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Copanlisib (BAY 80-6946)

目录号：S2802 中文名称：库潘尼西

仅限科研使用

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。

Copanlisib (BAY 80-6946) Chemical Structure

CAS: 1032568-63-0

规格	价格	库存
5mg	RMB 2193.76	现货
10mg	RMB 3038.51	现货
50mg	RMB 8763.3	现货
大包装	有超大折扣
大剂量询单有大折扣!
今日订购，明日送达全国免运费分装免费分装成小规格产品（单支最小为1mg）如1支10mg产品可分装为10支1mg产品全国免费电话：400-668-6834 \| Email：info@selleck.cn

客户使用Selleck生产的Copanlisib (BAY 80-6946)发表文献34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 (KRAS^G12D) 和EGI-1 (KRAS^G12D) 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	MYTHdo94fGhiaX7obYJqfG:wIHHzd4F6	M2W5flExOCCwTR?=		M4q5eWNweGGwbHnzbYIh\G:\|ZT3k[ZBmdmSnboTsfUBqdmirYnn0[YQh[2WubDDndo94fGhiaX6geol1em9wIFnDOVA:PDdwOTDuUU4>	NFnMbHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
HepG2	NWTzNGlYT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?=	NHGwWGoyODBibl2=		NUT2epVoS2:yYX7sbZNq[iCmb4PlMYRmeGWwZHXueIx6KGmwaHnibZRm\CClZXzsJIdzd3e2aDDpckB3cXS{bz6gTWM2OD1\|MT62JI5ONg>?	M2LpdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[yPVUzLz5\|MEm2Nlk2OjxxYU6=
Hep3B	NH\FdFBIem:5dHigbY5pcWKrdH;uJIF{e2G7			MlvSTWM2OD15Mj60JI5O	Mnq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NkK5OVIoRjNyOU[yPVUzRC:jPh?=
PLCPRF5	MVnHdo94fGhiaX7obYJqfG:wIHHzd4F6			NVn5XpMzUUN3ME2yPFMhdk1?	M4j0UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[yPVUzLz5\|MEm2Nlk2OjxxYU6=
Chang	NYflO4xRT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?=			NHjadW9KSzVyPUS0NkBvVQ>?	NWK3RZFlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OlI6PTJpPkOwPVYzQTV{PD;hQi=>
JVM-3	NW[3OXhHTnWwY4Tpc44h[XO\|YYm=		M{izPFQ5KGh?	NF7mZ5lqdmirYnn0d{Bu\XSjYn;sbYMh[WO2aY\peJkhf2m2aDDhckBKSzVyIH;mJFIh\|ryPIHnuJJRp\SC[VGSgZZN{[Xl?	M4Tsd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUGyOlM2Lz5{NUmxNlY{PTxxYU6=
BT-474	NX7qTWY5TnWwY4Tpc44h[XO\|YYm=	MkPuOVAhdk1?	MnjVNE42NCB{LDC0MEA5NCB{NDDo	NUjuVXFSemGyaXTsfUBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApWzR5MzygWFMxQCliYYOge4VtdCCjczDpeJMh\Gm{ZXP0JJN2[nO2cnH0[ZMhWFKDU{SwJEhVOjR4KTDhcoQhT1ONM98yJEhUQSluIHHu[EBqdmirYnn0bY9vKHejczDzeZN1[WmwZXSg[o9zKHWyIITvJFI1KGixdYLz	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
SK-BR-3	Mm\JSpVv[3Srb36gZZN{[Xl?		M2q3fVAtKDFuIEKsJFQhcA>?	NVLRWHVU\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
UACC-893	M4nabmZ2dmO2aX;uJIF{e2G7		MljJNEwhOSxiMjygOEBp	NF7lcFBld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	M{jkTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
HCC-1954	MmjTSpVv[3Srb36gZZN{[Xl?		MUOwMEAyNCB{LDC0JIg>	MVjkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NID1Vow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
MDA-MB-453	MWnGeY5kfGmxbjDhd5NigQ>?		MmDqNEwhOSxiMjygOEBp	NGXHdIdld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	NIH4SYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
MDA-MB-361	NETjXG9HfW6ldHnvckBie3OjeR?=		M3r2d\|AtKDFuIEKsJFQhcA>?	MUfkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
BT-20	MUTGeY5kfGmxbjDhd5NigQ>?		MmLINEwhOSxiMjygOEBp	NY\0XYh3\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
MCF-7	M4\QUGZ2dmO2aX;uJIF{e2G7		NVLMeJBCOCxiMTygNkwhPCCq	MlTu[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	Mon4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
T-47D	NY\CW\|ZCTnWwY4Tpc44h[XO\|YYm=		MkPyNEwhOSxiMjygOEBp	NHnIfGNld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	M4mwZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
HCC1806	MX\GeY5kfGmxbjDhd5NigQ>?		M3LGSFAtKDFuIEKsJFQhcA>?	MVvkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	MoXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
NCI-H292	NVKyTWdxTnWwY4Tpc44h[XO\|YYm=		M1rjPFAtKDFuIEKsJFQhcA>?	MmLp[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	NV\mVYZlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N\|YxPDhpPkK0OFM3ODR6PD;hQi=>
NCI-H1650	MlTHSpVv[3Srb36gZZN{[Xl?		M1T3flAtKDFuIEKsJFQhcA>?	MVjkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NI\6SlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
CCRF-SB	M{DrZmZ2dmO2aX;uJIF{e2G7		MmjSNEwhOSxiMjygOEBp	MoTU[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	NHTiZ4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
U937	NGjPNFNHfW6ldHnvckBie3OjeR?=		MoLjNEwhOSxiMjygOEBp	NETtco9ld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
SU-DHL-4	NFjq[nRHfW6ldHnvckBie3OjeR?=		NUTuTZpzOCxiMTygNkwhPCCq	MVfkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NXjK[I5pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N\|YxPDhpPkK0OFM3ODR6PD;hQi=>
SU-DHL-5	MmTuSpVv[3Srb36gZZN{[Xl?		Ml\UNEwhOSxiMjygOEBp	M2rVN4Rwf26{ZXf1cIF1cW:wIH;mJHAuSUuW	NE\Dd4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
HCT116	MoHSSpVv[3Srb36gZZN{[Xl?		NYTBZY9bOCxiMTygNkwhPCCq	MVHkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NWCxWXJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N\|YxPDhpPkK0OFM3ODR6PD;hQi=>
A549 cells	MVfGeY5kfGmxbjDhd5NigQ>?		NInqUGkxNCBzLDCyMEA1KGh?	NF;kZYZld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	M1HMbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
SK-MEL-30	Ml3CSpVv[3Srb36gZZN{[Xl?		MnzJNEwhOSxiMjygOEBp	MWDkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	MlzhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
SK-MEL-2 cells	MlzNSpVv[3Srb36gZZN{[Xl?		NWOxO2ZuOCxiMTygNkwhPCCq	NYjmR2NF\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
NCI-H1703	Mn;GSpVv[3Srb36gZZN{[Xl?		M4Pqd\|AtKDFuIEKsJFQhcA>?	MnvZ[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	NXXwR29TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N\|YxPDhpPkK0OFM3ODR6PD;hQi=>
NCI-H661	Mmq2SpVv[3Srb36gZZN{[Xl?		MnjZNEwhOSxiMjygOEBp	M1j6PYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW	M1\BVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
PC9	MVPGeY5kfGmxbjDhd5NigQ>?		M3\5S\|AtKDFuIEKsJFQhcA>?	NUfrUllR\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	NEDlXo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
TC32	MYHxTHRUKGG\|c3H5			MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXEN\|MjDj[Yxtew>?	NW\FNmlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673	MXvxTHRUKGG\|c3H5			MlTXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	NX\vOJdZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2	Ml;3dWhVWyCjc4PhfS=>			MlXWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?=	NVT3ZlVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD	MlfqdWhVWyCjc4PhfS=>			M{j1WpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>?	NXj2OlR2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R)	MYPxTHRUKGG\|c3H5			NIXKOplyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO=	NY\jSolCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50	NIHUcWRyUFSVIHHzd4F6			NVHRdItYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	MlK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	NGrqVZJyUFSVIHHzd4F6			M4HLeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGxCVi13IHPlcIx{	MkK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	NIrWdmFyUFSVIHHzd4F6			NEO5NoRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSi2HQnOxJINmdGy\|	NV7hNWQ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SK-N-MC	NGH5dm9yUFSVIHHzd4F6			M3TnWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN?	NG[wVJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
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Saos-2	NVu1fpR7eUiWUzDhd5NigQ>?			MnL2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{	NWrkbotVRGFidHHy[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 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

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]

激酶实验：^[1]	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]	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。
动物实验：^[1]	Animal Models: Rats bearing KPL4 or HCT116 xenografts Dosages: 6 mg/kg Administration: i.v.

参考文献	[1] Liu N, et al. Mol Cancer Ther. 2013, 12(11), 2319-2330. [2] Elster N, et al. Breast Cancer Res Treat. 2015, 149(2), 373-383.

溶解度（25°C）

体外

* 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	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download Copanlisib (BAY 80-6946) SDF

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 μL 动物数量只

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

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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