BEZ235 (NVP-BEZ235, Dactolisib)

BEZ235 (NVP-BEZ235,Dactolisib)は一種の二重ATP競争性PI3KとmTOR抑制剤で、無細胞試験でp110α/γ/δ/β/mTOR(p70S6K)を抑制する時のIC50値は 4 nM /5 nM /7 nM /75 nM /6 nMそれぞれ分かれます。BEZ235 (NVP-BEZ235,Dactolisib)はT3TopBP1-ER 細胞の中でATRを抑制して、IC50 値が21 nMになって、Akt とPDK1に作用することが弱くなります。臨床2期。

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BEZ235 (NVP-BEZ235, Dactolisib) 化学構造
分子量: 469.55

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製品説明

  • Compare PI3K Inhibitors
    PI3K製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 BEZ235 (NVP-BEZ235,Dactolisib)は一種の二重ATP競争性PI3KとmTOR抑制剤で、無細胞試験でp110α/γ/δ/β/mTOR(p70S6K)を抑制する時のIC50値は 4 nM /5 nM /7 nM /75 nM /6 nMそれぞれ分かれます。BEZ235 (NVP-BEZ235,Dactolisib)はT3TopBP1-ER 細胞の中でATRを抑制して、IC50 値が21 nMになって、Akt とPDK1に作用することが弱くなります。臨床2期。
ターゲット

p110α

p110γ

p110δ

p110β

ATR

IC50

4 nM

5 nM

7 nM

75 nM [1]

21 nM [8]

In vitro試験 BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ235 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of BEZ235 with an average GI50 of 10-12 nM. [1] BEZ235 is an mTORC1/2 catalytic inhibitor. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Trypanosoma brucei brucei M3fSTmFvfGmvaXPyc4Jq[WxiQYPzZZk> MWCxPEBp M{nKUWROW09? NEHXPIRCdnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JJdqfGhiRVO1NEBw\iByLkCwNlUh|ryP NWjhc3R4OjR6MEW5OFY>
MCF7 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETXVZQxNjBzLUGwNEDPxE1? M4nsRVQ5KGh? MkjuSG1UVw>? M3LJ[2lEPTB;MD63N{DPxE1? MnLQNlM5PzF7MES=
HCT116 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2wMlAyNTFyMDFOwG0> NUPBb5c2PDhiaB?= NUS3UGdDTE2VTx?= MWTJR|UxRTFwMU[g{txO MoXLNlM5PzF7MES=
U87MG NYnsNm1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWiwMlAyNTFyMDFOwG0> MnvyOFghcA>? MXfEUXNQ MVnJR|UxRTFwM{Kg{txO MYiyN|g4OTlyNB?=
HBC4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMlAyNTFyMDFOwG0> NF;senE1QCCq MXLMc4chT0l3ME2tPE43OSCP M2HmTFIzOzN4MkS2
BSY1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;DU5E1OC5yMT2xNFAh|ryP MlTsOFghcA>? M4K2Umxw\yCJSUWwQU05NjR6IF2= NWnNNotSOjJ|M{[yOFY>
HBC5 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDqU|MxNjBzLUGwNEDPxE1? M1S1S|Q5KGh? NHnaeJZNd2diR1m1NF0uPy56NzDN MlOzNlI{OzZ{NE[=
MCF7 NUDhV2o3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOwMlAyNTFyMDFOwG0> MUW0PEBp MnPWUI9oKEeLNUC9MVgvOTZiTR?= NEnkRpgzOjN|NkK0Oi=>
MDA-MB-231 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMlAyNTFyMDFOwG0> NV7PV4V{PDhiaB?= MXTMc4chT0l3ME2tPE4xQSCP NYWydFNqOjJ|M{[yOFY>
U251 NX7yPJV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jwdVAvODFvMUCwJO69VQ>? NU[yeVZDPDhiaB?= MnjDUI9oKEeLNUC9MVcvPjZiTR?= Mn7FNlI{OzZ{NE[=
SF268 NF\kXoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFiycXUxNjBzLUGwNEDPxE1? NYPOTHR7PDhiaB?= NUHoPFFmVG:pIFfJOVA:NTdwOUKgUS=> M4DFR|IzOzN4MkS2
SF295 NVXUbG9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;BcZZwOC5yMT2xNFAh|ryP NIL0[IE1QCCq MnLXUI9oKEeLNUC9MVgvOzFiTR?= NXzxRY1{OjJ|M{[yOFY>
SF539 M2eyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoCxNE4xOS1zMECg{txO MVy0PEBp M2rBNGxw\yCJSUWwQU05NjV7IF2= MlT3NlI{OzZ{NE[=
SNB75 MmjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPFcWoxNjBzLUGwNEDPxE1? MkPCOFghcA>? NGW3eoJNd2diR1m1NF0uQC53ODDN M2jPWVIzOzN4MkS2
SNB78 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMlAyNTFyMDFOwG0> NWPQeGlDPDhiaB?= NV71bVhyVG:pIFfJOVA:NThwNkWgUS=> M37BR|IzOzN4MkS2
HCC2998 NETqfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ns[VAvODFvMUCwJO69VQ>? NGOweIQ1QCCq M3uzO2xw\yCJSUWwQU05NjB3IF2= MVKyNlM{PjJ2Nh?=
KM12 NVzkcGJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrXV4d5OC5yMT2xNFAh|ryP MYi0PEBp MWXMc4chT0l3ME2tO{42PCCP MVSyNlM{PjJ2Nh?=
HT-29 Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7Hd5B7OC5yMT2xNFAh|ryP NVy4fFBHPDhiaB?= MornUI9oKEeLNUC9MVcvPzViTR?= MWKyNlM{PjJ2Nh?=
HCT15 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCwMlAyNTFyMDFOwG0> NXrVblkxPDhiaB?= NFj3dmpNd2diR1m1NF0uQC5yMzDN NEDVTmYzOjN|NkK0Oi=>
HCT116 MkL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGwMlAyNTFyMDFOwG0> MVO0PEBp NFzhbGxNd2diR1m1NF0uPy54MTDN NFLHVIEzOjN|NkK0Oi=>
NCI-H23 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\yT2sxNjBzLUGwNEDPxE1? NU\iN|R7PDhiaB?= M4[2Z2xw\yCJSUWwQU04NjZ2IF2= MYWyNlM{PjJ2Nh?=
NCI-H226 M1jlfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvCO2wxNjBzLUGwNEDPxE1? MnH4OFghcA>? MVvMc4chT0l3ME2tPE41PCCP MoC0NlI{OzZ{NE[=
NCI-H522 M{S0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrtcpcxNjBzLUGwNEDPxE1? MXq0PEBp NUGxRnRwVG:pIFfJOVA:NThwNEWgUS=> M3fHZ|IzOzN4MkS2
NCI-H438 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHEfHJQOC5yMT2xNFAh|ryP MVi0PEBp MkLFUI9oKEeLNUC9MVgvOTFiTR?= MlHKNlI{OzZ{NE[=
A549 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnRZoN1OC5yMT2xNFAh|ryP M3LXVFQ5KGh? NULVPZFKVG:pIFfJOVA:NThwMEegUS=> MX2yNlM{PjJ2Nh?=
DMS273 NYXIV4I4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvic5UzOC5yMT2xNFAh|ryP M3H3WFQ5KGh? MXXMc4chT0l3ME2tO{45OCCP MXyyNlM{PjJ2Nh?=
DMS114 NEWzbZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3W5VFAvODFvMUCwJO69VQ>? NV7GXXJsPDhiaB?= MnfKUI9oKEeLNUC9MVgvOzliTR?= MX2yNlM{PjJ2Nh?=
LOXIMVI NHrBSJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLTZ4ExNjBzLUGwNEDPxE1? NHXrRW41QCCq MoS1UI9oKEeLNUC9MVgvPjZiTR?= MWCyNlM{PjJ2Nh?=
OVCAR3 NV3rXpBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn1dVFlOC5yMT2xNFAh|ryP M3HFOFQ5KGh? NXfYOohYVG:pIFfJOVA:NThwMUegUS=> NWHhbll5OjJ|M{[yOFY>
OVCAR4 M4\wOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvIS5hIOC5yMT2xNFAh|ryP NFvXXFg1QCCq NUHwOm5UVG:pIFfJOVA:NThwNUigUS=> M{\w[|IzOzN4MkS2
OVCAR5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXuSXVJOC5yMT2xNFAh|ryP MkLiOFghcA>? NEDneHBNd2diR1m1NF0uPy53NzDN Mm[2NlI{OzZ{NE[=
OVCAR8 NFr3[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPPNE4xOS1zMECg{txO NWLibJY1PDhiaB?= MmfHUI9oKEeLNUC9MVcvQDRiTR?= MXuyNlM{PjJ2Nh?=
SKOV3 NWTKdYhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPXcXoxNjBzLUGwNEDPxE1? MXu0PEBp NV7qfoNpVG:pIFfJOVA:NThwNEGgUS=> Mnm3NlI{OzZ{NE[=
RXF631L NHPnemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\hcFg3OC5yMT2xNFAh|ryP M3jjRlQ5KGh? M4jCeGxw\yCJSUWwQU05NjJzIF2= NIOwe5czOjN|NkK0Oi=>
ACHN MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSwMlAyNTFyMDFOwG0> NWO3UFFyPDhiaB?= NYrqO|BNVG:pIFfJOVA:NTdwOUWgUS=> MXWyNlM{PjJ2Nh?=
St-4 MnvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrlPFlbOC5yMT2xNFAh|ryP MknvOFghcA>? M2jLbWxw\yCJSUWwQU04NjR5IF2= NH;n[oczOjN|NkK0Oi=>
MKN1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKwMlAyNTFyMDFOwG0> NUDKcZBoPDhiaB?= MXvMc4chT0l3ME2tPE41OSCP NVuxZVFnOjJ|M{[yOFY>
MKN7 M3\FS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;GNFAvODFvMUCwJO69VQ>? NUXlTG1lPDhiaB?= NHL0flBNd2diR1m1NF0uPy54ODDN NVviZnlwOjJ|M{[yOFY>
MKN28 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX36RoJjOC5yMT2xNFAh|ryP MYS0PEBp M4jXRmxw\yCJSUWwQU04NjB5IF2= MYOyNlM{PjJ2Nh?=
MKN45 M2i3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWi3VXpwOC5yMT2xNFAh|ryP MV60PEBp MWPMc4chT0l3ME2tPE4{PCCP NWnQNoNDOjJ|M{[yOFY>
MKN74 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDpNE4xOS1zMECg{txO M4Phe|Q5KGh? Mli4UI9oKEeLNUC9MVcvPDJiTR?= NYTWfFF6OjJ|M{[yOFY>
DU145 NHnJXVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHrNoV6OC5yMT2xNFAh|ryP MUi0PEBp MYPMc4chT0l3ME2tPE4yPiCP MXiyNlM{PjJ2Nh?=
PC3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjme5VnOC5yMT2xNFAh|ryP MoXzOFghcA>? NIDoSJpNd2diR1m1NF0uQC54NjDN NWG5NFlzOjJ|M{[yOFY>
Trypanosoma brucei brucei MV3GeY5kfGmxbjDBd5NigQ>? MXiyNFAhdk1? NFfLVYUyOiCq NIDCfXFFVVOR M4XD[GRm[3KnYYPlJIlvKHCqb4PwbI91cWS7bDDpco9{cXSxbDDwbI9{eGijdHWgcIV3\Wx? NWr6dllOOjR6MEW5OFY>
Trypanosoma brucei brucei MkXrSpVv[3Srb36gRZN{[Xl? NInh[GsyQCCq MXXEUXNQ Mn[yTY5pcWKrdHnvckBw\iC{ZXPldJRwei2vZXTpZZRm\CCnbnTvZ5l1d3OrczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC2cnHud4ZmenKrbjD1dJRic2V? NXfFb3BLOjR6MEW5OFY>
Trypanosoma brucei brucei NWTKPVJ5TnWwY4Tpc44hSXO|YYm= NFL6eVMzODBibl2= NGHUcGkyOiCq NEi1S5VFVVOR NWDiWHp1TW[oZXP0JI9vKHOyaHnu[49ugWynaX6gcIV3\Wx? M3\kSlI1QDB3OUS2
Trypanosoma brucei brucei Ml\pSpVv[3Srb36gRZN{[Xl? NHXYSWMzODBibl2= MWSxNkBp M4HsSGROW09? MUDF[oZm[3Rib36gdIhwe3CqYYTp[Jlt[2ixbHnu[UBt\X[nbB?= NUXD[HhMOjR6MEW5OFY>
UM-UC-3 NFO2T2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MluzTWM2OD1|MUWgdG0> M1fycXNCVkeHUh?=
SBC-1 NGPVXFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fwSWlEPTB;N{SyJJBO NV[zSIdGW0GQR1XS
MKN1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvVTWM2OD1{Lkigcm0> NHfuOo9USU6JRWK=
NCI-H720 NYTpXmttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXaTWM2OD1|LkW3JI5O M2PrU3NCVkeHUh?=
BFTC-909 NXfZeG1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTCTWM2OD1|LkexJI5O MmPtV2FPT0WU
BPH-1 NXztW4FNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTRwN{[gcm0> Mnn4V2FPT0WU
PC-3 MoHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHGTWM2OD13LkC5JI5O NIi4NIZUSU6JRWK=
AN3-CA MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DwV2lEPTB;NT61OkBvVQ>? MUHTRW5ITVJ?
HN NWLQeVdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHublJKSzVyPUWuPVYhdk1? NF7kbpBUSU6JRWK=
HCC2218 M1W5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17oW2lEPTB;Nj62NUBvVQ>? MV;TRW5ITVJ?
KP-4 NIP1fm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HWVWlEPTB;NzDuUS=> NVXMRpZbW0GQR1XS
LU-139 NVLRT215T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLNTWM2OD15Lke3JI5O NFrlcXZUSU6JRWK=
ETK-1 NIHHTYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTdwOEigcm0> MoLzV2FPT0WU
Ramos-2G6-4C10 NGfqe4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDVSZBqUUN3ME24MlQ6KG6P MnvtV2FPT0WU
MHH-PREB-1 M{HXbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3senU4UUN3ME25MlEzKG6P MWPTRW5ITVJ?
DU-4475 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf6TWM2OD17LkS0JI5O NFHzPGZUSU6JRWK=
NCI-H1666 NIHmUYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDPUZR4UUN3ME25MlcyKG6P M{flV3NCVkeHUh?=
CAMA-1 NYC1VXI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzJTWM2OD17Lkigcm0> Mm\oV2FPT0WU
TYK-nu NI\RZlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHrUnhKSzVyPUmuPVQhdk1? M3TzT3NCVkeHUh?=
MFE-280 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojsTWM2OD17Lkm5JI5O Mnz4V2FPT0WU
A549 NVjEbHY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFyLkG0JI5O M{jyTHNCVkeHUh?=
769-P M2rsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFyLkS0JI5O Mnn3V2FPT0WU
L-363 NYHFN2V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH5TWM2OD1zMD62PUBvVQ>? NEPMOXhUSU6JRWK=
ES8 M1LEUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\RRppKSzVyPUGwMlkhdk1? NFrl[|FUSU6JRWK=
PA-1 Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFzLkiyJI5O M{n3XnNCVkeHUh?=
Mewo MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfYbJVHUUN3ME2xNU46QSCwTR?= MknUV2FPT0WU
HSC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XITWlEPTB;MUKuNlEhdk1? M3zTWnNCVkeHUh?=
H4 NEX1Z2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjqSnFKSzVyPUGyMlY4KG6P MVLTRW5ITVJ?
BB65-RCC M2[xT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHnTWM2OD1zMj63NkBvVQ>? M3rGTnNCVkeHUh?=
NCI-H1793 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\yTWM2OD1zMj64NkBvVQ>? MUTTRW5ITVJ?
KARPAS-45 NV3xSIZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTF|LkWxJI5O NFTIVWpUSU6JRWK=
GCT NIXvWlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP1dHdKSzVyPUGzMlY5KG6P MkXhV2FPT0WU
EoL-1 NGXneFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHe3PHpKSzVyPUGzMlk{KG6P M{fTOHNCVkeHUh?=
LB2241-RCC MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnT1TWM2OD1zND6wNUBvVQ>? NEHodFRUSU6JRWK=
ES5 M3jQcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vndGlEPTB;MUSuO|Qhdk1? NVvIXXI6W0GQR1XS
LOXIMVI Mmf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF2Lkm5JI5O NIXmNXNUSU6JRWK=
COR-L105 NVfZXFdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF3LkC0JI5O MkPnV2FPT0WU
P12-ICHIKAWA MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK3XohvUUN3ME2xOU4yKG6P M1zaRXNCVkeHUh?=
CHL-1 NIHiN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fVPGlEPTB;MUWuOFUhdk1? Mkm3V2FPT0WU
VMRC-RCZ MlvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTF3Lk[zJI5O Mor0V2FPT0WU
HH NF3ke29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\MOnpXUUN3ME2xOU44KG6P MlvrV2FPT0WU
NUGC-3 NGXDbHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInpPGZKSzVyPUG2MlM1KG6P NVvYdpZ6W0GQR1XS
EGI-1 M1XHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF4LkSzJI5O NGrmdHRUSU6JRWK=
OS-RC-2 M3fZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e2cGlEPTB;MU[uOFchdk1? NFjDUIpUSU6JRWK=
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SW1710 M4jLdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF6LkeyJI5O MoLkV2FPT0WU
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RT-112 NWTqRWM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPMZ2xJUUN3ME2xPU43PiCwTR?= NUjKTIEzW0GQR1XS
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RXF393 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;qOGc{UUN3ME2yNU41PSCwTR?= M3HyPHNCVkeHUh?=
NCI-H2030 NXjDUlVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnITWM2OD1{MT61NkBvVQ>? MojVV2FPT0WU
YH-13 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:4S|k4UUN3ME2yNU45QCCwTR?= NHPJSpBUSU6JRWK=
HT-1080 NGjr[4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXRV4FKSzVyPUKxMlk{KG6P MnuzV2FPT0WU
NCI-SNU-1 M1THOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\KR4JKSzVyPUKxMlk2KG6P MkWyV2FPT0WU
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786-0 NV;jSHpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrDVmt4UUN3ME2yNk4zQSCwTR?= MYrTRW5ITVJ?
ME-180 NVfZc4xWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:2TWM2OD1{Mj60N{BvVQ>? M3fYenNCVkeHUh?=
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SW780 MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWyXWZKSzVyPUKzMlE{KG6P MoToV2FPT0WU
MG-63 Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nRWWlEPTB;MkOuOFUhdk1? M3;aenNCVkeHUh?=
BV-173 NX2yTpVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoWxTWM2OD1{Mz64O{BvVQ>? M3\QdHNCVkeHUh?=
CAL-51 M4qzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHRb4NpUUN3ME2yN{45QSCwTR?= NXv2N2NIW0GQR1XS
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MEL-HO MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ2LkC0JI5O MUTTRW5ITVJ?
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Hs-578-T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDXTWM2OD1{ND61PEBvVQ>? MlL1V2FPT0WU
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FTC-133 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLW[IlKSzVyPUK1MlEhdk1? MV7TRW5ITVJ?
MOLT-4 M2HsPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJ3LkGyJI5O M4HUZ3NCVkeHUh?=
HO-1-N-1 NHXVZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DReWlEPTB;MkWuNVUhdk1? MVnTRW5ITVJ?
ES3 NF3kNZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLCemdKSzVyPUK1MlIzKG6P NIjRN2JUSU6JRWK=
TI-73 MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG2TWM2OD1{NT6yPEBvVQ>? MVPTRW5ITVJ?
MPP-89 MkDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LRPGlEPTB;MkWuN|Ihdk1? MkmxV2FPT0WU
KYSE-150 MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2SwOmlEPTB;MkWuPFkhdk1? M2nUVnNCVkeHUh?=
LXF-289 M{PBfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7jTWM2OD1{Nj6wOEBvVQ>? NFmxOHRUSU6JRWK=
SK-LU-1 NUS3fFZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDQbm1zUUN3ME2yOk4yPyCwTR?= Mli1V2FPT0WU
HOP-92 M3nxdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Tm[mlEPTB;Mk[uOFghdk1? MWfTRW5ITVJ?
HuO9 M3\kO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC4V4M1UUN3ME2yOk44PiCwTR?= MXfTRW5ITVJ?
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RS4-11 M2O4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LBU2lEPTB;Mk[uPVEhdk1? MXXTRW5ITVJ?
NCI-H292 M3\GVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HCTmlEPTB;Mkegcm0> M1;KVHNCVkeHUh?=
DB NX:yUZI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KzTGlEPTB;MkeuN|Yhdk1? NEPWPWtUSU6JRWK=
SW1088 M1;PZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j6VmlEPTB;MkiuNlkhdk1? NVS5b|BsW0GQR1XS
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MV-4-11 MmjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7HTWM2OD1{OD63JI5O Mmm5V2FPT0WU
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D-263MG MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rlVGlEPTB;MkmuN|Uhdk1? MlvIV2FPT0WU
U-2-OS MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi0V5dKSzVyPUK5MlUhdk1? M1nMT3NCVkeHUh?=
T98G Mor1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDVTWM2OD1{OT64PEBvVQ>? NEjvSYpUSU6JRWK=
GI-ME-N MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\VTWM2OD1{OT65NUBvVQ>? MYHTRW5ITVJ?
BHT-101 MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXOZoI3UUN3ME2zNE4xPSCwTR?= MY\TRW5ITVJ?
NOS-1 M4TLU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHXTWM2OD1|MD6xNkBvVQ>? MkjSV2FPT0WU
AsPC-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noSWlEPTB;M{CuNkBvVQ>? M3i3T3NCVkeHUh?=
QIMR-WIL NFnvfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTNyLk[gcm0> MlnnV2FPT0WU
JVM-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\ScW9KSzVyPUOwMlg{KG6P MVLTRW5ITVJ?
KU-19-19 MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXMTWM2OD1|MT6xN{BvVQ>? NHjTS|JUSU6JRWK=
OVCAR-8 NGjaXmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPaNmg4UUN3ME2zNU4zPiCwTR?= MWLTRW5ITVJ?
BEN NV\LVndKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDacmgyUUN3ME2zNU43OyCwTR?= M4DNVHNCVkeHUh?=
BE-13 Mkm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\VOZM2UUN3ME2zNU45OiCwTR?= M{LuOnNCVkeHUh?=
EW-18 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTNzLki2JI5O MoLmV2FPT0WU
ECC10 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;NT4gyUUN3ME2zNU46PSCwTR?= M1rU[XNCVkeHUh?=
CTV-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m3[WlEPTB;M{KuPFIhdk1? NH7CT3VUSU6JRWK=
COLO-800 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\pXJdXUUN3ME2zNk46OiCwTR?= M4Lt[HNCVkeHUh?=
A2058 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn2dHZKSzVyPUOzMlI2KG6P MlfRV2FPT0WU
VM-CUB-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYewelJ2UUN3ME2zN{41OyCwTR?= M1rkXHNCVkeHUh?=
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COLO-684 NVP0XWU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7OTWM2OD1|Mz61PEBvVQ>? MXzTRW5ITVJ?
RPMI-8226 MlTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Tte2lEPTB;M{OuPFIhdk1? M4nydHNCVkeHUh?=
SK-NEP-1 M3n0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13abmlEPTB;M{SuNVUhdk1? NGDJTnFUSU6JRWK=
Becker MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN2LkKxJI5O MoCzV2FPT0WU
NCI-H28 M3\Gdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTN2LkS0JI5O NWO3c4N5W0GQR1XS
CAL-120 NFz5SZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIryeGpKSzVyPUO0MlczKG6P NWrvc3NXW0GQR1XS
MDA-MB-157 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\ybGlEPTB;M{WuOFEhdk1? NVXHWWRzW0GQR1XS
OVCAR-5 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDiPIY2UUN3ME2zOU41PyCwTR?= NEHYWWFUSU6JRWK=
LAMA-84 MnfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTN3Lki3JI5O MofDV2FPT0WU
CAKI-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjxTWM2OD1|Nj60N{BvVQ>? NVTWTmR2W0GQR1XS
Daoy NIXlflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nKVGlEPTB;M{[uO{BvVQ>? M4S3dnNCVkeHUh?=
CAL-62 NHHj[I9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPsNnNKSzVyPUO2Mlg3KG6P NVTn[JBGW0GQR1XS
8-MG-BA MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fqVmlEPTB;M{euNlUhdk1? NUfnUGh5W0GQR1XS
8505C NV75U2hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFznVW9KSzVyPUO3MlUyKG6P NVOwXnp1W0GQR1XS
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CAL-39 NGX1VnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrQTWM2OD1|Nz65JI5O M2nHdnNCVkeHUh?=
MN-60 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nDXGlEPTB;M{euPVYhdk1? MmTKV2FPT0WU
RKO NXzs[4syT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrFXmRkUUN3ME2zPE4{OyCwTR?= NH3QSXZUSU6JRWK=
U251 Ml;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17WcWlEPTB;M{iuOFMhdk1? MX7TRW5ITVJ?
SJSA-1 NYjOe2lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXFXlhKSzVyPUO4MlU1KG6P MV7TRW5ITVJ?
CAL-12T NYfSbXo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorsTWM2OD1|OD62JI5O MnnTV2FPT0WU
HCC1419 Mn\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\ON2lEPTB;M{iuO|Ehdk1? M4O4THNCVkeHUh?=
CO-314 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTN6Lke0JI5O M4fXNHNCVkeHUh?=
LB1047-RCC MlXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW4[HVKSzVyPUO4MlgyKG6P NGTVVXlUSU6JRWK=
A101D MkTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH2TWM2OD1|OD65O{BvVQ>? MXnTRW5ITVJ?
MDA-MB-175-VII MkPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTN7LkWxJI5O M4TBTHNCVkeHUh?=
MZ2-MEL MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\wdWtKSzVyPUO5MlY3KG6P M3TGUXNCVkeHUh?=
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G-401 NVTMTIFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWX6Wo86UUN3ME20NE45OiCwTR?= MoriV2FPT0WU
HT MojpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPtTWM2OD12MT6wNkBvVQ>? Mn7TV2FPT0WU
8305C NEXueodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vvOmlEPTB;NEGuPFchdk1? NEjsPJJUSU6JRWK=
BHY M3vPemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr3TWM2OD12Mj63NkBvVQ>? NUH1Z4U{W0GQR1XS
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T-24 NU\oeo01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X4W2lEPTB;NEOuPFMhdk1? NIP6em9USU6JRWK=
EPLC-272H NWOyV|U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfGeWtlUUN3ME20OE4{QSCwTR?= MkfLV2FPT0WU
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NCI-H2452 NWXlWGtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnF[lZKSzVyPUS0MlU5KG6P M4Oyd3NCVkeHUh?=
KS-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LQfmlEPTB;NESuOlYhdk1? NIXafGJUSU6JRWK=
HD-MY-Z NYfF[Gt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPnXoRKSzVyPUS0MlkzKG6P M17LWnNCVkeHUh?=
KNS-62 NHzqXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTR3LkO4JI5O M3fFXHNCVkeHUh?=
NOMO-1 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7KUIRKSzVyPUS1Mlg4KG6P MlfOV2FPT0WU
SK-HEP-1 NEjxbXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\CTGlEPTB;NE[uNFQhdk1? NVO1U4RiW0GQR1XS
IGR-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDETWM2OD12Nj6xN{BvVQ>? M3rkUXNCVkeHUh?=
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LB996-RCC MojBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nKN2lEPTB;NEeuNVkhdk1? MWfTRW5ITVJ?
NCI-H1623 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TFZmlEPTB;NEeuO|Yhdk1? M2HsVXNCVkeHUh?=
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AGS MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\afmlEPTB;NEiuO|chdk1? Mn7oV2FPT0WU
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COR-L23 MmnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLyTWM2OD12OT6xOkBvVQ>? MnvPV2FPT0WU
D-283MED NGPZZ45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnX[lNXUUN3ME20PU43OSCwTR?= NH30UZBUSU6JRWK=
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SW620 M3\5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTVyLkO2JI5O MoLtV2FPT0WU
KYSE-140 NUTze2gyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13xWGlEPTB;NUCuOVUhdk1? MkixV2FPT0WU
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D-423MG M2HsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTV{LkC4JI5O NF;YW3ZUSU6JRWK=
SF539 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\nN5lQUUN3ME21Nk4{PSCwTR?= M3LKNHNCVkeHUh?=
RPMI-2650 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fRV2lEPTB;NUKuOlkhdk1? M{DpdXNCVkeHUh?=
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C32 MnLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTV|LkizJI5O NVfudlFCW0GQR1XS
GB-1 MkK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zLXmlEPTB;NUSuNkBvVQ>? M3vMPXNCVkeHUh?=
SNB75 NH:0V2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDYPGRQUUN3ME21OE4zPiCwTR?= MmDLV2FPT0WU
EM-2 MoTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrrZVJKSzVyPUW0MlQhdk1? NXLCS|VFW0GQR1XS
RH-1 NFK5S5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIKxSpdKSzVyPUW0Mlchdk1? Mm\EV2FPT0WU
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NCI-H2405 NEHLeHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTV2Lki4JI5O MVHTRW5ITVJ?
KYSE-450 NXvLbXY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL2TWM2OD13NT6xOkBvVQ>? NGi2cnJUSU6JRWK=
A704 Mn7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXaS3hsUUN3ME21OU42QSCwTR?= NWLFcVJmW0GQR1XS
HAL-01 Mo\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LiRWlEPTB;NUWuPFMhdk1? NV3VNnNDW0GQR1XS
TE-11 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrZdZBFUUN3ME21OU46QSCwTR?= M4fCXHNCVkeHUh?=
DOK NFvSVXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XObmlEPTB;NU[uNFIhdk1? MYHTRW5ITVJ?
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ML-2 NED3[|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrTTWM2OD14MD62NkBvVQ>? M1vqVHNCVkeHUh?=
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MEG-01 M2XZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M373Z2lEPTB;NkOuOVIhdk1? MWjTRW5ITVJ?
M059J NE[xS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTsVJpKSzVyPU[zMlU5KG6P MX\TRW5ITVJ?
LN-405 NXzVXVZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTZ|Lki1JI5O MnzSV2FPT0WU
NCI-H1581 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH3c3RKSzVyPU[0MlA{KG6P NH;i[|JUSU6JRWK=
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SW872 M2m3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHqTWM2OD14ND61O{BvVQ>? MWfTRW5ITVJ?
KYSE-510 NWjVWJRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTZ3Lke1JI5O M{PPfXNCVkeHUh?=
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TE-8 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLrTWM2OD14Nj61NkBvVQ>? MnzZV2FPT0WU
SCH NIf3fFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHIWppKSzVyPU[3MlEhdk1? NWHpcJZCW0GQR1XS
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KOSC-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnDVHJKSzVyPU[5Mlk4KG6P MYnTRW5ITVJ?
MC-IXC NHX0epVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTdyLkC4JI5O NEPYUG1USU6JRWK=
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RPMI-8866 MkjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTd{LkiyJI5O NV\lcYVrW0GQR1XS
OVCAR-4 M2DJS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojJTWM2OD15Mz6zOkBvVQ>? MWDTRW5ITVJ?
OAW-42 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTd|LkO5JI5O MVfTRW5ITVJ?
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S-117 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HtfmlEPTB;N{[uNlchdk1? MULTRW5ITVJ?
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CP50-MEL-B M{nJN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XVSWlEPTB;N{euOEBvVQ>? MnuyV2FPT0WU
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NCI-H1048 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jZb2lEPTB;OE[uN|Ehdk1? M{nMZXNCVkeHUh?=
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NCI-H2228 NGrj[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zFXWlEPTB;OEiuNlYhdk1? M3yy[HNCVkeHUh?=
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A431 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTh7Lkm3JI5O M37VNXNCVkeHUh?=
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HuCCT1 NIDCfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu5NnZFUUN3ME25NE44PiCwTR?= MVnTRW5ITVJ?
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CCRF-CEM NHTjeZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnnR49QUUN3ME2xOE44QDB7IN88US=> NF7DdVFUSU6JRWK=
ZR-75-30 NEXhdZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTMO4lKSzVyPUG2MlM{ODNizszN MmnyV2FPT0WU
A673 NYn1WnpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHyTWM2OD1{MD61OVA4KM7:TR?= NXPSWm82W0GQR1XS
K-562 NYnXbGhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PDe2lEPTB;MkiuOFE5OyEQvF2= NFzNSIdUSU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo試験 BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies. [1]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

In vitro Protein Kinase, PI3K, and mTOR Assays PI3Kα, β, and δ proteins are composed of the iSH2 domain of p85 NH2-terminally fused to the full-length protein p110 protein, with the exception of α that also does not contain the last 20 amino acids. PI3Kγ is produced as full-length protein deleted for its first 144 amino acids. All constructs are fused to a COOH-terminal His tag for convenient purification and then cloned into the pBlue-Bac4.5 (for α, β, and δ isoforms) or pVL1393 (for γ isoform) plasmids. The different vectors are then cotransfected with BaculoGold WT genomic DNA using methods recommended by the vendor for production of the respective recombinant baculoviruses and proteins. BEZ235 are tested for their activity against PI3K using a Kinase-Glo assay. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 μL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate (l-α-phosphatidylinositol; Avanti Polar Lipids; prepared in 3% octyl-glucoside) and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110δ, and p110γ, respectively) are then added to it. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and is incubated for either 60 (for p110α, p110β, and p110δ) or 120 min (for p110γ). It is terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection.

細胞アッセイ:

[2]

細胞株 HCT116, DLD-1 and SW480 cells
濃度 0-1 μM
反応時間 48 hours
実験の流れ

The human CRC cell lines, HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) and isogenic DLD-1 PIK3CA mutant as well as wild-type cells are maintained in DMEM with 10% FBS and 1 × Penicillin/Streptomycin. Cells are plated at different initial densities (HCT116: 3 × 103 cells/well, DLD-1: 5.5 × 103 cells/well, SW480: 4.5 × 103 cells/well, DLD-1 PIK3CA mutant: 7 × 103 cells/well, and DLD-1 PIK3CA wild-type: 9 × 103 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235, and the drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96® AQueous One Solution Cell Proliferation Assay, as per the manufacturer's instructions. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. For western blot analysis, cells are plated with zero or maximum inhibitory dose (500 nM) BEZ235 for 2, 6, 24, or 48 hours.

動物実験:

[1]

動物モデル Female Harlan athymic nude mice
製剤 NMP/polyethylene glycol 300 (10/90, v/v)
投薬量 45 mg/kg
投与方法 p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download BEZ235 (NVP-BEZ235, Dactolisib) SDF
分子量 469.55
化学式

C30H23N5O

CAS No. 915019-65-7
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMF 18 mg/mL warming (38.33 mM)
DMSO 0.01 mg/mL (0.02 mM)
Water <1 mg/mL
In vivo NMP+polyethylene glycol 300 (10+90, v+v) 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 2-methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile

文献中の引用 (80)

Frequently Asked Questions

  • Question 1
    With difficulties in dissolving BEZ235, How can I improve its solubility?

    Answer: For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve BEZ235 in NMP as more as possible. You can sonicate and warm it in water bath for a while. Then dilute with PEG 300.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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