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。

规格

价格

库存

购买数量

5mg	RMB 2193.76	现货
10mg	RMB 3038.51	现货
50mg	RMB 8763.3	现货
200mg	RMB 20229.3	现货
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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23篇：

Nature, 2018, 560(7719):499-503

PubMed: 30051890 ( click the link to review the publication )

J Transl Med, 2021, 19(1):184

PubMed: 33933113 ( click the link to review the publication )

Nat Commun, 2020, 25;11(1):1556

PubMed: 32214092 ( click the link to review the publication )

Cells, 2020, 9(1)

PubMed: 31952221 ( click the link to review the publication )

Mol Cancer Ther, 2020, molcanther.0259.2020

PubMed: 33087508 ( click the link to review the publication )

Mol Cancer Res, 2020, 11

PubMed: 32161139 ( click the link to review the publication )

Sci Rep, 2020, 1;10(1):8867

PubMed: 32483262 ( click the link to review the publication )

Breast Cancer Res Treat, 2020, 179(2):337-347

PubMed: 31655920 ( click the link to review the publication )

Cell Signal, 2020, 68:109525

PubMed: 31911180 ( click the link to review the publication )

Oncol Lett, 2020, 20(1):533-540

PubMed: 32565979 ( click the link to review the publication )

Cell Death Discov, 2019, 5:86

PubMed: 30962952 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2019, 381:114729

PubMed: 31445927 ( click the link to review the publication )

BMC Cancer, 2019, 19(1):936

PubMed: 31601188 ( click the link to review the publication )

J Biol Chem, 2018, 293(42):16518-16527

PubMed: 30166343 ( click the link to review the publication )

Biomed Res Int, 2018, 2018:1023490

PubMed: 29750146 ( click the link to review the publication )

Nat Commun, 2017, 8(1):1090

PubMed: 29061961 ( click the link to review the publication )

Oncol Rep, 2017, 37(5):3137-3145

PubMed: 28350104 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(11):2713-2722

PubMed: 28476872 ( click the link to review the publication )

Oncol Rep, 2017, 38(5):3167-3176

PubMed: 28901470 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2017, 114(6):E980-E989

PubMed: 28049849 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2016, 29(3):317-28

PubMed: 26850518 ( click the link to review the publication )

Oncotarget, 2016, 7(15):19620-30

PubMed: 26934000 ( click the link to review the publication )

Oncotarget, 2016, 7(26):40398-40417

PubMed: 27259258 ( click the link to review the publication )

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	Activity Description	PMID
Huh7	M{nCbGdzd3e2aDDpcohq[mm2b36gZZN{[Xl?	MX[xNFAhdk1?		MnftR49x[W6uaYPpZkBld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTl[EBk\WyuIHfyc5d1cCCrbjD2bZRzdy5iSVO1NF01Py57IH7NMi=>	NEDnOVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
HepG2	MnrQS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>?	MlW4NVAxKG6P		NYrrb5JQS2:yYX7sbZNq[iCmb4PlMYRmeGWwZHXueIx6KGmwaHnibZRm\CClZXzsJIdzd3e2aDDpckB3cXS{bz6gTWM2OD1\|MT62JI5ONg>?	M4L1NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOU[yPVUzLz5\|MEm2Nlk2OjxxYU6=
Hep3B	Mk\VS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>?			MULJR\|UxRTd{LkSgcm0>	NHfRZWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
PLCPRF5	Mlz6S5Jwf3SqIHnubIljcXSxbjDhd5NigQ>?			NH3R[2pKSzVyPUK4N{BvVQ>?	NH\udpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm2Nlk2Oid-M{C5OlI6PTJ:L3G+
Chang	MXHHdo94fGhiaX7obYJqfG:wIHHzd4F6			MUPJR\|UxRTR2MjDuUS=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl4Mkm1Nkc,OzB7NkK5OVI9N2F-
JVM-3	NX[1bGs6TnWwY4Tpc44h[XO\|YYm=		NYHqRpRJPDhiaB?=	NV;GTlNtcW6qaXLpeJMhdWW2YXLvcIlkKGGldHn2bZR6KHerdHigZY4hUUN3MDDv[kAzKM7:TTDpckB1cGViWGTUJIF{e2G7	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzMk[zOUc,OjV7MUK2N\|U9N2F-
BT-474	MWTGeY5kfGmxbjDhd5NigQ>?	MknEOVAhdk1?	MkHQNE42NCB{LDC0MEA5NCB{NDDo	Mn:xdoFxcWSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV\|Q4OyxiVEOwPEkh[XNid3XscEBieyCrdIOg[Ilz\WO2IIP1ZpN1emG2ZYOgVHJCWzRyIDjUNlQ3MSCjbnSgS3NMO87{IDjTPUktKGGwZDDpcohq[mm2aX;uJJdieyC\|dYP0ZYlv\WRiZn;yJJVxKHSxIEK0JIhwfXK\|	NFHpTpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
SK-BR-3	Mn;YSpVv[3Srb36gZZN{[Xl?		NWT0d3dTOCxiMTygNkwhPCCq	MmLW[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	NHzHZ3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
UACC-893	MUXGeY5kfGmxbjDhd5NigQ>?		NYfNXo5WOCxiMTygNkwhPCCq	NUGwNGJM\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	Mln6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
HCC-1954	MlS2SpVv[3Srb36gZZN{[Xl?		MlPSNEwhOSxiMjygOEBp	MWLkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NYHOR5JRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N\|YxPDhpPkK0OFM3ODR6PD;hQi=>
MDA-MB-453	NEPnfZVHfW6ldHnvckBie3OjeR?=		MlPhNEwhOSxiMjygOEBp	NFXzbJJld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	NEfvWm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
MDA-MB-361	MXHGeY5kfGmxbjDhd5NigQ>?		M1vYUFAtKDFuIEKsJFQhcA>?	NHy3WFRld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR\|NkC0PEc,OjR2M{[wOFg9N2F-
BT-20	MVHGeY5kfGmxbjDhd5NigQ>?		MmHmNEwhOSxiMjygOEBp	M{PjSIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW	MlfxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
MCF-7	NInJW5dHfW6ldHnvckBie3OjeR?=		MXmwMEAyNCB{LDC0JIg>	MoH6[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	MkfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
T-47D	NIjYZWVHfW6ldHnvckBie3OjeR?=		NFOyNIsxNCBzLDCyMEA1KGh?	NY\pN\|Zo\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	M3P2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
HCC1806	NGi1SXJHfW6ldHnvckBie3OjeR?=		NH\5OIsxNCBzLDCyMEA1KGh?	NFK5UW9ld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	NGHuclQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
NCI-H292	MVPGeY5kfGmxbjDhd5NigQ>?		NYHFbWxSOCxiMTygNkwhPCCq	NVP3XHdx\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	MlXEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
NCI-H1650	MUTGeY5kfGmxbjDhd5NigQ>?		MYCwMEAyNCB{LDC0JIg>	MUDkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NFXXeXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
CCRF-SB	NIjN[nNHfW6ldHnvckBie3OjeR?=		MkjKNEwhOSxiMjygOEBp	MmTp[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	MnftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
U937	MWXGeY5kfGmxbjDhd5NigQ>?		MkDHNEwhOSxiMjygOEBp	M4rLdIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW	MnLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
SU-DHL-4	MWPGeY5kfGmxbjDhd5NigQ>?		NIf0em8xNCBzLDCyMEA1KGh?	MWHkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	NF\abHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
SU-DHL-5	MU\GeY5kfGmxbjDhd5NigQ>?		MoHqNEwhOSxiMjygOEBp	NF62cIZld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	M1L0VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
HCT116	M32ybWZ2dmO2aX;uJIF{e2G7		MnvJNEwhOSxiMjygOEBp	NWfR[FJK\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	M2\4TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
A549 cells	NWD4VG01TnWwY4Tpc44h[XO\|YYm=		NUjJe4lOOCxiMTygNkwhPCCq	NIX0PGpld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	M2rvSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
SK-MEL-30	MkS4SpVv[3Srb36gZZN{[Xl?		MVKwMEAyNCB{LDC0JIg>	NW\BXoY{\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S=	NEjk[pg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
SK-MEL-2 cells	NVrVVldoTnWwY4Tpc44h[XO\|YYm=		NIj0cYYxNCBzLDCyMEA1KGh?	MWDkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>?	M1zSSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEO2NFQ5Lz5{NESzOlA1QDxxYU6=
NCI-H1703	M4nhbGZ2dmO2aX;uJIF{e2G7		MkXVNEwhOSxiMjygOEBp	MkjH[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	MknoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2M{[wOFgoRjJ2NEO2NFQ5RC:jPh?=
NCI-H661	MXXGeY5kfGmxbjDhd5NigQ>?		NHrWVnUxNCBzLDCyMEA1KGh?	NEfNZ5Fld3ewcnXneYxifGmxbjDv[kBRNUGNVB?=	NULDe5p7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0N\|YxPDhpPkK0OFM3ODR6PD;hQi=>
PC9	NUHaXItUTnWwY4Tpc44h[XO\|YYm=		MkjPNEwhOSxiMjygOEBp	Mnf3[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R?	NEXVfpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESzOlA1QCd-MkS0N\|YxPDh:L3G+
TC32	NWHodXpteUiWUzDhd5NigQ>?			NHT2e2VyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?=	NV;sT3JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673	NYX6UHNUeUiWUzDhd5NigQ>?			NEf4NJNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?=	M3fWTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2	M4nrNJFJXFNiYYPzZZk>			NHvibXJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz	NXq1S3dsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD	NF3lW3dyUFSVIHHzd4F6			NGXkPW9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN?	NFH6Z3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
MG 63 (6-TG R)	MkHIdWhVWyCjc4PhfS=>			M3\PNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	M2rFVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50	MmPVdWhVWyCjc4PhfS=>			NWjvUWFEeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	MmLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
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Rh18	NU\ieXdNeUiWUzDhd5NigQ>?			MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>?	Ml33QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB1643	MkLqdWhVWyCjc4PhfS=>			MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM>	NIDyVXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-MC	NWf0N\|RXeUiWUzDhd5NigQ>?			M2HHd5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN?	M4Oze\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	MWPxTHRUKGG\|c3H5			MorBdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2ouT0KPMjDj[Yxtew>?	NH7tVXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
TC32	MlzJdWhVWyCjc4PhfS=>			MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR\|MzKGOnbHzz	MlziQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh18	NVnld29weUiWUzDhd5NigQ>?			M2XFWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOThiY3XscJM>	NH3NRnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	M3niPJFJXFNiYYPzZZk>			NX\aO2ZxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy\|	NUe0[oJjRGFidHHy[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 Cancer Discov 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 Cancer Discov 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 Cancer Discov 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]

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)

参考文献

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 Download Copanlisib (BAY 80-6946) SDF

分子量	480.52
化学式	C₂₃H₂₈N₈O₄
CAS号	1032568-63-0
储存条件	3年-20°C 粉状 2年-80°C 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

每只动物给药体积

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

计算重置

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。

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。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04572763	Not yet 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 2021	Phase 1\|Phase 2
NCT04431635	Recruiting	Drug: Copanlisib\|Drug: Nivolumab\|Drug: Rituximab	Indolent Lymphoma	Big Ten Cancer Research Consortium	June 15 2020	Phase 1
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

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。

常见问题及建议解决方法

问题 1：
S2802 (BAY 80-6946) has poor solubility in DMSO and water. Do you have any other suggestion to dissolve this chemical?
回答：
We've tested the solubility of S2802 BAY80-6946 in dichloromethane, chloroform, acetonitrile, acetone, tetrahydrofuran and TFA (aq), and finally found it can be dissolved in 10% Trifluoroacetic acid water solution at 1 mg/ml as a clear solution.

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

选择性强的PI3K抑制剂

CAL-101 (Idelalisib, GS-1101) : p110δ-selective, IC50=2.5 nM.
选择性强的PI3K抑制剂

TGX-221 : p110β-specific, IC50=5 nM.
活性最高的PI3K抑制剂

BEZ235 (NVP-BEZ235, Dactolisib) : p110α/γ/δ/β, IC50=4 nM/5 nM/7 nM/75 nM.
FDA批准的PI3K抑制剂

CAL-101 (Idelalisib, GS-1101) : Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.
最新的PI3K抑制剂

VS-5584 (SB2343) ^New : Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

研究领域

产品类型

定制您的化合物库

Copanlisib (BAY 80-6946)

客户使用Selleck生产的Copanlisib (BAY 80-6946)发表文献23篇：

产品安全说明书

PI3K抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Copanlisib (BAY 80-6946) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技术支持

常见问题及建议解决方法

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

相关PI3K产品