY5pcWKrdIOgRYt1KGGldHn2ZZRqd25? NEPNVHMzPTl|N{K5PS=>
A549 Mn;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTEWZUyKM7:TR?= MXy3NkBp NGG3eJVFVVOR NGXMU|VKdmirYnn0d{Bk\WyuIHfyc5d1cA>? M2PFWFI2QTN5Mkm5
H522 NEDJV5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWexJO69VQ>? NGD0Tm84OiCq MV;EUXNQ M{HoXWlvcGmkaYTzJINmdGxiZ4Lve5Rp NUnYW5VnOjV7M{eyPVk>
LNCaP NVKzVIxjTnWwY4Tpc44hSXO|YYm= Mlu2NUDPxE1? M3;V[XN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NIrrWVAzPTN4MEe5PS=>
LNCaP95 NUTWfoZwTnWwY4Tpc44hSXO|YYm= NUXlWFZrOSEQvF2= MmL0V5VxeHKnc4Pld{BxNUGNVDDs[ZZmdHN? M135dVI2OzZyN{m5
HCT-15 M1e0UmFxd3Sxc3nzJGF{e2G7 M17KT|ExKM7:TR?= NYnO[3pWPDhiaB?= MoTpSG1UVw>? M4fnSGlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xOUBk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NFH5ZVczPTF3MkK0OS=>
HCT-116 M2fldmFxd3Sxc3nzJGF{e2G7 NYjoeJVXOTBizszN NFntZ241QCCq M3z3d2ROW09? M{TsPGlv\HWlZYOgZZBweHSxc3nzJIlvKEiFVD2xNVYh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NEPYdJUzPTF3MkK0OS=>
NCI-H460 NUnMOWZRSXCxdH;zbZMhSXO|YYm= MlXZNVAh|ryP M{fVNVQ5KGh? NXzkZ5M2TE2VTx?= M4TvWGlv\HWlZYOgZZBweHSxc3nzJIlvKE6FST3IOFYxKGOnbHzzJIhiemKxdYLpcochWEmNM1PBJIhwfHOyb4SgcZV1[XSrb36= NHjCco4zPTF3MkK0OS=>
SKOV-3 NFTQR3FCeG:2b4Ppd{BCe3OjeR?= NVvhcGpjOTBizszN NUPG[plDPDhiaB?= M2jSfGROW09? MljkTY5lfWOnczDhdI9xfG:|aYOgbY4hW0uRVj2zJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? NXqyWlZTOjVzNUKyOFU>
BSY-1 NVThVmNYSXCxdH;zbZMhSXO|YYm= NEXjfmUyOCEQvF2= MoHFOFghcA>? NGnld4pFVVOR MYPJcoR2[2W|IHHwc5B1d3OrczDpckBDW1lvMTDj[YxteyCqYYLic5VzcW6pIGDJT|NESSCqb4TzdI91KG23dHH0bY9v NFHZeFEzPTF3MkK0OS=>
MKN-1 MX7BdI91d3OrczDBd5NigQ>? NUXBU4xOOTBizszN NUHsV4liPDhiaB?= MVHEUXNQ NVqxc2Q6UW6mdXPld{BieG:ydH;zbZMhcW5iTVvOMVEh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= M4\nOFI2OTV{MkS1
NCI-H522 NFLCUZBCeG:2b4Ppd{BCe3OjeR?= NUTkS|kyOTBizszN MlXmOFghcA>? MYXEUXNQ NG\aXJVKdmS3Y3XzJIFxd3C2b4Ppdy=> MX:yOVE2OjJ2NR?=
OVCAR-3 NUTBbZlWSXCxdH;zbZMhSXO|YYm= MnnYNVAh|ryP NH35V401QCCq MXrEUXNQ MXnJcoR2[2W|IHHwc5B1d3Orcx?= NYrweHpQOjVzNUKyOFU>
HBC-5 M3y4R2Fxd3Sxc3nzJGF{e2G7 NGWyVGUyOCEQvF2= MorpOFghcA>? M4GyWGROW09? MmqwTY5lfWOnczDhdI9xfG:|aYO= NYjUbWtHOjVzNUKyOFU>
RXF-631L NFjMSIZCeG:2b4Ppd{BCe3OjeR?= NHPZfpYyOCEQvF2= M3:2XlQ5KGh? M2[0c2ROW09? NEewR5lKdmS3Y3XzJIFxd3C2b4Ppdy=> NEDNcoEzPTF3MkK0OS=>
MKN-45 M1zwO2Fxd3Sxc3nzJGF{e2G7 MmfBNVAh|ryP MUi0PEBp MVHEUXNQ NXLPPIU3UW6mdXPld{BieG:ydH;zbZM> NIjtcIUzPTF3MkK0OS=>
BON-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C2dVUxOCCwTR?= NGjqS2gyOCCm MX7EUXNQ MnnsTY5pcWKrdIOgZ4VtdCCpcn;3eIg> NXLPXJRUOjVyMk[yPVI>
BON-1 MXnGeY5kfGmxbjDBd5NigQ>? NF\QVpI2ODBibl2= MV[0JIg> MYTEUXNQ NV7uNHZRUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> MlPYNlUxOjZ{OUK=
QGP-1 M{XCXGZ2dmO2aX;uJGF{e2G7 NVW3cXNCPTByIH7N NIL3RWw1KGh? MnzGSG1UVw>? MojpTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= MWSyOVAzPjJ7Mh?=
Huh7 NF;MRY1HfW6ldHnvckBCe3OjeR?= MXexJO69VQ>? M3TxUlEhcA>? MUDEUXNQ MlnMTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDT[ZI1PzR? MYWyOVAxPDRyMx?=
BNL NWjnUGNvTnWwY4Tpc44hSXO|YYm= MVWxJO69VQ>? NV7ZN4dGOSCq M1nLZmROW09? M{DtWmlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBUPg>? NXr4NpREOjVyMES0NFM>
MDA-MB-175 NUexPYJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTVfpdVOSEQvF2= MUC1JIQ> M1fYPWROW09? NUHhSIlXUUN3MEyxJO69VQ>? M4P2ZlI1QDd7N{m2
MDA-MB-134 NGTaTm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3XNUDPxE1? MWq1JIQ> NEjON41FVVOR NFvJW|BKSzVyPEGg{txO NHfEPVMzPDh5OUe5Oi=>
HCC1500 NGq1N5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDYNUDPxE1? MYe1JIQ> MWLEUXNQ NHqxZ3hKSzVyPEGg{txO MUOyOFg4QTd7Nh?=
EFM-19 MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PKZVEh|ryP MmHqOUBl Mki0SG1UVw>? NWTtSmZ6UUN3MEyxJO69VQ>? NFKyNo0zPDh5OUe5Oi=>
ZR-75-30 NV[ycGt[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nrUFEh|ryP MnPOOUBl M3zZbmROW09? NWDYWG9FUUN3MEyxJO69VQ>? MYqyOFg4QTd7Nh?=
MDA-MB-361 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWWySYtZOSEQvF2= Ml;mOUBl NWn1Zm9TTE2VTx?= NVKyRmtlUUN3MEyxJO69VQ>? NXvzbJdOOjR6N{m3PVY>
T-47D NIPtfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFi0ZlkyKM7:TR?= MnzJOUBl M3\ldGROW09? NGm2bXVKSzVyPEGg{txO NIO5ZXMzPDh5OUe5Oi=>
SK-BR-3 M1zNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxJO69VQ>? NGLRS4U2KGR? NYrKfGp{TE2VTx?= M4DKVmlEPTB:MTFOwG0> NYXYcIxNOjR6N{m3PVY>
UACC-732 Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL4bnR5OSEQvF2= M2mzc|Uh\A>? M1TWWGROW09? M1LxOmlEPTB:MTFOwG0> MUKyOFg4QTd7Nh?=
BT-474 NUjvcGhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLiNUDPxE1? MX21JIQ> MWnEUXNQ NV[xN5pTUUN3MEyxJO69VQ>? NWrTdZdyOjR6N{m3PVY>
HCC202 MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGThbYEyKM7:TR?= MX:1JIQ> MXvEUXNQ M1KyTmlEPTB:MTFOwG0> MXGyOFg4QTd7Nh?=
MCF7 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG4VlkyKM7:TR?= NFm5Smo2KGR? Mnm1SG1UVw>? M{nuO2lEPTB:MTFOwG0> NVTKV3NlOjR6N{m3PVY>
MDA-MB-415 NHPPUphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK2NUDPxE1? Ml\4OUBl MUXEUXNQ NIrZfnJKSzVyPEGg{txO NGXLTpUzPDh5OUe5Oi=>
MDA-MB-453 NEDod|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXsWpEyKM7:TR?= MoPnOUBl MlzYSG1UVw>? MlvvTWM2ODxzIN88US=> NYLscVV5OjR6N{m3PVY>
ZR-75-1 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe3RmcyKM7:TR?= NIfk[2o2KGR? Mkj3SG1UVw>? M3HH[2lEPTB:MTFOwG0> MWiyOFg4QTd7Nh?=
HCC38 M3fpc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nnXVEh|ryP MX:1JIQ> M1n2bmROW09? Mn;FTWM2ODxzIN88US=> NGexSJYzPDh5OUe5Oi=>
HCC1419 MlzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:3b4oyKM7:TR?= Mn3TOUBl MVrEUXNQ NVT6b2FVUUN3MEyxJO69VQ>? NFn5RoYzPDh5OUe5Oi=>
UACC-812 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHGNUDPxE1? MUO1JIQ> Mmj5SG1UVw>? MnrpTWM2ODxzIN88US=> NUHBS5FyOjR6N{m3PVY>
HCC1187 NFzPXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[yNUDPxE1? MUi1JIQ> M{fzSmROW09? NF[wNohKSzVyPEGg{txO M4\nNVI1QDd7N{m2
KPL-1 NHXRSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LaUVEh|ryP M37kSFUh\A>? M1HKW2ROW09? MkK0TWM2ODxzIN88US=> M33mUVI1QDd7N{m2
SUM-225 NFznfXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPBc4cyKM7:TR?= MXG1JIQ> M33wT2ROW09? M{DJfGlEPTB:MTFOwG0> M33BT|I1QDd7N{m2
EFM-192A M4PqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvyNGwyKM7:TR?= M{TkSlUh\A>? M{KxNGROW09? MkjCTWM2ODxzIN88US=> M3\zflI1QDd7N{m2
JIMT-1 NFfkUWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT0cY1OOSEQvF2= NV\JcWREPSCm M1PLWWROW09? Mlv0TWM2ODxzIN88US=> MUKyOFg4QTd7Nh?=
HCC1143 M1jFfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\pdnoyKM7:TR?= M2PHclUh\A>? NGPkWJRFVVOR NH22WY5KSzVyPEGg{txO NI\4bI0zPDh5OUe5Oi=>
HCC2218 MlHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHXNol4OSEQvF2= M3;jOlUh\A>? NWf5R|ZzTE2VTx?= NHq1fXlKSzVyPEGg{txO NIG2UWszPDh5OUe5Oi=>
MDA-MB-468 M1i0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;yR2EyKM7:TR?= M{DlelUh\A>? MorZSG1UVw>? MWDJR|UxRDFizszN NHLGNmQzPDh5OUe5Oi=>
BT-20 NGrnUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTEUYRlOSEQvF2= MYi1JIQ> NXXqbI11TE2VTx?= MnXtTWM2ODxzIN88US=> M4\mVlI1QDd7N{m2
MDA-MB-435 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jUZ|Eh|ryP Mk\kOUBl M17wWmROW09? MlHVTWM2ODxzIN88US=> MWGyOFg4QTd7Nh?=
BT-549 NFLRUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmzT2MyKM7:TR?= NF;nVoQ2KGR? Mn7zSG1UVw>? MWXJR|UxRDFizszN NYPXNW1vOjR6N{m3PVY>
HCC1806 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjldpIyKM7:TR?= NVe5VFd5PSCm NFHmdY9FVVOR NVzOO2tmUUN3MEyxJO69VQ>? MnvWNlQ5Pzl5OU[=
HCC1937 MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPBNUDPxE1? MmHjOUBl MUHEUXNQ NV;vcpl1UUN3MEyxJO69VQ>? M1Syc|I1QDd7N{m2
Hs578T MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqxJO69VQ>? NIOzUJA2KGR? NVq2ZnF6TE2VTx?= M1n2emlEPTB:MTFOwG0> MVGyOFg4QTd7Nh?=
LN18 M{PvdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUeyNEDPxE1? NVTYUYJUPzJiaB?= NHrpZ3dFVVOR NIDDe5NKSzVyPEWg{txO M4PnOVI1PzRzMEe0
LN229 M{\ZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmyNEDPxE1? MYe3NkBp NY\lfVdCTE2VTx?= NHnPWWtKSzVyPEWg{txO MnfsNlQ4PDFyN{S=
LNZ308 NHvDeGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXENlAh|ryP Mn;6O|IhcA>? NETyV|NFVVOR MWDJR|UxRDVizszN M3jE[|I1PzRzMEe0
T98G NIXqOlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3pNlAh|ryP NFjs[HU4OiCq NU[1OWNZTE2VTx?= MlL1TWM2ODx3IN88US=> NGfJXpczPDd2MUC3OC=>
U87 NFzmeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DKTFIxKM7:TR?= MVG3NkBp MlPSSG1UVw>? Mn;2TWM2ODx3IN88US=> MVmyOFc1OTB5NB?=
LN18 M13sWGZ2dmO2aX;uJGF{e2G7 NV;6TI9nPSEQvF2= MoLoNlQhcA>? NX\iXohWTE2VTx?= MmG5TY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXA>? M2XN[|I1PzRzMEe0
LNZ308 MonZSpVv[3Srb36gRZN{[Xl? MnftOUDPxE1? MWeyOEBp MlPuSG1UVw>? NFvsR2VKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhSUuW M{jSdFI1PzRzMEe0
Saos-2 MV;GeY5kfGmxbjDBd5NigQ>? M{X4UFUxKM7:TR?= NGjm[Gc1QCCq MnHOTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? MX:yOFczPzZ4MB?=
MG-63 NH7Hb|ZHfW6ldHnvckBCe3OjeR?= NYCyeYZXPTBizszN NHzlcoE1QCCq NETXe5lKdmirYnn0d{Bk\WyuIHnueoF{cW:w NH;XVJYzPDd{N{[2NC=>
SJSA-1 NXPTVGVKTnWwY4Tpc44hSXO|YYm= M17xdFUxKM7:TR?= NU\TPJl2PDhiaB?= MlrZTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? M3fzV|I1PzJ5Nk[w
Saos-2 NWLVfYc{TnWwY4Tpc44hSXO|YYm= MXG1NEDPxE1? NVXGXmpPPDhiaB?= NVG0eFlvUW6qaXLpeJMhdWG2cnn4JI1mfGGubH;wdo91\WmwYYPlMVIh\XiycnXzd4lwdg>? MX[yOFczPzZ4MB?=
MG-63 MkexSpVv[3Srb36gRZN{[Xl? NV;YPG04PTBizszN MnHkOFghcA>? MXzJcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u NHHtbVAzPDd{N{[2NC=>
SJSA-1 MonWSpVv[3Srb36gRZN{[Xl? MnfyOVAh|ryP NE\nPG81QCCq MV7Jcohq[mm2czDtZZRzcXhibXX0ZYxtd3C{b4TlbY5ie2VvMjDlfJBz\XO|aX;u MkPlNlQ4Ojd4NkC=
Saos-2 MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:zOVAh|ryP MmXjOFghcA>? MYXJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? NXrod3R6OjR5Mke2OlA>
MG-63 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLBb4M2OCEQvF2= MkP5OFghcA>? M4roT2lvcGmkaYTzJINmdGxidnnhZoltcXS7 NVu5W2xiOjR5Mke2OlA>
SJSA-1 NHrLPINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVv5W4szPTBizszN M2TYUFQ5KGh? NXTzR|c2UW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= M3vaZVI1PzJ5Nk[w
FaDu Mlz2SpVv[3Srb36gRZN{[Xl? MV61JO69VQ>? NXi1eJFZOjRiaB?= NFPyPWFFVVOR NXHEVGo4WmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> MlLjNlQ3OzFzNEe=
EMT6 MWfGeY5kfGmxbjDBd5NigQ>? NUfub5poPSEQvF2= M2nud|I1KGh? NIrQNIZFVVOR M4r0THJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u NYnRZYUyOjR4M{GxOFc>
HCT116 NYr2e|JWTnWwY4Tpc44hSXO|YYm= NXzPVJlIPSEQvF2= NULK[|FEOjRiaB?= M3\JeWROW09? M4HUTnJm\HWlZYOgc5h6\2WwIHPvcpN2dXC2aX;u NFfIRmUzPDZ|MUG0Oy=>
U87 NVHaZ|NmTnWwY4Tpc44hSXO|YYm= MWC1JO69VQ>? M3P0VFI1KGh? NXzaTIdwTE2VTx?= MY\S[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NEm1ZmEzPDZ|MUG0Oy=>
GBM NHjKdGJCeG:ydH;zbZMhSXO|YYm= NEXVUIUz|ryP NF;HVpo1QGh? M2XMb2ROW09? M{\nS4lv\HWlZXSgbIlocGW{IHzleoVteyCxZjDhdI9xfG:|aYOsJIFv\CCmZXPy[YF{\WRiY3XscEB3cWGkaXzpeJk> MXGyOFUxODR7Mh?=
BON MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr3NU02|ryP NXniTJd5PzKq MkXi[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> NXjKcnNYOjR2NEO1NlM>
BON M4rONWFxd3C2b4Ppd{BCe3OjeR?= NH7XNVMyNTYQvF2= NGiyVIszPGh? NUfUfm9RcW6lcnXhd4V{KGGyb4D0c5Nqew>? NXW1fZJwOjR2NEO1NlM>
H1975 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqwMlMuQS54zszN MkjyO|Jp M{nEdWROW09? MXrJR|UxRTFwM{i1{txO MoGzNlQ{Ozd6NE[=
H1975 NF\mbJNCeG:ydH;zbZMhSXO|YYm= M{TLUVLPxE1? MV[yOIg> NUfqdpVZTE2VTx?= M4fZfYlv[3KnYYPld{BieG:ydH;zbZMhemG2ZTDzbYdvcW[rY3HueIx6 NYn5OmRmOjR|M{e4OFY>
T-ALL MnPtRZBweHSxc3nzJGF{e2G7 MoTBZoV1f2WnbjCxMlQh[W6mIEWuN{BuVSCjdDCyOIgh[W6mIECuPUBidmRiNT61JI1OKGG2IES4bEBqdiCmaX\m[ZJmdnRiY3XscEBtcW6n MnfCNlQhd3JiNEjo MWnEUXNQ NWPafYJz[W[oZXP0d{B1cGViUFmzT{Bx[XSqd3H5JIlvKFRvQVzMJINmdGxibHnu[ZM> NFLOboszPDNzMEezOi=>
BCR-ABL NWTOcmtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\6NVAvOjVvMUFOwG0> Mkn1OIQ> MUnzbYdvcW[rY3HueIx6KGmwaHnibZQh[2WubDDwdo9tcW[ncnH0bY9v MUWyOFI1PDZzMh?=
LC-1/SQSF MnLnSpVv[3Srb36gRZN{[Xl? MVez{txO NH:0SHAzPGh? M3vsR2ROW09? M37s[oRm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> NH3lb2QzOzl6MEC5Ny=>
Primary CLL cells MXHBdI9xfG:|aYOgRZN{[Xl? MV:xMVEx|ryP MlXPOFhp M1TCTIlv\HWlZYOgZZBweHSxc3nzJIlvKEOOTDDj[YxteyCrbnTldIVv\GWwdDDv[kBxem:pbn;zeIlkKG2jcnvldpM> NWLPdFV1OjN6NUC4NFc>
Primary CLL cells M4iyRmtqdmG|ZTDBd5NigQ>? MUiy{txO NHziXHQ{OG2rbh?= NGPK[Zdl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= MVmyN|g2ODhyNx?=
Primary CLL cells M3ruS2N6fG:2b4jpZ{BCe3OjeR?= NYi0coZXOs7:TR?= M1X1UVI1cA>? M2DXTIlv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MY[yN|g2ODhyNx?=
human NSCLC cell lines MYrBdI9xfG:|aYOgRZN{[Xl? NIf4fFAxNjF{NT20{txO NXq5NVhKOjSq M4DVfmROW09? NH2zb2pKSzVyczDyZY5o\XNiZoLvcUAxNjRvMt88US=> NH[1[XkzOzV4MkS3Ni=>
human HCC cell lines M1jJSWNmdGxidnnhZoltcXS7IHHzd4F6 NXmzc45kOC5yMEWtNe69VQ>? MVu0PIg> MWXJR|UxRTIQvF2= M1:3[FI{PDh7OUm5
Huh7 MofkT4lv[XOnIFHzd4F6 MkjYNe69VQ>? MknuOFhp M1PBWJNq\26r77{BZ4FvfGy7IILl[JVk\XNicHjvd5Bpd3K7bHH0bY9vKG:oIFHreC=> NVXVe2x5OjN2OEm5PVk>
SK-HEP1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3SZXAyNTJyzszN MlnLO|Jp MYjEUXNQ MV7JR|Ux97zeMd88US=> NWW0eJl4OjN2N{mxN|Y>
786-0 MkfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3sNogyNTJyzszN MYi3Nog> NFT3cpBFVVOR MlLMTWM2OO,:nEJOwG0> MnewNlM1PzlzM{[=
JVM2 MXjDfZRwfG:6aXPpeJkh[XO|YYm= NU\4S5RxOC5{LUKw{txO NIXoSZU4Omh? M33ZUWROW09? MUXJR|UxRTBwOd88US=> M3TaO|I{OjN6NkO5
EHEB NGewOVNEgXSxdH;4bYNqfHliYYPzZZk> M1zZW|AvOi1{MN88US=> MnGxO|Jp NX;CTIdwTE2VTx?= NXj6R|NSUUN3ME2wMlfPxE1? MofaNlMzOzh4M{m=
MEC2 NIXyUXVEgXSxdH;4bYNqfHliYYPzZZk> M2XxU|AvOi1{MN88US=> Mnz3O|Jp MYjEUXNQ M2jldGlEPTB;MD63{txO MlK1NlMzOzh4M{m=
primary B-CLL lymphocytes NXvGZo5VSXCxcITvd4l{KEG|c3H5 M1ThdGlEPTBiZn;yJIVi[2hicILpcYFzgSClZXzsJIxqdmV? NH7KbYozPGh? MX\EUXNQ NFTOVohKSzVy78{cN:69VSCob4KgZYxtKHCjdHnlcpR{ M2ja[lI{OjN6NkO5
primary B-CLL lymphocytes M{HodmtqdmG|ZTDBd5NigQ>? NGTuOo9KSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n MmjCNlRp NWnVS2RpcW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> NFrnOoYzOzJ|OE[zPS=>
human NSCLC NIPpXZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljqNE42NTMQvF2= M3j5VlczcA>? M3TJN2lEPTB;Md88US=> MliwNlI4QDF|OUO=
human NSCLC NX;vUmtPU2mwYYPlJGF{e2G7 NI\QbXky|ryP NVmxXGNuOjSq M4iwTIlvcGmkaYTzJJRp\SCDa4SvcXRQWiC|aXfuZYxqdmdicHH0bJdigSCjdDCzbEBi\nSncjD0doVifG2nboS= NH:2T3ozOjd6MUO5Ny=>
Y1 cell line MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHyZZd5OC5zzszNM|HPxE1? NX35Z2NzOjSq NEXOZ4lFVVOR NFXnPWRqdmirYnn0d{A3OO,:hTDj[YxtKH[rYXLpcIl1gSCrbjDNfYMuW2O2cj30doFve2[nY4Tl[EBk\Wyucx?= Mm\nNlI3QTJ7MES=
PIK3CA-mutant MCF7 NYLhbIJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC5S2k2OD1zNkFCtVkydk4xvJzMSFUxRTl6MNMxNlc{dk1? NHzSPXo4Omh? M2\SfWdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P Mo\vNlI3PTN7Nke=
PIK3CA-mutant MCF7 NYnI[W0{U2mwYYPlJGF{e2G7 M3fs[2lEPTB;MUG0xtE{dk1? NEnjPVY4Omh? NXzsXpJNUUN3ME2xNVTDuTOwTTDpckBz\WS3Y3nu[{BCc3RicHjvd5Bpd3K7bHH0bY9vKGyndnXsdy=> NWTiSG16OjJ4NUO5Olc>
MCF7-myr-Akt NGr0bZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFSyXVJIUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= MXu3Nog> MWjHTVUxRTJ7OdMxOlhvVe,:jFzEOVDwxJ5zMDywNFBvVQ>? NXy2dIlxOjJ4NUO5Olc>
colon cancer cell lines NInTcnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWwMVEx|ryP MkLmO|Jp MmfWSG1UVw>? NHvSclJKSzVyPUJOwG0> MlzwNlI2PDN6NUe=
gastric cancer cell lines M2T3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX6wMVEx|ryP MYm3Nog> NGfZU3pFVVOR Ml\qTWM2OD1{LUZOwG0> NUL2RmNOOjJ3NEO4OVc>
HCT-116/HT-29/MKN-45 MmjLRZBweHSxc3nzJGF{e2G7 M3\TNFLPxE1? NH73Zpc1QGh? M2rtPZNpcW[2IHnuJGczKHCqYYPl Ml2xNlI2PDN6NUe=
HT-29 and HCT-116 NWrWdYJVS2G|cHHz[UBie3OjeR?= M4rHU|XPxE1? MljzNlRp MXfpcoR2[2W|IHPhd5Bie2ViYXP0bZZqfHl? MlPoNlI2PDN6NUe=
MM cell lines MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXixNO69VQ>? NUXmToc1OjSq NIW0Z|hFVVOR M4W4TGlEPTBidnHybYV{KGGvb37nJIRq\m[ncnXueEBk\WyuIHzpcoV{KGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y5k\Q>? MnTTNlIzODd2OEW=
ARP-1 M{[xfWFxd3C2b4Ppd{BCe3OjeR?= NHrZb3AyOM7:TR?= NUDsNYNMOjSq NIG4V|lFVVOR NF\UVHJqdmS3Y3XzJG1OKGOnbHygZZBweHSxc3nzJJRpem:3Z3igZ4F{eGG|ZTDhZ5RqfmG2aX;u NYDCR3E4OjJ{MEe0PFU>
SNU-601 NFzUbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInrNHQ4Omh? MYDEUXNQ NXTxe|R4UUN3ME2wMlgyPsLzMD6wOlPPxE1? MofXNlIyPTl6MUS=
SNU-1 NW\HV|RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi3Nog> NWLNcIx[TE2VTx?= MVXJR|UxRTFwMEiyxtExNjB{ON88US=> NHzsdm4zOjF3OUixOC=>
SNU-668 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjpc5E4Omh? NFfKWmJFVVOR NXP4bnE1UUN3ME2xMlU4QcLzMD6wO|TPxE1? MWCyNlE2QThzNB?=
AGS NYfLOWRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnyyO|Jp MWHEUXNQ MmL2TWM2OD1zLkexOOKyOC5zMUhOwG0> MYiyNlE2QThzNB?=
SNU-216 M{[2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnGxO|Jp MXrEUXNQ NWrsNlNIUUN3ME2yMlY6OsLzMD6wPFLPxE1? M3HyR|IzOTV7OEG0
SNU-5 NYD4SHlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvkO|Jp Ml\qSG1UVw>? NFq2dFZKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? MnOwNlIyPTl6MUS=
SNU-638 MoTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[3Nog> MWLEUXNQ Mmr4TWM2OD1{LkK4NuKyOC5yNUROwG0> NXK5VHZOOjJzNUm4NVQ>
SNU-16 NFrsfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPPO|Jp NVPmdmcxTE2VTx?= M2CzSWlEPTB;MT61O|PDuTBwMECx{txO M{fNZVIzOTV7OEG0
SNU-484 NUDXc5hMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fJVFczcA>? MmHLSG1UVw>? MYjJR|UxRTFwN{K4xtExNjB2Nd88US=> NHm3WIozOjF3OUixOC=>
SNU-620 NF;GcJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P1OlczcA>? NWfHPJF4TE2VTx?= NGXmWW1KSzVyPUKuPVM6yrFyLkCwNe69VQ>? NXS0TIY{OjJzNUm4NVQ>
SNU-719 NHjkV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlu1O|Jp MYDEUXNQ MYjJR|UxRTNwMEO3xtExNjB|Mt88US=> MX2yNlE2QThzNB?=
glioma cell lines MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfPZnJIPzKq NEXjZZZKSzVyPUGtNu69VQ>? MViyNlA3PTB6MB?=
U87 NXrUd2dLSXCxcITvd4l{KEG|c3H5 NUDWTG14Os7:TR?= MU[3Nog> MXnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGGwZDDjcIVifmWmIGDBVnAh[W6mIHPhd5Bie2VvMx?= M1SxW|IzODZ3MEiw

... 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(Data is from Selleck tests instead of citations):
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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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
NCT02756247 Active not 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
NCT02756247 Active not 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
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
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

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID