Volasertib (BI 6727)

目录号:S2235

仅限科研使用

Volasertib (BI 6727)是一种高度有效的Plk1抑制剂,无细胞试验中IC50为0.87 nM,比作用于Plk2和Plk3选择性高6和65倍。Volasertib可在多种癌细胞中诱导细胞周期停滞和自噬。Phase 3。

Volasertib (BI 6727) Chemical Structure

CAS: 755038-65-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1654.53 现货
RMB 974.11 现货
RMB 3005.97 现货
大包装 有超大折扣

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)
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客户使用Selleck生产的Volasertib (BI 6727)发表文献136篇:

产品安全说明书

PLK抑制剂选择性比较

相关PLK产品

生物活性

产品描述 Volasertib (BI 6727)是一种高度有效的Plk1抑制剂,无细胞试验中IC50为0.87 nM,比作用于Plk2和Plk3选择性高6和65倍。Volasertib可在多种癌细胞中诱导细胞周期停滞和自噬。Phase 3。
特性 BI6727具有高的体积分布,良好的组织穿透力和长的半衰期。
靶点
PLK1 [1]
(Cell-free assay)
0.87 nM
体外研究

如同BI2536,BI6727是属于dihydropteridinone类化合物的ATP竞争性激酶抑制剂。除了Plk1,BI6727也有效地抑制两个密切相关的激酶Plk2和Plk3,IC50分别为为5 nM和56 nM。 BI6727在浓度高达10 μM时对五十多种激酶均没有抑制活性。BI6727抑制从各种癌组织来源的多种细胞系的增殖,包括HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1 和 Raji 细胞,EC50 分别为23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM 和 37 nM。在NCI-H460细胞中,BI6727 (100 nM)诱导有丝分裂细胞聚集,这些细胞中有单极纺锤体和组蛋白H3的磷酸丝氨酸10阳性染色,这表明细胞处于M期,随后诱导细胞凋亡。[1] BI6727低纳摩尔浓度表现对神经母细胞瘤(NB)肿瘤起始细胞(NB TIC)的抑制活性,EC 50为21 nM,而只有微摩尔浓度的BI6727对正常小儿神经干细胞有毒性作用。[2] 类似于BI2536,BI6727诱导Daoy和ONS-76髓母细胞瘤细胞的生长停滞。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KASUMI-1 NIXncFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYG3NkBp MYrJR|UxRTF5MNMxOVEhdk1? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV5NkC3OEc,OjV3N{[wO|Q9N2F-
KG-1 NYnSNnZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYG3NkBp NHK4NWJKSzVyPUG1NOKyPjdibl2= MnrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{[wO|QoRjJ3NUe2NFc1RC:jPh?=
MOLM-13 MlzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHLR4U4OiCq M1LpNWlEPTB;NUhCtVQ1KG6P MnTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{[wO|QoRjJ3NUe2NFc1RC:jPh?=
MV-4-11 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37PZVczKGh? NE\Ge2FKSzVyPUG2xtE3KG6P Mm\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3N{[wO|QoRjJ3NUe2NFc1RC:jPh?=
NOMO-1 M3TueGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUm3NkBp NXHsXHo6UUN3ME2xOFXDuTdibl2= NG\ZVVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW3OlA4PCd-MkW1O|YxPzR:L3G+
OCI-AML3 NX;BfJBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrkVZRoPzJiaB?= NIGyXJVKSzVyPUmwxtE2OSCwTR?= NV3xXVBFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|YxPzRpPkK1OVc3ODd2PD;hQi=>
SKM-1 NW\QfGp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYK3NkBp M2HPe2lEPTB;OUZCtVUzKG6P NUTVb2J[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|YxPzRpPkK1OVc3ODd2PD;hQi=>
THP-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYW3NkBp NWrYWYRxUUN3ME21OuKyOzlibl2= NYS4O5NRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1O|YxPzRpPkK1OVc3ODd2PD;hQi=>
MCF7/LTED  MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXeyMlUuPDBibl2= M3HLZVUh\A>? MlzwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR6MEm0N{c,OjV2OEC5OFM9N2F-
HCC1428/LTED MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fDcFIvPS12MDDuUS=> M1HI[VUh\A>? MoGxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUfqT2liRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFA6PDNpPkK1OFgxQTR|PD;hQi=>
A431 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PpdlAuOzBibl2= MWKxMVQh\A>? MmLWbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh7MUC5Okc,OjN6OUGwPVY9N2F-
FaDu  NFjDfpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWwMVExODBibl2= M3\6VFEuPCCm NWXJUG1VcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U1l\XCnbnTlcpQhdWGwbnXy NV;hd4dqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4PVExQTZpPkKzPFkyODl4PD;hQi=>
SF188 NX3rR2w{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPzOVAuOTVyIH7N MkfxO|IhcA>? NVfib|ZOTE2VTx?= M3fibYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh6N{[0OUc,OjN6OEe2OFU9N2F-
T98G MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1frTlUxNTF3MDDuUS=> NWTMZoJkPzJiaB?= MVfEUXNQ M4TaeIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M2DDfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEi3OlQ2Lz5{M{i4O|Y1PTxxYU6=
DU145 MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS5bJcyOC93MD:yOVAhdk1? NYjKRXBROjRiaB?= MV7JR|UxRDFyIH7N MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh6NESyPEc,OjN6OES0Nlg9N2F-
LNCaP NW\k[ppGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;BTGxbOTBxNUCvNlUxKG6P NIDUS3EzPCCq M3;JTmlEPTB:MUCgcm0> M4PVUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEi0OFI5Lz5{M{i4OFQzQDxxYU6=
PC3 NGf5SJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEf6fXkyOC93MD:yOVAhdk1? M1HofFI1KGh? M13N[2lEPTEkiMy2NFAhdk1? NGTQPXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i4OFQzQCd-MkO4PFQ1Ojh:L3G+
RT4 MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH1OFghcA>? NVfKRpVKUUN3ME2xNVEvOjdibl2= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7Mk[zPUc,OjN5OUK2N|k9N2F-
5637 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzxPJI1QCCq NF\QWVdKSzVyPUGxOlUvOTRibl2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7Mk[zPUc,OjN5OUK2N|k9N2F-
T24 NFK3UZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX2OFghcA>? NH\ITYVKSzVyPUKwOE46OSCwTR?= MojEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK2N|koRjJ|N{myOlM6RC:jPh?=
KMCH-1 Mm[wRZBweHSxc3nzJGF{e2G7 NFfNU|EzODBibl2= NEfjOJozPCCq MnfsbY5lfWOnczDhdI9xfG:|aYO= NWTQcm1rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NFM3PzNpPkKzO|A{Pjd|PD;hQi=>
Mz-ChA-1 Mo\3RZBweHSxc3nzJGF{e2G7 MVGyNFAhdk1? MkPiNlQhcA>? NUTB[FB[cW6mdXPld{BieG:ydH;zbZM> NWPD[GtHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NFM3PzNpPkKzO|A{Pjd|PD;hQi=>
HUCCT-1 NEHQV4dCeG:ydH;zbZMhSXO|YYm= MXyyNFAhdk1? MojpNlQhcA>? MkixbY5lfWOnczDhdI9xfG:|aYO= NHr4ZXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ewN|Y4Oyd-MkO3NFM3PzN:L3G+
HCT 116 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\zR2hGSzVywrC9JFI{KG6P MmHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|OEO4NlMoRjF7M{izPFI{RC:jPh?=
NCI-H460 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\ONWVEPTEEoE2gNlEhdk1? M17NSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7M{izPFI{Lz5zOUO4N|gzOzxxYU6=
BRO M1TJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW5[4JVTUN3MNMgQUAyOSCwTR?= M4DSS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7M{izPFI{Lz5zOUO4N|gzOzxxYU6=
GRANTA-519 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{WyfmVEPTEEoE2gNVUhdk1? NHjjNJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUO4N|gzOyd-MUmzPFM5OjN:L3G+
HL-60 NWPCcm1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHaSWM2OMLiPTCzNkBvVQ>? NXTTOXhbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmzPFM5OjNpPkG5N|g{QDJ|PD;hQi=>
THP-1 Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\LVGVEPTBiPTCzOkBvVQ>? MnHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|OEO4NlMoRjF7M{izPFI{RC:jPh?=
Raji M2DvRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;GZVNMTUN3MDC9JFM4KG6P MkWwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl|OEO4NlMoRjF7M{izPFI{RC:jPh?=
TC32 NYHpUWpseUiWUzDhd5NigQ>? M1rGZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS M2\PXpFJXFNiYYPzZZk> NUjxUok3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=> MmjuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 Ml\qdWhVWyCjc4PhfS=> NHjVOYlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= M1;hUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY MX7xTHRUKGG|c3H5 NHrQ[41yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= M1PiU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 NHHOUlFyUFSVIHHzd4F6 MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| M4LxWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 MX3xTHRUKGG|c3H5 M1;SeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MlGxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD M2rNV5FJXFNiYYPzZZk> MoTKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NYTPZY8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH M{fyXJFJXFNiYYPzZZk> NIW1ToxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> NWGxOZpnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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MG 63 (6-TG R) NUmxTHYzeUiWUzDhd5NigQ>? MnfrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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OHS-50 MWHxTHRUKGG|c3H5 NWP6W3pWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> Mm\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NWHke2RJeUiWUzDhd5NigQ>? Mo\mdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MnXjdWhVWyCjc4PhfS=> NFrZWWJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnizNEBk\Wyucx?= NWDzPY1LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NVTLdmVCeUiWUzDhd5NigQ>? NXvOVHA1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> MnHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC M1\hWZFJXFNiYYPzZZk> MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NFv5PI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 MkfKdWhVWyCjc4PhfS=> MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NXjQWFNQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 M3\hVZFJXFNiYYPzZZk> MknqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 NH\nN5dyUFSVIHHzd4F6 M{LpUpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| Mn3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SKBR3 MXTDfZRwfG:6aXPpeJkh[XO|YYm= NXrYe|RLOjRiaILz NWTW[XB4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigQ>? M3nYWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQ5Lz5{OUK4PFk1QDxxYU6=
MDA-MB-231 NEXBPGxEgXSxdH;4bYNqfHliYYPzZZk> NI\vPXIzPCCqcoO= NWjpO3o4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5 MmjZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFgoRjJ7Mki4PVQ5RC:jPh?=
MDA-MB-468 Mm\mR5l1d3SxeHnjbZR6KGG|c3H5 MYGyOEBpenN? NIXKR4lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYm= MoLzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFgoRjJ7Mki4PVQ5RC:jPh?=
BT474 NIXmNHREgXSxdH;4bYNqfHliYYPzZZk> NW[2OVRJOjRiaILz MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFQ4PCClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5 NWL1UXVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDhpPkK5Nlg5QTR6PD;hQi=>
ZR-75-1 NUWzeWgzS3m2b4TvfIlkcXS7IHHzd4F6 MUmyOEBpenN? NGi3fYZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBbWi15NT2xJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCPVGSgZZN{[Xl? NWPxcoNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDhpPkK5Nlg5QTR6PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-PLK1 / PLK1 p-AKT / AKT / p-MAPK / MAPK PARP / c-myc p-c-Met / c-Met / p-FAK / FAK / p-Src / Src Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3 29108241 29383095 31040125
Immunofluorescence PLK1 / Wee1 29108241
Growth inhibition assay Cell viability 29383095
体内研究 BI6727显著抑制多种人类肿瘤异种移植物的生长,包括HCT116, NCI-H460, 和紫杉类耐药CXB1结肠癌,伴随着增加的有丝分裂指数以及细胞凋亡的增加。[1] 体内研究表明,BI6727表现出比BI2536更好的毒性和药动学特征。[3]

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]
  • 体外激酶抑制试验:

    重组人类Plk1的(残基1-603)是用杆状病毒表达系统表达的带有NH2末端和GST-标记的融合采用的蛋白质。酶的活性测定法测定Plk1是在梯度稀释的BI6727中进行,以20 ng重组激酶以及10 μg牛乳酪蛋白为底物。激酶反应在60微升的终体积在30℃下进行45分钟[15 mM MgCl2, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi γ-32P-ATP]。反应通过加入125μL冰冷的5%三氯乙酸终止。转移沉淀到多屏幕混合酯纤维素过滤板后,洗涤板用1%三氯乙酸洗涤并测量辐射量。剂量-反应曲线用于计算IC 50值。

细胞实验:[1]
  • Cell lines: HCT116,NCI-H460,BRO,GRANTA-519,HL-60,THP-1,和Raji细胞
  • Concentrations: 溶解在DMSO中至终浓度约1 μM
  • Incubation Time: 24, 48和72小时
  • Method: 细胞增殖测定是将细胞孵育在不同浓度的BI6727中24,48和72小时,而后在荧光分光光度计上通过测量的Alamar蓝染料的转换测定。有效浓度在哪些细胞生长是由50%(EC 50)抑制从剂量 - 反应曲线拟合推断的。为了确定DNA含量,细胞悬浮液被固定在80%乙醇中,用含0.25%Triton X-100的PBS处理5分钟,并用含0.1%RNA酶和10 μg/mL的碘化丙锭的PBS室温孵育20分钟。细胞周期的测定是用流式细胞仪分析的。
动物实验:[1]
  • Animal Models: 雌性BomTac:NMRI-Foxn1 NU小鼠腹腔移植HCT116,NCI-H460,或CXB1细胞。
  • Dosages: 约25 mg/kg/day
  • Administration: 静脉注射,或通过灌胃针

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+corn oil

2mg/mL

* 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 618.81
化学式

C34H50N8O3

CAS号 755038-65-4
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02722135 Withdrawn Drug: Volasertib Leukemia Myeloid Acute Boehringer Ingelheim November 2016 Phase 1
NCT02721875 Terminated Drug: Volasertib|Drug: Azacitidine Myelodysplastic Syndromes Boehringer Ingelheim April 28 2016 Phase 1
NCT02201329 Completed Drug: Azacitidine|Drug: Volasertib Myelodysplastic Syndromes|Leukemia Myelomonocytic Chronic Boehringer Ingelheim August 2014 Phase 1
NCT01971476 Completed Drug: volasertib Leukemia|Neoplasms Boehringer Ingelheim October 22 2013 Phase 1
NCT01662505 Completed Drug: Volasertib Leukemia Myeloid Acute Boehringer Ingelheim August 2012 Phase 1

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

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操作手册

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常见问题及建议解决方法

问题 1:
I wonder how to reconstitute the inhibitor for in vivo studies?

回答:
Volasertib can be dissolved in 4% DMSO+Corn oil at 2mg/ml for i.p. injection in mice. For oral administration, it can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose as indicated in the publications. We also suggest the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol for a suspension which we tested in house.

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