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25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 MljaS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? NVX0O3Y4OTByIH7N NVSwXGZ5S2:yYX7sbZNq[iCmb4PlMYRmeGWwZHXueIx6KGmwaHnibZRm\CClZXzsJIdzd3e2aDDpckB3cXS{bz6gTWM2OD12Nz65JI5ONg>? MoT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NkK5OVIoRjNyOU[yPVUzRC:jPh?=
HepG2 NH:2VnRIem:5dHigbY5pcWKrdH;uJIF{e2G7 MV2xNFAhdk1? M2T3NmNweGGwbHnzbYIh\G:|ZT3k[ZBmdmSnboTsfUBqdmirYnn0[YQh[2WubDDndo94fGhiaX6geol1em9wIFnDOVA:OzFwNjDuUU4> M371fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[yPVUzLz5|MEm2Nlk2OjxxYU6=
Hep3B M4LNcWdzd3e2aDDpcohq[mm2b36gZZN{[Xl? NED0NIdKSzVyPUeyMlQhdk1? NXjDVJJJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlI6PTJpPkOwPVYzQTV{PD;hQi=>
PLCPRF5 MUjHdo94fGhiaX7obYJqfG:wIHHzd4F6 NFHuXXFKSzVyPUK4N{BvVQ>? M3y0[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[yPVUzLz5|MEm2Nlk2OjxxYU6=
Chang NIrDdJdIem:5dHigbY5pcWKrdH;uJIF{e2G7 NWP4RYtVUUN3ME20OFIhdk1? NHfpd3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
JVM-3 M3Xq[WZ2dmO2aX;uJIF{e2G7 M3n4[VQ5KGh? M{n6bIlvcGmkaYTzJI1mfGGkb3zpZ{Bi[3Srdnn0fUB4cXSqIHHuJGlEPTBib3[gNkDPxE1iaX6geIhmKFiWVDDhd5NigQ>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzMk[zOUc,OjV7MUK2N|U9N2F-
BT-474 NV;vTnJuTnWwY4Tpc44h[XO|YYm= Ml;BOVAhdk1? M17XdFAvPSxiMjygOEwhQCxiMkSgbC=> NEfWNGpz[XCrZHz5JIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhUPDd|LDDUN|A5MSCjczD3[YxtKGG|IHn0d{BlcXKnY4Sgd5Vje3S{YYTld{BRWkGVNECgLHQzPDZrIHHu[EBIW0t|zsKgLHM6MSxiYX7kJIlvcGmkaYTpc44hf2G|IIP1d5RicW6nZDDmc5IhfXBidH:gNlQhcG:3coO= Mli3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
SK-BR-3 MkLWSpVv[3Srb36gZZN{[Xl? MmDpNEwhOSxiMjygOEBp Mkew[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
UACC-893 M4nzeWZ2dmO2aX;uJIF{e2G7 NVnlTVA5OCxiMTygNkwhPCCq MWfkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NV7XU|lORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
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MDA-MB-453 NEL3e|dHfW6ldHnvckBie3OjeR?= MnX6NEwhOSxiMjygOEBp MojL[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NEDXRWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
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NCI-H292 MULGeY5kfGmxbjDhd5NigQ>? NGHvbIsxNCBzLDCyMEA1KGh? M2fhTIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NHPQ[Jo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
NCI-H1650 MlXtSpVv[3Srb36gZZN{[Xl? MVGwMEAyNCB{LDC0JIg> MYXkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NXXhZ2hFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
CCRF-SB NHTvSJZHfW6ldHnvckBie3OjeR?= NVnNTY5xOCxiMTygNkwhPCCq M1rSVoRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
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HCT116 NESyXGtHfW6ldHnvckBie3OjeR?= Ml\tNEwhOSxiMjygOEBp MoL2[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
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SK-MEL-2 cells M2S4fmZ2dmO2aX;uJIF{e2G7 MkfKNEwhOSxiMjygOEBp MkLx[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NULKTHFyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
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NCI-H661 M1exW2Z2dmO2aX;uJIF{e2G7 M2\uPVAtKDFuIEKsJFQhcA>? Mkjr[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MmKzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
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BT-37 MlfJdWhVWyCjc4PhfS=> MmnJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOzdiY3XscJM> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) NHzjenVyUFSVIHHzd4F6 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> MmLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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OHS-50 M4TIN5FJXFNiYYPzZZk> NUHMZpNFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| Ml;hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 NVj6O29VeUiWUzDhd5NigQ>? MmfPdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NHrCOpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NGPiNpFyUFSVIHHzd4F6 M4GyeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NFHvN|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NVP5PVB3eUiWUzDhd5NigQ>? NFXyNVJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> Ml7LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MWjxTHRUKGG|c3H5 Mnu4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MnzIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 M3T0fZFJXFNiYYPzZZk> M1vBOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| M2rSb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NXfZU5VqeUiWUzDhd5NigQ>? M{KyW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG5DOTZ2MzDj[Yxtew>? NXrmNYxWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NHrEWohyUFSVIHHzd4F6 MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ MlW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MmPKdWhVWyCjc4PhfS=> MmDEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2ouT0KPMjDj[Yxtew>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 MX;xTHRUKGG|c3H5 M1XmVZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NFXPd209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 M{HjRpFJXFNiYYPzZZk> MoLEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVogyQCClZXzsdy=> MoLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NEPFO5dyUFSVIHHzd4F6 MkDYdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ NHzKZ3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... 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、MSDS / 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、MSDS / 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
NCT04042051 Terminated Drug: Copanlisib|Drug: Trastuzumab emtansine HER2-positive Breast Cancer|Metastatic Breast Cancer|Locally Advanced Breast Cancer|Unresectable Breast Cancer Cancer Trials Ireland November 12 2019 Phase 1
NCT03711058 Recruiting Drug: Copanlisib|Drug: Nivolumab Unresectable or Metastatic Microsatellite Stable (MSS) Solid Tumor Along With Microsatellite Stable (MSS) Colon Cancer|Colon Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Bayer|Bristol-Myers Squibb January 10 2019 Phase 1|Phase 2
NCT03498430 Completed Drug: Copanlisib (Aliqopa BAY80-6946) Lymphoma Non-Hodgkin Bayer April 27 2018 Phase 1
NCT03172884 Completed Drug: Copanlisib (ALIQOPA BAY80-6946) Hepatic Insufficiency Renal Insufficiency Bayer June 14 2017 Phase 1
NCT02822482 Terminated Drug: Copanlisib|Drug: Cetuximab Carcinoma Squamous Cell of Head and Neck UNICANCER June 2016 Phase 1|Phase 2
NCT02155582 Completed Drug: Copanlisib (BAY80-6946) Non Hodgkin Lymphoma Bayer August 12 2014 Phase 1

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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

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID