Buparlisib (BKM120, NVP-BKM120)

製品コードS2247

Buparlisib (BKM120, NVP-BKM120)化学構造

分子量(MW):410.39

Buparlisib (BKM120, NVP-BKM120)は1種のセレクティブPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は52 nM/166 nM/116 nM/262 nMそれぞれに分かれます。BKM120 (NVP-BKM120, Buparlisib)はVPS34、mTORとDNAPKに作用する効果が良くなくて、PI4Kβにほとんど活性を表しません。臨床2期。

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文献中の引用(37)

カスタマーフィードバック(5)

  • 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.

製品安全説明書

PI3K阻害剤の選択性比較

生物活性

製品説明 Buparlisib (BKM120, NVP-BKM120)は1種のセレクティブPI3K阻害剤で、無細胞試験でp110α/β/δ/γに作用する時のIC50値は52 nM/166 nM/116 nM/262 nMそれぞれに分かれます。BKM120 (NVP-BKM120, Buparlisib)はVPS34、mTORとDNAPKに作用する効果が良くなくて、PI4Kβにほとんど活性を表しません。臨床2期。
靶点
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試験

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 M{HqWWN6fG:2b4jpZ{BCe3OjeR?= MnK5O|IhcA>? NF\jc2tFVVOR NV7TN2RRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCneIDy[ZN{cW6pIGDJN2tidHCqYTDFOVQ2UyCvdYThcpQhf2m2aDDHTVUxKG:oIECuNFAxOTV6IN88US=> NH;UVnMzPDlyMEK2Oi=>
DU145 MYrDfZRwfG:6aXOgRZN{[Xl? NYrx[2E3PzJiaB?= MlfkSG1UVw>? M1:zUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGW6cILld5NqdmdiTFvCNUBufXSjboSge4l1cCCJSUWwJI9nKDBwMECwOFM2KM7:TR?= NFLXWXQzPDlyMEK2Oi=>
A2780 NWrlPW5vS3m2b4TvfIlkKEG|c3H5 M4rRZ|czKGh? M1HMfmROW09? NFrrS|hEgXSxdH;4bYNqfHliYXfhbY5{fCCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFfJOVAhd2ZiMD6wNFA3OzVizszN M1TjU|I1QTByMk[2
U87MG NGT3ZZBEgXSxdH;4bYMhSXO|YYm= MXW3NkBp NEO2e2RFVVOR M1fqNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KFCWRV6t[IVncWOrZX70JIh2dWGwIGW4O21IKGOnbHzzJJdqfGhiR1m1NEBw\iByLkCwNFY6QCEQvF2= NILIbFAzPDlyMEK2Oi=>
A2780 M1:wbWZ2dmO2aX;uJGF{e2G7 MUSxJIg> M2K3N2ROW09? MmHVTY5pcWKrdHnvckBw\iCSSUPLMY1m\GmjdHXkJGFMXCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJJdqfGhiRVO1NEBw\iByLkC1OUDPxE1? M1fBb|I1QTByMk[2
DU145 NHzl[WJHfW6ldHnvckBCe3OjeR?= MYexJIg> MoPXSG1UVw>? NGXhfINKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hTFVzNEWgZ4VtdHNiaHHyZo9zcW6pIFzLRlEhdXW2YYTpc44hf2m2aDDFR|UxKG:oIECuNFc{KM7:TR?= M1K0d|I1QTByMk[2
A2780 MXXGeY5kfGmxbjDBd5NigQ>? Mkm4NUBp Ml60SG1UVw>? M4TlV2lvcGmkaYTpc44hd2ZiUFmzT{1u\WSrYYTl[EBCU1RiU3XyOFc{KHCqb4PwbI9zgWyjdHnvckBqdiCSVFXOMYRm\mmlaXXueEBpfW2jbjDBNlc5OCClZXzsd{B4cXSqIFXDOVAhd2ZiMD6wO|Qh|ryP NF\HWpczPDlyMEK2Oi=>
MCF7 MVXGeY5kfGmxbjDBd5NigQ>? NWLLdYZZOSCq MYjEUXNQ NV60OmZqUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgSVU1PUtibYX0ZY51NW2nZHnheIVlKEGNVDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKHerdHigSWM2OCCxZjCwMlEh|ryP NG\hSYozPDlyMEK2Oi=>
U87MG Mn;JSpVv[3Srb36gRZN{[Xl? MoPONUBp MXrEUXNQ NF7xUVJKdmirYnn0bY9vKG:oIGDJN2sudWWmaXH0[YQhSUuWIGPldlQ4OyCyaH;zdIhwenmuYYTpc44hcW5iUGTFUk1l\W[rY3nlcpQhcHWvYX6gWVg4VUdiY3XscJMhf2m2aDDFR|UxKG:oIECuNVMh|ryP NYnSVG96OjR7MECyOlY>
A2780 NF\URWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M161TlczKGh? NFHTRmFFVVOR NFXmSIhGSzVyPUCuOVIh|ryP MWKyOFkxODJ4Nh?=
SKMES-1 MoXvR5l1d3SxeHnjJGF{e2G7 NH3reI8yKM7:TR?= NHfLT3k4OiCq MlTtTY5lfWOnczDj[YxtKGSnYYTo NX\CXGFGOjZyMUOzNVg>
H596 MXrGeY5kfGmxbjDBd5NigQ>? NUXheHJ2OSEQvF2= NUHqVIpLUW2yYXnyd{Bk\WyuIH3p[5JifGmxbh?= M{jrRVI3ODF|M{G4
HCC2450 NHi5SmdHfW6ldHnvckBCe3OjeR?= MkP1NUDPxE1? NETlV|lKdXCjaYLzJINmdGxiaX72ZZNqd25? MVyyOlAyOzNzOB?=
A549 MV7GeY5kfGmxbjDBd5NigQ>? MofZOVAxKG6P NYXFboFIPDhiaB?= NI\ne2NFVVOR NH:5VIxKdmirYnn0d{BCc3RiYXP0bZZifGmxbh?= NH;V[YkzPTl|N{K5PS=>
A549 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rESVEh|ryP MW[3NkBp MnLpSG1UVw>? NVHBTFdjUW6qaXLpeJMh[2WubDDndo94fGh? MmPPNlU6Ozd{OUm=
H522 MlrWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxJO69VQ>? MYK3NkBp MVrEUXNQ NVOzSZZlUW6qaXLpeJMh[2WubDDndo94fGh? MV6yOVk{PzJ7OR?=
LNCaP M{PiS2Z2dmO2aX;uJGF{e2G7 NGfKd4UyKM7:TR?= NUjtc3A1W3WycILld5NmeyCyLVHLWEBt\X[nbIO= NVWwWlBNOjV|NkC3PVk>
LNCaP95 MYfGeY5kfGmxbjDBd5NigQ>? NIjQN48yKM7:TR?= M3TlWHN2eHC{ZYPz[ZMheC2DS2SgcIV3\Wy| NHv5U3YzPTN4MEe5PS=>
HCT-15 NVXyN25oSXCxdH;zbZMhSXO|YYm= MnHmNVAh|ryP MnvCOFghcA>? MWXEUXNQ MV7JcoR2[2W|IHHwc5B1d3OrczDpckBJS1RvMUWgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? NIPvPXMzPTF3MkK0OS=>
HCT-116 M1X5emFxd3Sxc3nzJGF{e2G7 MmruNVAh|ryP MmSyOFghcA>? MVrEUXNQ NWnlWmlZUW6mdXPld{BieG:ydH;zbZMhcW5iSFPUMVEyPiClZXzsd{Bp[XKkb4XybY5oKFCLS{PDRUBpd3S|cH;0JI12fGG2aX;u M2fidVI2OTV{MkS1
NCI-H460 MUHBdI91d3OrczDBd5NigQ>? MWGxNEDPxE1? MVO0PEBp M2fvNGROW09? MnLlTY5lfWOnczDhdI9xfG:|aYOgbY4hVkOLLVi0OlAh[2WubIOgbIFz[m:3cnnu[{BRUUt|Q1GgbI91e3CxdDDteZRifGmxbh?= NVj2cYlJOjVzNUKyOFU>
SKOV-3 NYLod4VlSXCxdH;zbZMhSXO|YYm= MmnRNVAh|ryP M1vSZlQ5KGh? NFPoOpNFVVOR M{\oVWlv\HWlZYOgZZBweHSxc3nzJIlvKFONT2[tN{Bk\WyuczDoZZJjd3W{aX7nJHBKUzOFQTDoc5R{eG:2IH31eIF1cW:w NFflbpQzPTF3MkK0OS=>
BSY-1 NXXnfWZnSXCxdH;zbZMhSXO|YYm= MXexNEDPxE1? NXXWVWI3PDhiaB?= MkPjSG1UVw>? M{DBVGlv\HWlZYOgZZBweHSxc3nzJIlvKEKVWT2xJINmdGy|IHjhdoJwfXKrbnegVGlMO0ODIHjveJNxd3RibYX0ZZRqd25? MXqyOVE2OjJ2NR?=
MKN-1 M1XCR2Fxd3Sxc3nzJGF{e2G7 NHXmPYsyOCEQvF2= M2nvOlQ5KGh? NV\yNmJoTE2VTx?= MkXWTY5lfWOnczDhdI9xfG:|aYOgbY4hVUuQLUGgZ4VtdHNiaHHyZo92emmwZzDQTWs{S0FiaH;0d5BwfCCvdYTheIlwdg>? MUOyOVE2OjJ2NR?=
NCI-H522 M3[4VGFxd3Sxc3nzJGF{e2G7 M3XTNlExKM7:TR?= NEDuU|k1QCCq MmHVSG1UVw>? NWTWeIdmUW6mdXPld{BieG:ydH;zbZM> NIfqTZMzPTF3MkK0OS=>
OVCAR-3 M2T2c2Fxd3Sxc3nzJGF{e2G7 MUCxNEDPxE1? NGq3TZM1QCCq NWHRSmJOTE2VTx?= NI\QVHhKdmS3Y3XzJIFxd3C2b4Ppdy=> NH70dZEzPTF3MkK0OS=>
HBC-5 M3LkeGFxd3Sxc3nzJGF{e2G7 MXexNEDPxE1? M2\vflQ5KGh? MkL0SG1UVw>? NEnlPFhKdmS3Y3XzJIFxd3C2b4Ppdy=> M3y2UlI2OTV{MkS1
RXF-631L Moe4RZBwfG:|aYOgRZN{[Xl? NG\6T4MyOCEQvF2= NUCwPYhuPDhiaB?= M{joe2ROW09? NEXLTGhKdmS3Y3XzJIFxd3C2b4Ppdy=> MnfRNlUyPTJ{NEW=
MKN-45 NIL5O3RCeG:2b4Ppd{BCe3OjeR?= M2nNbFExKM7:TR?= MlrGOFghcA>? MkXRSG1UVw>? NYK1XpV{UW6mdXPld{BieG:ydH;zbZM> M2PCd|I2OTV{MkS1
BON-1 NVi2R3RvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXe1NFAhdk1? NXTjd2xYOTBiZB?= MXnEUXNQ MkTLTY5pcWKrdIOgZ4VtdCCpcn;3eIg> M17jNFI2ODJ4Mkmy
BON-1 MXrGeY5kfGmxbjDBd5NigQ>? MUG1NFAhdk1? NITrR5Q1KGh? NGP6Om9FVVOR NX[yUldkUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVDDheEBVcHJ|MEigZY5lKFOnckS3Ny=> NVu1copnOjVyMk[yPVI>
QGP-1 NH;zPY1HfW6ldHnvckBCe3OjeR?= MnHzOVAxKG6P NEfpelU1KGh? MX3EUXNQ MnKzTY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGFMXCCjdDDUbJI{ODhiYX7kJHNmejR5Mx?= NF3EfIYzPTB{NkK5Ni=>
Huh7 MYnGeY5kfGmxbjDBd5NigQ>? MUKxJO69VQ>? MkOyNUBp MnzYSG1UVw>? M1fnR2lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBCU1RiYYSgV4VzPDd2 NF3DblkzPTByNESwNy=>
BNL M4rwbWZ2dmO2aX;uJGF{e2G7 M4jTWlEh|ryP NYjCW4NpOSCq NHjDR5RFVVOR NEm5cGRKdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhWzZ? NGHSNWUzPTByNESwNy=>
MDA-MB-175 MnHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLBNUDPxE1? M{HzUVUh\A>? NUPPdWVNTE2VTx?= M1frPGlEPTB:MTFOwG0> NX3U[IdZOjR6N{m3PVY>
MDA-MB-134 NULlVoptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjSd3gyKM7:TR?= M4XHUlUh\A>? M122OmROW09? Mm\JTWM2ODxzIN88US=> NIjGe5kzPDh5OUe5Oi=>
HCC1500 NU\SfZhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\oblhJOSEQvF2= MYC1JIQ> MX\EUXNQ M1\5Z2lEPTB:MTFOwG0> Mn\yNlQ5Pzl5OU[=
EFM-19 M1PQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;Rc3hNOSEQvF2= NWW2XZhOPSCm NWPjOpk4TE2VTx?= Mon6TWM2ODxzIN88US=> MX2yOFg4QTd7Nh?=
ZR-75-30 NYHvdId5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4q5R|Eh|ryP NEjlTY82KGR? MoSxSG1UVw>? NHjWdo9KSzVyPEGg{txO NIH5VmMzPDh5OUe5Oi=>
MDA-MB-361 NWHCXW9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HucVEh|ryP M{mxVVUh\A>? NXjaXIJQTE2VTx?= MWfJR|UxRDFizszN MYeyOFg4QTd7Nh?=
T-47D NVPmZno4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:xJO69VQ>? MmTkOUBl NIHh[VJFVVOR M3rJSmlEPTB:MTFOwG0> MUmyOFg4QTd7Nh?=
SK-BR-3 M3XyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULXfY1nOSEQvF2= NI\wXoc2KGR? NEmw[IZFVVOR NEf2[nRKSzVyPEGg{txO MX[yOFg4QTd7Nh?=
UACC-732 MmixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXwT4cyKM7:TR?= NILLUHQ2KGR? NIjiRohFVVOR MmfnTWM2ODxzIN88US=> MonSNlQ5Pzl5OU[=
BT-474 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHNUVU{OSEQvF2= MmfhOUBl MX;EUXNQ M1rpZmlEPTB:MTFOwG0> M2PwU|I1QDd7N{m2
HCC202 M3L1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSxJO69VQ>? MU[1JIQ> NV7De2prTE2VTx?= M4fzWmlEPTB:MTFOwG0> MYmyOFg4QTd7Nh?=
MCF7 NXv0dYZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXJW4hMOSEQvF2= NYrobXFOPSCm MoPjSG1UVw>? MnuxTWM2ODxzIN88US=> M3jXVVI1QDd7N{m2
MDA-MB-415 Ml7YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nqZVEh|ryP MUm1JIQ> NEjlOoRFVVOR M2P2TGlEPTB:MTFOwG0> NFT3O2UzPDh5OUe5Oi=>
MDA-MB-453 NFi3eZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXm[JgyKM7:TR?= MX:1JIQ> MYjEUXNQ MXfJR|UxRDFizszN M1zQeFI1QDd7N{m2
ZR-75-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXGxR3FiOSEQvF2= NW\BXHN2PSCm NUPCTmhrTE2VTx?= MY\JR|UxRDFizszN Mn64NlQ5Pzl5OU[=
HCC38 M{PmdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV73cllGOSEQvF2= NGPBTmQ2KGR? M{LzcWROW09? NYW3SXdUUUN3MEyxJO69VQ>? MYKyOFg4QTd7Nh?=
HCC1419 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:3e|Eh|ryP Mlr6OUBl MlnFSG1UVw>? M3naRmlEPTB:MTFOwG0> NGW5T|YzPDh5OUe5Oi=>
UACC-812 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXuNUDPxE1? NWnLN414PSCm NYfHdplJTE2VTx?= MoraTWM2ODxzIN88US=> MV6yOFg4QTd7Nh?=
HCC1187 NFfBV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\QXZljOSEQvF2= NXPtc|JWPSCm M3H2UGROW09? NX;XZZBvUUN3MEyxJO69VQ>? NYL0OW5kOjR6N{m3PVY>
KPL-1 Mlu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfCPIVNOSEQvF2= M37nPFUh\A>? MoPGSG1UVw>? NIizeYpKSzVyPEGg{txO M{HVV|I1QDd7N{m2
SUM-225 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVm0b2ttOSEQvF2= M2XxZVUh\A>? NWLjWXpqTE2VTx?= MkPITWM2ODxzIN88US=> NF;McHEzPDh5OUe5Oi=>
EFM-192A MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILjO2kyKM7:TR?= M33CZlUh\A>? NHz0dlhFVVOR NWjCRYdjUUN3MEyxJO69VQ>? MVeyOFg4QTd7Nh?=
JIMT-1 M2\Hb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v5c|Eh|ryP NWmyXpFvPSCm M1TJT2ROW09? MYDJR|UxRDFizszN MWOyOFg4QTd7Nh?=
HCC1143 NVrLd4N{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfn[pkyKM7:TR?= NUjQSpVNPSCm M4fNcWROW09? MVXJR|UxRDFizszN MoXXNlQ5Pzl5OU[=
HCC2218 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjJRox1OSEQvF2= MYi1JIQ> Moi1SG1UVw>? NXTXe2I1UUN3MEyxJO69VQ>? MkTpNlQ5Pzl5OU[=
MDA-MB-468 MmrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DObVEh|ryP MXS1JIQ> NYfqcHJmTE2VTx?= NXjKXVhEUUN3MEyxJO69VQ>? M2Ty[FI1QDd7N{m2
BT-20 NV\SeXdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHLfYhDOSEQvF2= MUG1JIQ> NXfYT2dZTE2VTx?= MoLTTWM2ODxzIN88US=> MnvINlQ5Pzl5OU[=
MDA-MB-435 M1fFZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofWNUDPxE1? M4nuRlUh\A>? NUjoW4ZmTE2VTx?= M1;3[mlEPTB:MTFOwG0> NYTBbolFOjR6N{m3PVY>
BT-549 NIrXbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYq2UWpQOSEQvF2= MmLpOUBl Mlu5SG1UVw>? NVnsPGV1UUN3MEyxJO69VQ>? M{HVfVI1QDd7N{m2
HCC1806 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES0ZXoyKM7:TR?= NXrTPG13PSCm NEGwVZRFVVOR MVXJR|UxRDFizszN NEezZmkzPDh5OUe5Oi=>
HCC1937 NHr3fmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyxJO69VQ>? NYrVe481PSCm NVHuXZJiTE2VTx?= MoTETWM2ODxzIN88US=> M{nRd|I1QDd7N{m2
Hs578T NIr2V2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHkeVBwOSEQvF2= MYG1JIQ> MYfEUXNQ M{TnVWlEPTB:MTFOwG0> NEPuOY8zPDh5OUe5Oi=>
LN18 MkTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfWTVFuOjBizszN MUK3NkBp M17GPWROW09? NFe3W5JKSzVyPEWg{txO NVS4XlQ6OjR5NEGwO|Q>
LN229 M3S3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;NUlIxKM7:TR?= M3WwWVczKGh? M3vndmROW09? NFjWeldKSzVyPEWg{txO M1jqWlI1PzRzMEe0
LNZ308 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOyNEDPxE1? MmOwO|IhcA>? M2LNdWROW09? M1TQVWlEPTB:NTFOwG0> NHGxSIUzPDd2MUC3OC=>
T98G Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLuOFVROjBizszN NVLqR5ZrPzJiaB?= MYDEUXNQ NHPpbXJKSzVyPEWg{txO NYTiWJdIOjR5NEGwO|Q>
U87 NEDpcZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTFPJUzOCEQvF2= MlqxO|IhcA>? NH\mO3VFVVOR MVLJR|UxRDVizszN NETjW2gzPDd2MUC3OC=>
LN18 M1TXVWZ2dmO2aX;uJGF{e2G7 MWO1JO69VQ>? M4jv[VI1KGh? NFTyU5RFVVOR NUnsepJWUW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEGNVB?= NYrwNmpTOjR5NEGwO|Q>
LNZ308 MlHBSpVv[3Srb36gRZN{[Xl? NUO0d|l[PSEQvF2= Mk[1NlQhcA>? M2\vVmROW09? MVfJcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gRWtV M4jDc|I1PzRzMEe0
Saos-2 M1myPWZ2dmO2aX;uJGF{e2G7 M17LTFUxKM7:TR?= MlKzOFghcA>? NUnPO4ZEUW6qaXLpeJMh[2WubDDpcpZie2mxbh?= NVf3THdoOjR5Mke2OlA>
MG-63 NXX0bIJiTnWwY4Tpc44hSXO|YYm= NGPqSYc2OCEQvF2= NHrxdZA1QCCq MkTGTY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? M2XWOFI1PzJ5Nk[w
SJSA-1 MYjGeY5kfGmxbjDBd5NigQ>? MWK1NEDPxE1? MYK0PEBp NHrwOWRKdmirYnn0d{Bk\WyuIHnueoF{cW:w NWnoOY93OjR5Mke2OlA>
Saos-2 M3f3SWZ2dmO2aX;uJGF{e2G7 M1XiblUxKM7:TR?= NVviU2kxPDhiaB?= NFm2Z2RKdmirYnn0d{Bu[XS{aYigcYV1[Wyub4Dyc5RmcW6jc3WtNkBmgHC{ZYPzbY9v MU[yOFczPzZ4MB?=
MG-63 M13nSGZ2dmO2aX;uJGF{e2G7 NGOyVWw2OCEQvF2= NV\oTlN4PDhiaB?= MknHTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> M3riS|I1PzJ5Nk[w
SJSA-1 NH[xbmRHfW6ldHnvckBCe3OjeR?= MWq1NEDPxE1? NXrNSoFJPDhiaB?= MmrzTY5pcWKrdIOgcYF1emm6IH3leIFtdG:ycn;0[Ylv[XOnLUKg[ZhxemW|c3nvci=> NIDrRmMzPDd{N{[2NC=>
Saos-2 Mn7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;sOVUxKM7:TR?= NGTsdGw1QCCq MmnOTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? Mo\NNlQ4Ojd4NkC=
MG-63 M3TEW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m1cVUxKM7:TR?= MnHUOFghcA>? NIS3d2hKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NVfCU4JUOjR5Mke2OlA>
SJSA-1 NXqxdFdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3viflUxKM7:TR?= NVX2V4t4PDhiaB?= M4HX[GlvcGmkaYTzJINmdGxidnnhZoltcXS7 M{PDeFI1PzJ5Nk[w
FaDu NVLad|M{TnWwY4Tpc44hSXO|YYm= M{W5[VUh|ryP MYCyOEBp NWnOdXJmTE2VTx?= NXflT2FyWmWmdXPld{BwgHmpZX6gZ49ve3WvcITpc44> NXjBN5ZIOjR4M{GxOFc>
EMT6 M{G5dmZ2dmO2aX;uJGF{e2G7 NIS5SWw2KM7:TR?= MnHlNlQhcA>? M3H4U2ROW09? MoO5VoVlfWOnczDvfJlo\W5iY3;ud5VueHSrb36= MXeyOFY{OTF2Nx?=
HCT116 MmXVSpVv[3Srb36gRZN{[Xl? NIjxUmQ2KM7:TR?= NIXh[GUzPCCq MYnEUXNQ MYnS[YR2[2W|IH;4fYdmdiClb37zeY1xfGmxbh?= NHL1OlEzPDZ|MUG0Oy=>
U87 NUXxcpZ5TnWwY4Tpc44hSXO|YYm= NUnP[INMPSEQvF2= MWGyOEBp M1jkdGROW09? NGfENldT\WS3Y3XzJI95gWenbjDjc45{fW2ydHnvci=> NGexT40zPDZ|MUG0Oy=>
GBM Mlu3RZBweHSxc3nzJGF{e2G7 Mon1Nu69VQ>? NWrsc|QxPDiq NXjSR2NxTE2VTx?= MoLRbY5lfWOnZDDobYdp\XJibHX2[Yx{KG:oIHHwc5B1d3OrczygZY5lKGSnY4LlZZNm\CClZXzsJJZq[WKrbHn0fS=> Mlm5NlQ2ODB2OUK=
BON MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCxMVXPxE1? MWq3Nog> M4jtd4Rm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> NVnVVIpGOjR2NEO1NlM>
BON MkPzRZBweHSxc3nzJGF{e2G7 NWHoXI96OS13zszN NGTafHgzPGh? MVHpcoNz\WG|ZYOgZZBweHSxc3nz M3\DRVI1PDR|NUKz
H1975 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v1T|AvOy17LkdOwG0> M2D6WlczcA>? MkTlSG1UVw>? M2\ibGlEPTB;MT6zPFXPxE1? MVuyOFM{Pzh2Nh?=
H1975 NE\MPXRCeG:ydH;zbZMhSXO|YYm= M1zxTVLPxE1? NIDqTGMzPGh? MU\EUXNQ NHP2SZVqdmO{ZXHz[ZMh[XCxcITvd4l{KHKjdHWgd4lodmmoaXPhcpRtgQ>? NFvmbY4zPDN|N{i0Oi=>
T-ALL MmfrRZBweHSxc3nzJGF{e2G7 NYTSWXFy[mW2d3XlckAyNjRiYX7kJFUvOyCvTTDheEAzPGhiYX7kJFAvQSCjbnSgOU42KG2PIHH0JFQ5cCCrbjDkbYZn\XKnboSgZ4VtdCCuaX7l NFn5bnIzPCCxcjC0PIg> MXXEUXNQ MV;h[oZm[3S|IITo[UBRUTONIIDheIh4[XliaX6gWE1CVExiY3XscEBtcW6ncx?= MoPpNlQ{OTB5M{[=
BCR-ABL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCwMlI2NTFyzszN MkfFOIQ> NVK1Rpd7e2mpbnnmbYNidnSueTDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= M{\ROlI1OjR2NkGy
LC-1/SQSF NWTKToV{TnWwY4Tpc44hSXO|YYm= M1KzblPPxE1? NWPXOldjOjSq Ml24SG1UVw>? M{HNT4Rm[3KnYYPlJG5TTjJicILveIVqdiCuZY\lcC=> M2rVV|I{QThyMEmz
Primary CLL cells MljDRZBweHSxc3nzJGF{e2G7 M3OzUlEuOTEQvF2= MnvsOFhp NFjYOVFqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCFTFygZ4VtdHNiaX7k[ZBmdmSnboSgc4YheHKxZ37vd5Rq[yCvYYLr[ZJ{ Ml7oNlM5PTB6MEe=
Primary CLL cells MlviT4lv[XOnIFHzd4F6 NGG4dHAz|ryP M2HscFMxdWmw NF;NNZNl\WO{ZXHz[YQhWEl|SzDhZ5Rqfmm2eR?= NVzYc4Q6OjN6NUC4NFc>
Primary CLL cells NV6yRXFyS3m2b4TvfIlkKEG|c3H5 NEP1SJUz|ryP M1X2ZVI1cA>? M33Rcolv\HWlZYOgZ4VtdCCleYTveI95cWOrdIm= MVmyN|g2ODhyNx?=
human NSCLC cell lines MXLBdI9xfG:|aYOgRZN{[Xl? NHOwTowxNjF{NT20{txO NHjLTlAzPGh? MX7EUXNQ NYrmV4V{UUN3MIOgdoFv\2W|IH\yc40hOC52LUNOwG0> MoixNlM2PjJ2N{K=
human HCC cell lines NFTqfnhE\WyuII\pZYJqdGm2eTDhd5NigQ>? M{e2S|AvODB3LUJOwG0> NYS2U4tyPDiq Ml30TWM2OD1zzszN NIXkVnQzOzR6OUm5PS=>
Huh7 MWfLbY5ie2ViQYPzZZk> NHjMOGwy|ryP NVf5WFg5PDiq MmXJd4lodmoxrJHjZY51dHlicnXkeYNmeyCyaH;zdIhwenmuYYTpc44hd2ZiQXv0 M4rEXVI{PDh7OUm5
SK-HEP1 M1HZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXwNU0zOM7:TR?= M2TOVlczcA>? MV7EUXNQ M3LPWWlEPTExvKyx{txO NEnP[lYzOzR5OUGzOi=>
786-0 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxMVIx|ryP NXTVN3NSPzKq NGOwRoVFVVOR Mmn4TWM2OO,:nEJOwG0> NEHmfIMzOzR5OUGzOi=>
JVM2 M1LQUmN6fG:2b4jpZ4l1gSCjc4PhfS=> NXm0fJdYOC5{LUKw{txO NUK3SVFoPzKq MX\EUXNQ M3W0bGlEPTB;MD65{txO MkHUNlMzOzh4M{m=
EHEB MWXDfZRwfG:6aXPpeJkh[XO|YYm= MUGwMlIuOjEQvF2= M3;VUVczcA>? MlfsSG1UVw>? NIe1N|FKSzVyPUCuO:69VQ>? M1PEeFI{OjN6NkO5
MEC2 NUGwWI5YS3m2b4TvfIlkcXS7IHHzd4F6 NXHHbZBROC5{LUKw{txO NGLQTYQ4Omh? NHTSOnVFVVOR M4HkbmlEPTB;MD63{txO M4L1ZVI{OjN6NkO5
primary B-CLL lymphocytes MkLiRZBweHSxc3nzJGF{e2G7 MmD0TWM2OCCob4Kg[YFkcCCycnntZZJ6KGOnbHygcIlv\Q>? NGPB[JAzPGh? MoqzSG1UVw>? NGWxXGtKSzVy78{cN:69VSCob4KgZYxtKHCjdHnlcpR{ NFvVfVQzOzJ|OE[zPS=>
primary B-CLL lymphocytes NVrrfWFYU2mwYYPlJGF{e2G7 NFfEfZZKSzVyIH\vdkBm[WOqIIDybY1ienliY3XscEBtcW6n NVr3dIlLOjSq NVGw[nB1cW6qaXLpeJMheDdyU{\LJEYhPEVvQmCxJIV5eHKnc4Ppc44> M4P5elI{OjN6NkO5
human NSCLC NIT2fndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\4OVAvPS1{zszN MVW3Nog> NHS2eZZKSzVyPUJOwG0> MWSyNlc5OTN7Mx?=
human NSCLC NYrUbVBwU2mwYYPlJGF{e2G7 MWqx{txO MmnMNlRp MXfpcohq[mm2czD0bIUhSWu2L33UU3Ihe2mpbnHsbY5oKHCjdHj3ZZkh[XRiM3igZYZ1\XJidILlZZRu\W62 NHLzSXIzOjd6MUO5Ny=>
Y1 cell line NWfMSm5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2wMlHPxE1xMd88US=> NILCVXQzPGh? MY\EUXNQ MUTpcohq[mm2czC2NQ+9jSClZXzsJJZq[WKrbHn0fUBqdiCPeXOtV4N1ei22cnHud4Zm[3SnZDDj[Yxtew>? MnnJNlI3QTJ7MES=
PIK3CA-mutant MCF7 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HFUWdKPTB;MU[wxtE6OW6P78{MUGQ2OD17OEFCtVI4O26P NUjLZmdWPzKq NFu2SVlIUTVyPUG2NOKyQTGwTf-8kGxFPTB;OUiwxtEzPzOwTR?= MYCyNlY2Ozl4Nx?=
PIK3CA-mutant MCF7 NH3S[25McW6jc3WgRZN{[Xl? M4\w[2lEPTB;MUG0xtE{dk1? M{ftOlczcA>? Ml;nTWM2OD1zMUVCtVNvVSCrbjDy[YR2[2mwZzDBb5QheGixc4Doc5J6dGG2aX;uJIxmfmWucx?= MVSyNlY2Ozl4Nx?=
MCF7-myr-Akt MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC1S2k2OD1{OUpCtVY5dk4xvJzMSFUx97zgMUCsNFAxdk1? MYK3Nog> NEXyV29IUTVyPUK5PeKyPjiwTf-8kGxFPTExvK6xNEwxODCwTR?= M4q5flIzPjV|OU[3
colon cancer cell lines M4\HdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jMd|AuOTEQvF2= M{j2UlczcA>? MXvEUXNQ NGDPdWRKSzVyPUJOwG0> MVOyNlU1Ozh3Nx?=
gastric cancer cell lines MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\zbmgxNTFyzszN NIqyeHE4Omh? M{XifmROW09? NYr5OXpvUUN3ME2yMVXPxE1? MVWyNlU1Ozh3Nx?=
HCT-116/HT-29/MKN-45 M361[WFxd3C2b4Ppd{BCe3OjeR?= M2fHNVLPxE1? MljBOFhp M37mVpNpcW[2IHnuJGczKHCqYYPl NH\aRZIzOjV2M{i1Oy=>
HT-29 and HCT-116 MlW5R4F{eGG|ZTDhd5NigQ>? MV21{txO NIeySoUzPGh? NVzqSVJPcW6mdXPld{Bk[XOyYYPlJIFkfGm4aYT5 NXLvOXpkOjJ3NEO4OVc>
MM cell lines NUn0fWJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj1NVDPxE1? NE[z[ZozPGh? MUfEUXNQ NUWwRo1NUUN3MDD2ZZJq\XNiYX3vcoch\GmoZnXy[Y51KGOnbHygcIlv\XNiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdmOn NULSTm9KOjJ{MEe0PFU>
ARP-1 MnqxRZBweHSxc3nzJGF{e2G7 MYexNO69VQ>? MkXJNlRp M1T6RmROW09? NX7DOIl7cW6mdXPld{BOVSClZXzsJIFxd3C2b4Ppd{B1cHKxdXfoJINie3Cjc3WgZYN1cX[jdHnvci=> M1exSVIzOjB5NEi1
SNU-601 M3nMe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjpOWhwPzKq NGXEToRFVVOR NEHVOJlKSzVyPUCuPFE3yrFyLkC2N:69VQ>? NIj3ZoEzOjF3OUixOC=>
SNU-1 NYj3XW9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LtOVczcA>? MUfEUXNQ M3TQcWlEPTB;MT6wPFLDuTBwMEK4{txO M3zUTlIzOTV7OEG0
SNU-668 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHFdZdjPzKq NFO3fYFFVVOR NUT3U2p6UUN3ME2xMlU4QcLzMD6wO|TPxE1? MWGyNlE2QThzNB?=
AGS MoD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmO1O|Jp NUPs[I1ETE2VTx?= NXzUXGN4UUN3ME2xMlcyPMLzMD6xNVfPxE1? NUTjUY5jOjJzNUm4NVQ>
SNU-216 NFf0dHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\qNlczcA>? M3\yOGROW09? M2HYZmlEPTB;Mj62PVLDuTBwMEiy{txO NGHLOZkzOjF3OUixOC=>
SNU-5 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn0fpE4Omh? NH3pOZpFVVOR NG\QdlRKSzVyPUGuN|UyyrFyLkC5Ne69VQ>? MWCyNlE2QThzNB?=
SNU-638 M33pZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUm3Nog> MUjEUXNQ NVLEd2hWUUN3ME2yMlI5OsLzMD6wOVPPxE1? NXO4dYpsOjJzNUm4NVQ>
SNU-16 NHnhTnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXpfmZ{PzKq M2[5UmROW09? MnTTTWM2OD1zLkW3N:KyOC5yMEJOwG0> M4TaNFIzOTV7OEG0
SNU-484 MlO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi2O|Jp NXu1XYVFTE2VTx?= NWXDZZRFUUN3ME2xMlczQMLzMD6wOFXPxE1? NFPLOmUzOjF3OUixOC=>
SNU-620 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXUO|Jp MoHJSG1UVw>? NGDWNmlKSzVyPUKuPVM6yrFyLkCwNe69VQ>? MYCyNlE2QThzNB?=
SNU-719 NVfBWnJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS0O|Jp MULEUXNQ NHnKfmdKSzVyPUOuNFM4yrFyLkCzNu69VQ>? MUCyNlE2QThzNB?=
glioma cell lines NVjETWE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXicndNPzKq Mo\DTWM2OD1zLUNOwG0> MWGyNlA3PTB6MB?=
U87 NYfFTow5SXCxcITvd4l{KEG|c3H5 M{TWeFLPxE1? MkLPO|Jp NEK3O3lqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHHu[EBkdGWjdnXkJHBCWlBiYX7kJINie3Cjc3WtNy=> MmXtNlIxPjVyOEC=

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[1]
+ 展開

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.
細胞アッセイ: [1]
+ 展開
  • 細胞株: A2780 cells.
  • 濃度: 0-6.6 μM
  • 反応時間: 3 days.
  • 実験の流れ: 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.
    (参考用のみ)
動物実験:[1]
+ 展開
  • 動物モデル: U87MG and A2780 xenografts are established in female nu/nu mice.
  • 製剤: In 15% Captisol.
  • 投薬量: ~60 mg/kg.
  • 投与方法: Dosed orally daily (q.d.).
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 82 mg/mL (199.8 mM)
Ethanol 2 mg/mL (4.87 mM)
Water <1 mg/mL
体内 0.5% CMC Na 6 mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 410.39
化学式

C18H21F3N6O2

CAS No. 944396-07-0
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID