Copanlisib (BAY 80-6946)

Catalog No.S2802

For research use only.

Copanlisib (BAY 80-6946) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.

Copanlisib (BAY 80-6946) Chemical Structure

CAS No. 1032568-63-0

Selleck's Copanlisib (BAY 80-6946) has been cited by 34 publications

Purity & Quality Control

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Biological Activity

Description Copanlisib (BAY 80-6946) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.
Targets
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
In vitro

In both KPL4 cells and LPA-stimulated PC3 cells, BAY 80-6946 reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, BAY 80-6946 shows antiproliferative activity and induces apoptosis. [1] The combination of HER2-targeted therapies and BAY 80-6946 inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 MoTHS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? MmjsNVAxKG6P MkDER49x[W6uaYPpZkBld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTl[EBk\WyuIHfyc5d1cCCrbjD2bZRzdy5iSVO1NF01Py57IH7NMi=> MoDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NkK5OVIoRjNyOU[yPVUzRC:jPh?=
HepG2 MYPHdo94fGhiaX7obYJqfG:wIHHzd4F6 Mlz2NVAxKG6P MoO4R49x[W6uaYPpZkBld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTl[EBk\WyuIHfyc5d1cCCrbjD2bZRzdy5iSVO1NF0{OS54IH7NMi=> NYW1eppDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlI6PTJpPkOwPVYzQTV{PD;hQi=>
Hep3B NH3IUW1Iem:5dHigbY5pcWKrdH;uJIF{e2G7 M4SwUGlEPTB;N{KuOEBvVQ>? NV3hO5E6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlI6PTJpPkOwPVYzQTV{PD;hQi=>
PLCPRF5 NVqzPWZ{T3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= M3G0Z2lEPTB;MkizJI5O NELKUmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
Chang NVOwXZh{T3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= NUPweHZVUUN3ME20OFIhdk1? NIHn[Gc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
JVM-3 NV\5PGF7TnWwY4Tpc44h[XO|YYm= NIT1cZQ1QCCq MUDpcohq[mm2czDt[ZRi[m:uaXOgZYN1cX[rdImge4l1cCCjbjDJR|UxKG:oIEKg{txOKGmwIITo[UBZXFRiYYPzZZk> NXnX[IVXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVI3OzVpPkK1PVEzPjN3PD;hQi=>
BT-474 NGGyc2lHfW6ldHnvckBie3OjeR?= MnT5OVAhdk1? MWmwMlUtKDJuIESsJFgtKDJ2IHi= MkPvdoFxcWSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV|Q4OyxiVEOwPEkh[XNid3XscEBieyCrdIOg[Ilz\WO2IIP1ZpN1emG2ZYOgVHJCWzRyIDjUNlQ3MSCjbnSgS3NMO87{IDjTPUktKGGwZDDpcohq[mm2aX;uJJdieyC|dYP0ZYlv\WRiZn;yJJVxKHSxIEK0JIhwfXK| MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
SK-BR-3 M4DBfWZ2dmO2aX;uJIF{e2G7 NEHTUlYxNCBzLDCyMEA1KGh? Mmn2[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
UACC-893 MXLGeY5kfGmxbjDhd5NigQ>? MYOwMEAyNCB{LDC0JIg> MmTu[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? Mmn0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
HCC-1954 MoDxSpVv[3Srb36gZZN{[Xl? M2r5[|AtKDFuIEKsJFQhcA>? MlP3[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MonjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
MDA-MB-453 NX6wflFYTnWwY4Tpc44h[XO|YYm= NF24cG8xNCBzLDCyMEA1KGh? MWDkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NGezSJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
MDA-MB-361 MYPGeY5kfGmxbjDhd5NigQ>? NI\rdGUxNCBzLDCyMEA1KGh? MVHkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NVTCUW8xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
BT-20 M4DIfmZ2dmO2aX;uJIF{e2G7 NWXmd5Q5OCxiMTygNkwhPCCq MUHkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NWLvfZd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
MCF-7 NVXQfmpnTnWwY4Tpc44h[XO|YYm= MV6wMEAyNCB{LDC0JIg> MoXo[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
T-47D NVy0SZZ5TnWwY4Tpc44h[XO|YYm= MoThNEwhOSxiMjygOEBp NWXEXlVb\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= M2nQOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
HCC1806 MlrCSpVv[3Srb36gZZN{[Xl? NUfnRm96OCxiMTygNkwhPCCq M{H3RYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NIT2fI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
NCI-H292 NYn4WllITnWwY4Tpc44h[XO|YYm= NYWzbFJxOCxiMTygNkwhPCCq MYHkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MmDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
NCI-H1650 MkDUSpVv[3Srb36gZZN{[Xl? MUGwMEAyNCB{LDC0JIg> NGnoT5Jld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NXG3N2k{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
CCRF-SB MWnGeY5kfGmxbjDhd5NigQ>? MkPINEwhOSxiMjygOEBp M3rqboRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MonUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
U937 NVfPWYVbTnWwY4Tpc44h[XO|YYm= M1n6UFAtKDFuIEKsJFQhcA>? M4m2dYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
SU-DHL-4 NXnjcZN7TnWwY4Tpc44h[XO|YYm= NUPXd3BGOCxiMTygNkwhPCCq M2PrOIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NXPDSWxmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
SU-DHL-5 NUjmWYRMTnWwY4Tpc44h[XO|YYm= MV6wMEAyNCB{LDC0JIg> NXSyb5FW\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NVi3NnBSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
HCT116 MoLmSpVv[3Srb36gZZN{[Xl? M4L2ZlAtKDFuIEKsJFQhcA>? MkfF[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
A549 cells NGfCUVBHfW6ldHnvckBie3OjeR?= NEnDPG4xNCBzLDCyMEA1KGh? MUXkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NES5cY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N|YxPDh:L3G+
SK-MEL-30 MULGeY5kfGmxbjDhd5NigQ>? MmC2NEwhOSxiMjygOEBp NIDWOIRld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NUHZTVluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
SK-MEL-2 cells M{HYWGZ2dmO2aX;uJIF{e2G7 NW[2VFV[OCxiMTygNkwhPCCq NELSPZFld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= M2[xPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
NCI-H1703 MlXRSpVv[3Srb36gZZN{[Xl? MkXVNEwhOSxiMjygOEBp MXjkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NVnFOotRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
NCI-H661 NYfLPYI3TnWwY4Tpc44h[XO|YYm= NGHNbIExNCBzLDCyMEA1KGh? MnG3[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NV7WZoV[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N|YxPDhpPkK0OFM3ODR6PD;hQi=>
PC9 NGrLeI5HfW6ldHnvckBie3OjeR?= NIjONZUxNCBzLDCyMEA1KGh? NIPNNWpld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR|NkC0PEc,OjR2M{[wOFg9N2F-
TC32 MVjxTHRUKGG|c3H5 NWLabJFzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGTDN|Ih[2WubIO= NV\5eHFrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 MVjxTHRUKGG|c3H5 NHuyRXdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= NFHCdnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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SK-N-SH MW\xTHRUKGG|c3H5 MlzDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? MnfWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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BT-37 MmLYdWhVWyCjc4PhfS=> NI\wR5ByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1|NzDj[Yxtew>? NYrVTHFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) MnHhdWhVWyCjc4PhfS=> Mnn1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MW\xTHRUKGG|c3H5 MnP2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog{OCClZXzsdy=> M3rDcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 M{DOc5FJXFNiYYPzZZk> MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDPTHMuPTBiY3XscJM> MmqyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MVXxTHRUKGG|c3H5 MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MmfSdWhVWyCjc4PhfS=> NFjkSJByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NIj0fIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 MXvxTHRUKGG|c3H5 M4DSR5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NGLwSWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MlvXdWhVWyCjc4PhfS=> M1zCVpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 NF\YNWpyUFSVIHHzd4F6 MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? Ml;SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 MmfmdWhVWyCjc4PhfS=> MnzNdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUmIyPjR|IHPlcIx{ MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NXWxWoJTeUiWUzDhd5NigQ>? MoTrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>? NXjXRolKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MlPOdWhVWyCjc4PhfS=> MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTTk1ISk1{IHPlcIx{ M4\GVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32 MmrYdWhVWyCjc4PhfS=> NVzDZ2lDeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? NF\1c2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 NYT0SJQyeUiWUzDhd5NigQ>? NEHxRolyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{ MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NXrv[mxyeUiWUzDhd5NigQ>? MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> NYHBRmhiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-PRAS40(T246) / p-GSK3β(S9) / cleaved caspase-3 / cleaved caspase-7 / PI3K-p85 ; 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 24436048
Growth inhibition assay Cell viability 24436048
In vivo In rat KPL4 or HCT116 tumor xenograft model, BAY 80-6946 (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, BAY 80-6946 (14 mg/kg, i.v.) also causes tumor growth inhibition. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Biochemical lipid kinase assays:

    The effect of BAY 80-6946 on PI3Kα, PI3Kβ, and PI3Kγ activity is measured by the inhibition of 33P incorporation into phosphatidylinositol (PI) in 384-well MaxiSorp® plates coated with 2 µg/well of PI and phosphatidylserine (PS) (1:1 molar ratio). In each PI3K isoform assay, 9 µL of reaction buffer (50 mM MOPSO, pH 7.0, 100 mM NaCl, 4 mM MgCl2, 0.1% BSA) containing 7.5 ng of His-tagged N-terminal truncated p110α or p110β protein, or 25 ng of purified human p110γ protein, is used. The reaction is started by adding 5 µL of a 40-µM ATP solution containing 20 µCi/mL [33>/sup>P]-ATP. After 2 hours incubation at room temperature, the reaction is terminated by addition of 5 µL of a 25-mM EDTA solution. The plates are washed and Ultima Gold™ scintillation cocktail (25 µL) is then added. The radioactivity incorporated into the immobilized PI substrate is determined with a BetaPlate Liquid Scintillation Counter.

Cell Research:[1]
  • Cell lines: A series of cancer cell lines
  • Concentrations: ~5 μM
  • Incubation Time: 72 hours
  • Method: Cell proliferation over a 72-hour period is determined using the CellTiter-Glo® luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37ºC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37ºC. Luminescence values are determined with a Wallac 1420 Victor2™ 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo® solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.
Animal Research:[1]
  • Animal Models: Rats bearing KPL4 or HCT116 xenografts
  • Dosages: 6 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 480.52
Formula

C23H28N8O4

CAS No. 1032568-63-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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 October 29 2022 Phase 2
NCT05217914 Not yet recruiting Drug: Copanlisib (BAY80-6946) Relapsed or Refractory Indolent Non-Hodgkin Lymphoma Bayer July 1 2022 --
NCT04939272 Recruiting Drug: Copanlisib Hydrochloride|Drug: Venetoclax Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma City of Hope Medical Center|National Cancer Institute (NCI) July 15 2022 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|Bayer|Bristol-Myers Squibb|University of Michigan June 15 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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