Dactolisib (BEZ235)

For research use only. Not for use in humans.

目录号:S1009 别名: NVP-BEZ235 中文名称:达克利司

Dactolisib (BEZ235) Chemical Structure

CAS No. 915019-65-7

Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。

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RMB 2530.71 现货
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客户使用Selleck生产的Dactolisib (BEZ235)发表文献369篇:

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3KmTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。
靶点
p110α [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
mTOR (p70S6K) [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
ATR [8]
(3T3TopBP1-ER cells)
4 nM 5 nM 6 nM 7 nM 21 nM
体外研究

BEZ235显著降低mTOR活化的激酶p70S6K的磷酸化水平。BEZ235导致S235/S236P-RPS6水平减少,IC50为6.5 nM。BEZ235抗mTOR的活性使用生化mTOR K-LISA试验测定,IC50为20.7 nM。BEZ235对其β旁系同源物的活性稍弱,IC50为75 nM。在人肿瘤细胞中,PI3K/Akt/mTOR通路经常被组成性活化。BEZ235阻断PI3K和mTOR激酶活性,通过结合于这些酶的ATP结合槽发挥作用。用逐渐增加浓度BEZ235处理PTEN-null细胞系PC3M和U87MG时,导致细胞增殖剂量依赖性减少,平均GI50为10-12 nM。[1] BEZ235是一种mTORC1/2催化抑制剂。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Trypanosoma brucei brucei MlfVRY51cW2rY4LvZolidCCDc4PhfS=> MkTzNVghcA>? NGjxUplFVVOR NH:3UnFCdnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JJdqfGhiRVO1NEBw\iByLkCwNlUh|ryP MYKyOFgxPTl2Nh?=
MCF7 M1fQbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LYbVAvODFvMUCwJO69VQ>? Mly4OFghcA>? M3PMcGROW09? MYDJR|UxRTBwN{Og{txO MV2yN|g4OTlyNB?=
HCT116 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M361OlAvODFvMUCwJO69VQ>? NUHiUmlUPDhiaB?= M1PT[2ROW09? MWrJR|UxRTFwMU[g{txO M1fTdFI{QDdzOUC0
U87MG NED3dVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{G1UlAvODFvMUCwJO69VQ>? NFvhV4E1QCCq NVK1RpJyTE2VTx?= MlrrTWM2OD1zLkOyJO69VQ>? NXThXGNbOjN6N{G5NFQ>
HBC4 M1zHU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrwNE4xOS1zMECg{txO NUj0cYZ6PDhiaB?= M1\Kb2xw\yCJSUWwQU05NjZzIF2= M1fSUVIzOzN4MkS2
BSY1 Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TSdlAvODFvMUCwJO69VQ>? MUG0PEBp MoW5UI9oKEeLNUC9MVgvPDhiTR?= MlOwNlI{OzZ{NE[=
HBC5 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVntOnFMOC5yMT2xNFAh|ryP M3jGXlQ5KGh? MoHGUI9oKEeLNUC9MVcvQDdiTR?= MYmyNlM{PjJ2Nh?=
MCF7 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NES2N5gxNjBzLUGwNEDPxE1? M3j4clQ5KGh? MUnMc4chT0l3ME2tPE4yPiCP M4jPb|IzOzN4MkS2
MDA-MB-231 MkfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHDNE4xOS1zMECg{txO NFHMPYI1QCCq MVPMc4chT0l3ME2tPE4xQSCP M1z3[FIzOzN4MkS2
U251 Mo\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2wMlAyNTFyMDFOwG0> M4nWeFQ5KGh? NYPSOJhyVG:pIFfJOVA:NTdwNk[gUS=> MnfvNlI{OzZ{NE[=
SF268 NWj3[nFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMlAyNTFyMDFOwG0> NV\wc3N2PDhiaB?= NWTiOHFjVG:pIFfJOVA:NTdwOUKgUS=> NH;oZ5ozOjN|NkK0Oi=>
SF295 M1zvOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKwMlAyNTFyMDFOwG0> NV7nSnhYPDhiaB?= NHe2PXhNd2diR1m1NF0uQC5|MTDN MUeyNlM{PjJ2Nh?=
SF539 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPtV3N3OC5yMT2xNFAh|ryP M{LjXFQ5KGh? Mnv3UI9oKEeLNUC9MVgvPTliTR?= NETlN3MzOjN|NkK0Oi=>
SNB75 NYDONGoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnJ[XI2OC5yMT2xNFAh|ryP M{P2eFQ5KGh? Mn63UI9oKEeLNUC9MVgvPThiTR?= MlixNlI{OzZ{NE[=
SNB78 NWez[VZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPZfFFDOC5yMT2xNFAh|ryP M{PCfFQ5KGh? M1H5NWxw\yCJSUWwQU05NjZ3IF2= M3K1NVIzOzN4MkS2
HCC2998 NI\NeIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7ON2k5OC5yMT2xNFAh|ryP MYS0PEBp NE\FW4dNd2diR1m1NF0uQC5yNTDN NH\GNYEzOjN|NkK0Oi=>
KM12 NGLFdlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF61SmcxNjBzLUGwNEDPxE1? M3rmNlQ5KGh? NHTsUJhNd2diR1m1NF0uPy53NDDN NXS3[oFROjJ|M{[yOFY>
HT-29 NX7kTVZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqwMlAyNTFyMDFOwG0> MXu0PEBp MorVUI9oKEeLNUC9MVcvPzViTR?= Mn3uNlI{OzZ{NE[=
HCT15 MmntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3e2cFAvODFvMUCwJO69VQ>? NGSzc5c1QCCq M2qwbWxw\yCJSUWwQU05NjB|IF2= NF\nc48zOjN|NkK0Oi=>
HCT116 MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInlOmgxNjBzLUGwNEDPxE1? M3jnS|Q5KGh? NGPBTlNNd2diR1m1NF0uPy54MTDN NIKySmkzOjN|NkK0Oi=>
NCI-H23 NFe0O4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjmfJMxNjBzLUGwNEDPxE1? NXuxRZE6PDhiaB?= NUDFXoU3VG:pIFfJOVA:NTdwNkSgUS=> NHT2bpczOjN|NkK0Oi=>
NCI-H226 NG[3V5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWwMlAyNTFyMDFOwG0> NWqx[Yo5PDhiaB?= M1rGOmxw\yCJSUWwQU05NjR2IF2= NFm0UpYzOjN|NkK0Oi=>
NCI-H522 M{TqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGwMlAyNTFyMDFOwG0> M1LNR|Q5KGh? MorlUI9oKEeLNUC9MVgvPDViTR?= MXuyNlM{PjJ2Nh?=
NCI-H438 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DD[lAvODFvMUCwJO69VQ>? MnnYOFghcA>? MW\Mc4chT0l3ME2tPE4yOSCP MmP4NlI{OzZ{NE[=
A549 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPKcoVuOC5yMT2xNFAh|ryP M{myc|Q5KGh? NEX4Z5RNd2diR1m1NF0uQC5yNzDN NWLxUGdUOjJ|M{[yOFY>
DMS273 M{X1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvCNE4xOS1zMECg{txO M2LMZVQ5KGh? MX3Mc4chT0l3ME2tO{45OCCP MkThNlI{OzZ{NE[=
DMS114 NX\RXY95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LPd|AvODFvMUCwJO69VQ>? MnLXOFghcA>? NX7kdokzVG:pIFfJOVA:NThwM{mgUS=> Ml3QNlI{OzZ{NE[=
LOXIMVI MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWwMlAyNTFyMDFOwG0> NH;rVmc1QCCq M4TESWxw\yCJSUWwQU05NjZ4IF2= MojmNlI{OzZ{NE[=
OVCAR3 NYfqdYNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnYWnR[OC5yMT2xNFAh|ryP MnPpOFghcA>? M2fHWWxw\yCJSUWwQU05NjF5IF2= NEWwdXQzOjN|NkK0Oi=>
OVCAR4 M2Hmdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOwMlAyNTFyMDFOwG0> NWLIc|N3PDhiaB?= MXPMc4chT0l3ME2tPE42QCCP M164OVIzOzN4MkS2
OVCAR5 NUPqd5dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWiwMlAyNTFyMDFOwG0> NILrbYY1QCCq MVXMc4chT0l3ME2tO{42PyCP M{XreFIzOzN4MkS2
OVCAR8 NGXaSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnLNE4xOS1zMECg{txO NXHKSFdwPDhiaB?= Ml3nUI9oKEeLNUC9MVcvQDRiTR?= NHr6[2EzOjN|NkK0Oi=>
SKOV3 M1e5NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV6wMlAyNTFyMDFOwG0> MlHwOFghcA>? M4TBeGxw\yCJSUWwQU05NjRzIF2= MXKyNlM{PjJ2Nh?=
RXF631L NH\LUplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf4fZMxNjBzLUGwNEDPxE1? NYXG[VZJPDhiaB?= MWnMc4chT0l3ME2tPE4zOSCP MmDXNlI{OzZ{NE[=
ACHN MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn2wNE4xOS1zMECg{txO Mlr5OFghcA>? Mo[0UI9oKEeLNUC9MVcvQTViTR?= MkXmNlI{OzZ{NE[=
St-4 NVfkToxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzZT3YxNjBzLUGwNEDPxE1? NETMXJY1QCCq NYDsXo9kVG:pIFfJOVA:NTdwNEegUS=> NG[0V3gzOjN|NkK0Oi=>
MKN1 NVjGeJk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[wMlAyNTFyMDFOwG0> NHG2bWo1QCCq MYPMc4chT0l3ME2tPE41OSCP MVGyNlM{PjJ2Nh?=
MKN7 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfoNE4xOS1zMECg{txO MVq0PEBp Mn;TUI9oKEeLNUC9MVcvPjhiTR?= M4LleFIzOzN4MkS2
MKN28 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX60VmdCOC5yMT2xNFAh|ryP NXTXVJRXPDhiaB?= MY\Mc4chT0l3ME2tO{4xPyCP M1P5SVIzOzN4MkS2
MKN45 M4rMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LLTFAvODFvMUCwJO69VQ>? MW[0PEBp M4D0c2xw\yCJSUWwQU05NjN2IF2= NFTsRm4zOjN|NkK0Oi=>
MKN74 M2XuVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGP6SIsxNjBzLUGwNEDPxE1? NITpVnU1QCCq NHTkVmhNd2diR1m1NF0uPy52MjDN M{OxNVIzOzN4MkS2
DU145 NGfUbItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPkNE4xOS1zMECg{txO NHftfpE1QCCq NVi0NIFbVG:pIFfJOVA:NThwMU[gUS=> M4HaR|IzOzN4MkS2
PC3 NWXsNoR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\1U4djOC5yMT2xNFAh|ryP NXfEbXBQPDhiaB?= NYXjS|ZOVG:pIFfJOVA:NThwNk[gUS=> NWDiPHczOjJ|M{[yOFY>
Trypanosoma brucei brucei M1;Be2Z2dmO2aX;uJGF{e2G7 NIqyc2kzODBibl2= NXuxXXNxOTJiaB?= MWDEUXNQ NET3W2dF\WO{ZXHz[UBqdiCyaH;zdIhwfGmmeXygbY5we2m2b3ygdIhwe3CqYYTlJIxmfmWu MmD3NlQ5ODV7NE[=
Trypanosoma brucei brucei MYjGeY5kfGmxbjDBd5NigQ>? NHfQUYUyQCCq NYC0dINrTE2VTx?= MXzJcohq[mm2aX;uJI9nKHKnY3XweI9zNW2nZHnheIVlKGWwZH;jfZRwe2m|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKHS{YX7z[oVzemmwIIXweIFs\Q>? Mlv1NlQ5ODV7NE[=
Trypanosoma brucei brucei MneySpVv[3Srb36gRZN{[Xl? NF72UIgzODBibl2= MkDwNVIhcA>? MmqxSG1UVw>? NVryeZdoTW[oZXP0JI9vKHOyaHnu[49ugWynaX6gcIV3\Wx? NUHmVpNjOjR6MEW5OFY>
Trypanosoma brucei brucei M1L0O2Z2dmO2aX;uJGF{e2G7 NWm2XnlqOjByIH7N NUL6SGdtOTJiaB?= M{PGe2ROW09? NUPjcHZLTW[oZXP0JI9vKHCqb4PwbIF1cWS7bHPoc4xqdmVibHX2[Yw> MWCyOFgxPTl2Nh?=
UM-UC-3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Sz[mlEPTB;M{G1JJBO M4HKZnNCVkeHUh?=
SBC-1 NWTLdnlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkKwTWM2OD15NEKgdG0> M3rRNXNCVkeHUh?=
MKN1 MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrETWM2OD1{Lkigcm0> NF71WmNUSU6JRWK=
NCI-H720 M2LmZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHTTWM2OD1|LkW3JI5O MojhV2FPT0WU
BFTC-909 NXy0cI52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHMenhKSzVyPUOuO|Ehdk1? NV\hZ|lLW0GQR1XS
BPH-1 Mlv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3yeVBTUUN3ME20Mlc3KG6P NIXje21USU6JRWK=
PC-3 NVH1[YJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW1TWM2OD13LkC5JI5O MVnTRW5ITVJ?
AN3-CA NGrQd3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTVwNU[gcm0> MVLTRW5ITVJ?
HN MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLTWVAzUUN3ME21Mlk3KG6P NUm3ZXM5W0GQR1XS
HCC2218 NYXSSWhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPS[ZZtUUN3ME22MlYyKG6P NIj2UI5USU6JRWK=
KP-4 NUDibmZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnNSmlFUUN3ME23JI5O NGnZbJBUSU6JRWK=
LU-139 MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUj6eFlHUUN3ME23Mlc4KG6P Mo[5V2FPT0WU
ETK-1 MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTdwOEigcm0> NHnCTFZUSU6JRWK=
Ramos-2G6-4C10 M2C2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRThwNEmgcm0> M2nWdXNCVkeHUh?=
MHH-PREB-1 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfrTWM2OD17LkGyJI5O NHf2N4xUSU6JRWK=
DU-4475 NXzZ[Y93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofSTWM2OD17LkS0JI5O M4[yUHNCVkeHUh?=
NCI-H1666 M2nZRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS2RXAyUUN3ME25MlcyKG6P M{fQT3NCVkeHUh?=
CAMA-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jremlEPTB;OT64JI5O MXvTRW5ITVJ?
TYK-nu M1OwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\Xc2lEPTB;OT65OEBvVQ>? NIixRlRUSU6JRWK=
MFE-280 NGTQTIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVT0bFdtUUN3ME25Mlk6KG6P M{\wUXNCVkeHUh?=
A549 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFyLkG0JI5O MnnEV2FPT0WU
769-P Mne1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkWwTWM2OD1zMD60OEBvVQ>? NInOZoxUSU6JRWK=
L-363 NVPo[ZNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HDVWlEPTB;MUCuOlkhdk1? NHr2cGNUSU6JRWK=
ES8 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrkeJZwUUN3ME2xNE46KG6P MYHTRW5ITVJ?
PA-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDkTWM2OD1zMT64NkBvVQ>? NHXxelZUSU6JRWK=
Mewo Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDsTY5KSzVyPUGxMlk6KG6P M4nadnNCVkeHUh?=
HSC-3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\nfGlEPTB;MUKuNlEhdk1? NFT6VpJUSU6JRWK=
H4 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTF{Lk[3JI5O MW\TRW5ITVJ?
BB65-RCC MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zHUGlEPTB;MUKuO|Ihdk1? M3nLVXNCVkeHUh?=
NCI-H1793 Mk\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV6zOXAzUUN3ME2xNk45OiCwTR?= M4DZUHNCVkeHUh?=
KARPAS-45 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDQcWZCUUN3ME2xN{42OSCwTR?= MnjIV2FPT0WU
GCT MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmT3TWM2OD1zMz62PEBvVQ>? NWDzcFNGW0GQR1XS
EoL-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXiTWM2OD1zMz65N{BvVQ>? MX3TRW5ITVJ?
LB2241-RCC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPqTWM2OD1zND6wNUBvVQ>? MkPzV2FPT0WU
ES5 NGfJPI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF2Lke0JI5O NF;oU5ZUSU6JRWK=
LOXIMVI NXrlbZNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnad2tvUUN3ME2xOE46QSCwTR?= NWnxcHRnW0GQR1XS
COR-L105 M1nUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHPV3dKSzVyPUG1MlA1KG6P MVvTRW5ITVJ?
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