Copanlisib (BAY 80-6946)

For research use only. Not for use in humans.

目录号:S2802 中文名称:库潘尼西

Copanlisib (BAY 80-6946) Chemical Structure

CAS No. 1032568-63-0

Copanlisib (BAY 80-6946)是一个高效的泛I型 PI3K抑制剂,其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3。

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客户使用Selleck生产的Copanlisib (BAY 80-6946)发表文献31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 Copanlisib (BAY 80-6946)是一个高效的泛I型 PI3K抑制剂,其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3。
靶点
PI3Kα [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
0.5 nM 0.7 nM 3.7 nM 6.4 nM
体外研究

BAY 80-6946是PI3K抑制剂,具有抗肿瘤活性。BAY 86-9766抑制HuCCT-1 (KRASG12D) 和EGI-1 (KRASG12D) 细胞系增殖,IC50分别为147 nM 和137 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 MXTHdo94fGhiaX7obYJqfG:wIHHzd4F6 M2DFZVExOCCwTR?= MWfDc5Bidmyrc3niJIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdHXkJINmdGxiZ4Lve5RpKGmwII\peJJwNiCLQ{WwQVQ4Njlibl2u M3S5NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[yPVUzLz5|MEm2Nlk2OjxxYU6=
HepG2 NHHpU2NIem:5dHigbY5pcWKrdH;uJIF{e2G7 M2rGS|ExOCCwTR?= MX3Dc5Bidmyrc3niJIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdHXkJINmdGxiZ4Lve5RpKGmwII\peJJwNiCLQ{WwQVMyNjZibl2u NYHZWGZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlI6PTJpPkOwPVYzQTV{PD;hQi=>
Hep3B NYP2WJJET3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= NYjaW3NmUUN3ME23Nk41KG6P MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl4Mkm1Nkc,OzB7NkK5OVI9N2F-
PLCPRF5 NF\abINIem:5dHigbY5pcWKrdH;uJIF{e2G7 Mn\xTWM2OD1{OEOgcm0> NELVdJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
Chang Mlm2S5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? M2HiS2lEPTB;NESyJI5O MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl4Mkm1Nkc,OzB7NkK5OVI9N2F-
JVM-3 M3zwUWZ2dmO2aX;uJIF{e2G7 Mn3UOFghcA>? NFLZW4VqdmirYnn0d{Bu\XSjYn;sbYMh[WO2aY\peJkhf2m2aDDhckBKSzVyIH;mJFIh|ryPIHnuJJRp\SC[VGSgZZN{[Xl? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzMk[zOUc,OjV7MUK2N|U9N2F-
BT-474 MnrUSpVv[3Srb36gZZN{[Xl? NYTyd3pNPTBibl2= NYj4XphXOC53LDCyMEA1NCB6LDCyOEBp M1TxXJJieGmmbImgbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHM1PzNuIGSzNFgqKGG|IIflcIwh[XNiaYTzJIRqemWldDDzeYJ{fHKjdHXzJHBTSVN2MDCoWFI1PiliYX7kJGdUUzQQsjCoV|kqNCCjbnSgbY5pcWKrdHnvckB4[XNic4XzeIFqdmWmIH\vdkB2eCC2bzCyOEBpd3W{cx?= NUDvdHZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
SK-BR-3 NV;LdGFVTnWwY4Tpc44h[XO|YYm= M4rpVVAtKDFuIEKsJFQhcA>? NVnPe|Bb\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MnTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
UACC-893 MlTkSpVv[3Srb36gZZN{[Xl? M33Cd|AtKDFuIEKsJFQhcA>? NIjkSZZld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NFP3TXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
HCC-1954 NYHGNFczTnWwY4Tpc44h[XO|YYm= M1fYNFAtKDFuIEKsJFQhcA>? Monn[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NFfrbpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
MDA-MB-453 MVvGeY5kfGmxbjDhd5NigQ>? M3zYelAtKDFuIEKsJFQhcA>? M4SwO4Rwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NGW5U289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
MDA-MB-361 NYDVeWdnTnWwY4Tpc44h[XO|YYm= Mnm0NEwhOSxiMjygOEBp Mofy[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NVHt[mRPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
BT-20 MnXXSpVv[3Srb36gZZN{[Xl? MVWwMEAyNCB{LDC0JIg> MVfkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MmnHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
MCF-7 MXXGeY5kfGmxbjDhd5NigQ>? NFvLXG8xNCBzLDCyMEA1KGh? MlXZ[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
T-47D NV\GRXNnTnWwY4Tpc44h[XO|YYm= NXXJNIlUOCxiMTygNkwhPCCq NF2ye2Vld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
HCC1806 NX3nPYdyTnWwY4Tpc44h[XO|YYm= NVH5RYZ3OCxiMTygNkwhPCCq M1nMUYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MofUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
NCI-H292 NYn6PYN6TnWwY4Tpc44h[XO|YYm= MkfINEwhOSxiMjygOEBp NFr1d4Jld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
NCI-H1650 MUDGeY5kfGmxbjDhd5NigQ>? NHqzW2cxNCBzLDCyMEA1KGh? Mlr1[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NYi3TWZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
CCRF-SB NXn6THJnTnWwY4Tpc44h[XO|YYm= MVmwMEAyNCB{LDC0JIg> NYrWco9r\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NVTXVnR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
U937 MnLqSpVv[3Srb36gZZN{[Xl? MXKwMEAyNCB{LDC0JIg> NV2zS|F1\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
SU-DHL-4 M2ja[GZ2dmO2aX;uJIF{e2G7 NYO3TYdqOCxiMTygNkwhPCCq MYTkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
SU-DHL-5 MmrTSpVv[3Srb36gZZN{[Xl? NF3zdWkxNCBzLDCyMEA1KGh? MVvkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NGLWb209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
HCT116 MoO0SpVv[3Srb36gZZN{[Xl? MUWwMEAyNCB{LDC0JIg> NH3pVmtld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NX3obGl3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
A549 cells NVzBeWNNTnWwY4Tpc44h[XO|YYm= M1fNZ|AtKDFuIEKsJFQhcA>? M4KzOIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NUez[opkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
SK-MEL-30 NYTBT|E2TnWwY4Tpc44h[XO|YYm= MY[wMEAyNCB{LDC0JIg> NUjwfW5x\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NYrQV2NTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
SK-MEL-2 cells MnHKSpVv[3Srb36gZZN{[Xl? NV\0NJZkOCxiMTygNkwhPCCq NYHyOnV2\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
NCI-H1703 NFm0fGlHfW6ldHnvckBie3OjeR?= NUS0SGVXOCxiMTygNkwhPCCq NIrocZRld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NFHqVWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
NCI-H661 MV3GeY5kfGmxbjDhd5NigQ>? NFj6ZlkxNCBzLDCyMEA1KGh? NYDDdVhv\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= Mn;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
PC9 M17JR2Z2dmO2aX;uJIF{e2G7 MXywMEAyNCB{LDC0JIg> MV7kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NWHPOIE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
TC32 M4rWbpFJXFNiYYPzZZk> MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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Saos-2 NGTnN2FyUFSVIHHzd4F6 MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NI\SNHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MoHSdWhVWyCjc4PhfS=> NH3VVYVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MnfIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NFvxNlVyUFSVIHHzd4F6 M3jPcpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= M2fSRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NV\DRWIzeUiWUzDhd5NigQ>? NGTi[IxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 MnT3dWhVWyCjc4PhfS=> NYO2XY5GeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NEPjVlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M2rU[pFJXFNiYYPzZZk> NUDqfoFleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= M2q5OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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BT-37 NX:zTYNIeUiWUzDhd5NigQ>? NWPj[|NieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? Ml7vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NIHycIFyUFSVIHHzd4F6 M1X5bpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG1IKDZ|IDi2MXRIKFJrIHPlcIx{ NVf6eFZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30 NXzSNlhPeUiWUzDhd5NigQ>? M1e5cpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOzBiY3XscJM> NV3qe|ZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M4DnNZFJXFNiYYPzZZk> NVHyXW86eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 MmixdWhVWyCjc4PhfS=> NUDTVmlCeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> M1q4flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NYO3RYxNeUiWUzDhd5NigQ>? NFSzV25yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NVK2fZV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 M2Xn[ZFJXFNiYYPzZZk> M3;6WZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 NFO4ZmNyUFSVIHHzd4F6 MlPCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| Mn3wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 MV7xTHRUKGG|c3H5 M3Pa[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| NF3VcJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 Mk\kdWhVWyCjc4PhfS=> NEnBcXlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSjF4NEOgZ4VtdHN? M3zMb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MoPkdWhVWyCjc4PhfS=> MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ NFKzVZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 NF33d45yUFSVIHHzd4F6 NFnBblFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| NXnQN2ttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 NX7TR456eUiWUzDhd5NigQ>? MnrLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=> MnHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 NY\KUYd4eUiWUzDhd5NigQ>? MlvtdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVogyQCClZXzsdy=> MnrDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NGLPU|ByUFSVIHHzd4F6 NUHtN49neUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NXjlfVNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-PRAS40(T246) / p-GSK3β(S9) / cleaved caspase-3 / cleaved caspase-7 / PI3K-p85; 

PubMed: 24436048     


BT-474 cells were treated with BAY 80-6946 (50nM) or MK2206 (2μM) and collected at indicated times. Immunoblots of AKT, AKT substrates, and surrogates for apoptosis show similar AKT inhibition but greater apoptosis with PI3K inhibition.

p-FoxO4(T28) / p-S6(S235/236) / p-4E-BP1(S65) / p-4E-BP1(T37/46) / p-HER3(Y1197) / HER3 / p-IGF1Rβ/ IGF1R / p-HER2 / p-EGFR / p-STAT3 / p-ERK; 

PubMed: 24436048     


BT-474 cells were treated with BAY 80-6946 (50nM) or MK2206 (2μM) and collected at indicated times. Immunoblots of AKT and mTOR substrates, RTKs, and parallel pathways like STAT and ERK.

24436048
Growth inhibition assay
Cell viability; 

PubMed: 24436048     


BT-474 cells were treated with DMSO, MK2206 (2μM), or BAY 80-6946 (50nM) and viable cells were counted at indicated times, demonstrating loss in viable cell number with PI3K inhibition. Results were reported as a mean of triplicate with standard errors.

24436048
体内研究 BAY 80-6946 耐受性良好,MTD(最大耐受剂量)为0.8 mg/kg。PK(药代动力学)研究结果支持每周给药。按MTD处理,在第一个24小时期间出现2/3级高血糖。PK, 临床SD和FDG-PET 数据与有效处理和PI3K 通路抑制情况一致。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

PI3Kα和PI3Kβ放射性脂质激酶检测:

p110α生化检测是一种放射性测定,测量33P渗透进p110α底物磷脂酰肌醇(PI)的程度。His标记的N-末端截短的(ΔN 1-108) p110α和同样截短的缺乏p85结合域的p110β(ΔN 1-108) 蛋白在Sf9细胞中表达,且纯化到50%以上纯度。为了获得 IC50值,使用 MaxiSorp 板在以下条件下在384孔板中进行反应。每孔使用2 μg在氯仿稀释的摩尔比为1:1的磷脂酰肌醇(PI)和磷脂酰丝氨酸(PS)包被实验板。将实验板置于通风橱中过夜,蒸发有机溶液。将实验板密封在4°C贮存1个月。每孔加入7.5 ng截短的p110α蛋白,每孔中含9 μL 实验 buffer (50mM MOPSO pH 7.0,100 mM NaCl, 4mM MgCl2, 0.1%(w/v)BSA),除了对照组只含实验 buffer。1μL 溶于DMSO的实验化合物从稀释液中转移,获得8点剂量反应 (0.0, 0.003, 0.01, 0.03, 0.1, 0.3, 1.0, 3.0 和 10 μM 终浓度BAY化合物)。加入含 20 μCi/mL [γ-33P]-ATP 的40 μM ATP 溶液开始反应,反应在室温下温和混合进行2小时。 加入 5μL 25 mM EDTA储存液终止反应。不使用洗涤剂清洗实验板,而使用384孔实验板洗涤器,然后每孔加入25μL UltimaGold 闪烁使用BetaPlate液体闪烁计数器测定渗透进固定化PI底物的放射性。
细胞实验:[2]
- 合并
  • Cell lines: KPL4, BT474, T47D, BT20, MCF7, MDA-MB-468, SK-Br-3, LNCaP, PC3, Colo205, HT29, HCT116, A549, H460, U87MG, 786O.
  • Concentrations: 0.0, 0.003, 0.01, 0.03, 0.1, 0.3, 1.0, 3.0 和 10 μM
  • Incubation Time: 72 小时
  • Method: 药物处理72小时后,使用Cell Titer-Glo 发光法细胞活力检测试剂盒测定细胞增殖。细胞按每孔500-1000个细胞接种到 384孔板中,孔中含 25 μL 生长培养基。对于每种细胞系的测定,细胞接种到单独的实验板上,在t=0小时和t=72小时测定发光值。在37°C下温育过夜,每孔加入25μL Cell Titer-Glo 溶液测定t=0时样品的发光值,转移实验板到摇床上,在室温下进行10分钟,然后使用发光检测仪(最大光检测在428 nm处测定)在Wallac Victor2 1420 Multilable HTS计数板上对实验板进行读数。使用在生长培养基中稀释的化合物(终体积为30 μL)处理t=72小时的剂量板。细胞在37°C下温育72小时。每孔加入30μL Cell Titer-Glo溶液测定t=72小时样品的发光值,然后将细胞置于摇床上在室温下进行10分钟,然后使用Victor发光检测仪读读取发光值。进行数据处理,实验组和对照组中t=72小时发光值减去t=0时发光值。实验组和对照组的发光值百分比差异用来测定生长抑制百分数。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: Rats bearing KPL4 or HCT116 xenografts
  • Dosages: 6 mg/kg
  • Administration: i.v.
    (Only for Reference)

溶解度 (25°C)

体外 1 mg/mL (2.08 mM)
Ethanol 0.01 mg/mL (0.02 mM)
DMSO 0.002 mg/mL (0.0 mM)

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 480.52
化学式

C23H28N8O4

CAS号 1032568-63-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05082025 Not yet recruiting Drug: Copanlisib|Drug: fulvestrant Endometrial Cancer|Ovarian Cancer M.D. Anderson Cancer Center|Bayer February 28 2022 Phase 2
NCT04939272 Not yet recruiting Drug: Copanlisib Hydrochloride|Drug: Venetoclax Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma City of Hope Medical Center|National Cancer Institute (NCI) December 15 2021 Phase 1|Phase 2
NCT04572763 Recruiting Drug: Copanlisib|Drug: Venetoclax Diffuse Large B Cell Lymphoma|Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma Dana-Farber Cancer Institute|AbbVie|Bayer September 8 2021 Phase 1|Phase 2
NCT04803123 Recruiting Drug: Copanlisib Leukemia Acute Lymphocytic Dorothy Sipkins MD PhD|Bayer|Duke University June 21 2021 Early Phase 1
NCT04431635 Recruiting Drug: Copanlisib|Drug: Nivolumab|Drug: Rituximab Indolent Lymphoma Big Ten Cancer Research Consortium June 15 2020 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID