Adavosertib (MK-1775)

目录号:S1525 别名: AZD1775

仅限科研使用

Adavosertib (MK-1775, AZD1775)是一种有效的,高选择性Wee1抑制剂,无细胞试验中IC50为5.2 nM;阻碍G2期DNA损伤检验点。Phase 2。

Adavosertib (MK-1775) Chemical Structure

CAS: 955365-80-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1960.96 现货
RMB 1376.38 现货
RMB 3835.28 现货
RMB 9582.3 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)
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Adavosertib (MK-1775)发表文献167篇:

产品安全说明书

Wee1抑制剂选择性比较

相关Wee1产品

生物活性

产品描述 Adavosertib (MK-1775, AZD1775)是一种有效的,高选择性Wee1抑制剂,无细胞试验中IC50为5.2 nM;阻碍G2期DNA损伤检验点。Phase 2。
特性 首个报道的 Wee1抑制剂。
靶点
Wee1 [1]
(Cell-free assay)
5.2 nM
体外研究

MK-1775以ATP竞争的方式抑制Wee1激酶。与作用于Wee1相比,MK-1775对Yes的效能低2-到3-倍,IC50为14 nM,对7种其他激酶的效能低10倍,1 μM浓度下抑制率>80%,比对人Myt 1选择性高100倍以上,并抑制周期蛋白依赖性激酶1 (CDC2) 在可选择位点(Thr14) 的磷酸化作用。通过阻断负荷突变型p53的WiDr细胞中Wee1活性,废止DNA损伤检控点,MK-1775治疗抑制Tyr15 (CDC2Y15)位点的CDC2基础磷酸化作用,EC50为49 nM,并剂量依赖性抑制gemcitabine-,carboplatin- 或cisplatin-诱导的CDC2磷酸化和细胞周期阻滞,EC50分别为82 nM和81 nM,180 nM 和163 nM,以及159 nM 和 160 nM。30-100 nM 的MK-1775单独治疗在WiDr 和 H1299细胞中没有显著的抗增殖作用,而300 nM的MK-1775足以抑制>80%的Wee1,表现出温和但显著的抗增殖作用,在WiDr和H1299细胞中抑制率分别为34.1%和28.4%。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ASPC-1 NHu5NpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTF|LkKgxtEhOS5zIN88US=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
BxPC-3 NEHQUYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjLUmVGUUN3ME2wMlghyrFiMD6wN{DPxE1? NYX0Vm05RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OVg6PTRpPkK1OFU5QTV2PD;hQi=>
CFPAC-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTNwMzFCtUAxNjJizszN NHW1dIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS1PFk2PCd-MkW0OVg6PTR:L3G+
HPAC M4Tvdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLVWGtpUUN3ME2wMlUhyrFiMD6wNUDPxE1? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
MIAPaCa-2 M17QW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwNTFCtUAxNjB3IN88US=> MnvZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NUi5OVQoRjJ3NEW4PVU1RC:jPh?=
PANC-1 NYXHfoNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFyLk[gxtEhOS5zIN88US=> NXP5[oE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OVg6PTRpPkK1OFU5QTV2PD;hQi=>
SK-N-BE (2) NX\xfXA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPhWppKSzVyPUKuOQKBkcLz4pEJNE4{KM7:TR?= MlvGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-BE (2), PAN→MK NEH3dGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M170eGlEPTB;Mk[uOwKBkcLz4pEJPU43KM7:TR?= NVzsVnN4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFg6OTZpPkK1N|A5QTF4PD;hQi=>
SK-N-BE (2), MK→PAN MoWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;Td2lEPTB;Mj605qCKyrIkgJmwMlMh|ryP NFXXPGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPFkyPid-MkWzNFg6OTZ:L3G+
SK-N-AS NXP1blRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrDXoFKSzVyPUCuOVDjiIoEsfMAjVAvODJizszN M1zjWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
SK-N-DZ M2L0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1GxUGlEPTB;MD6zOwKBkcLz4pEJNE4xOSEQvF2= M2\ucFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
SK-N-AS MoHVRZBweHSxc3nzJGF{e2G7 NF;rcZg2ODBibl2= NWLPT2tLPDhiaB?= NW[2fVdwcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M376NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
SK-N-DZ NFzzbG1CeG:ydH;zbZMhSXO|YYm= NF3xZmk2ODBibl2= M3;YOlQ5KGh? MoKxbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M4PGW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
THP-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLTfFNLOTJ3L{K1NE82ODBibl2= M2PXZlQ5KGh? Mmm1bY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NWm3N4h3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
MV4-11 NV;BfXdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjnNVI2NzJ3MD:1NFAhdk1? NWLIVHd2PDhiaB?= MknYbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NEfqSGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
U937 NV7MW|BLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPkNVI2NzJ3MD:1NFAhdk1? MVO0PEBp MYPpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NHTsdZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
HL-60 NYnROoxsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexNlUwOjVyL{WwNEBvVQ>? NVi4[IxnPDhiaB?= NXTmUGJQcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? M2jYflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEi0OlE1Lz5{NUC4OFYyPDxxYU6=
OCI-AML3 NFHtWXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVexNlUwOjVyL{WwNEBvVQ>? NEL2dYg1QCCq MmDkbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB6NE[xOEc,OjVyOES2NVQ9N2F-
MOLM-13 M4PIUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrQNVI2NzJ3MD:1NFAhdk1? MUC0PEBp MmLrbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MmLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOES2NVQoRjJ3MEi0OlE1RC:jPh?=
CMK MmHWR4VtdCCYaXHibYxqfHliQYPzZZk> NGXpRVIyOC1zMECwNEBvVQ>? NEG2bHk4OiCq NYnHUG9ZemWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4MkOzNUc,OjR7NkKzN|E9N2F-
CMY NXrqT2lFS2WubDDWbYFjcWyrdImgRZN{[Xl? NHG1cHkyOC1zMECwNEBvVQ>? MXS3NkBp NXGzbJQ4emWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?= NIDHSYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NlM{OSd-MkS5OlI{OzF:L3G+
Dayo NXqweXRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nmbWlEPTB;MUWwJI5O NVvvNmpyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OlE6OTBpPkK0OlYyQTFyPD;hQi=>
UW228 NGrTbnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ|MjDuUS=> Mm\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkG5NVAoRjJ2Nk[xPVExRC:jPh?=
IST-MES1 NVTJfJcxS2WubDDWbYFjcWyrdImgRZN{[Xl? MkfENVUxNzJ3MDDuUS=> M2jNTlczKGh? NF\zfGhmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NUe4Nkc,OjR|NkW3PFI9N2F-
IST-MES2 M2DEV2NmdGxiVnnhZoltcXS7IFHzd4F6 MmDONVUxNzJ3MDDuUS=> Mn;qO|IhcA>? M2O0XoVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NUe4Nkc,OjR|NkW3PFI9N2F-
REN M2nMS2NmdGxiVnnhZoltcXS7IFHzd4F6 NULtfIpuOTVyL{K1NEBvVQ>? MnnIO|IhcA>? M33OTYVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NHHufm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OVc5Oid-MkSzOlU4QDJ:L3G+
NCI-H2452 NH;kTJpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1[3U|E2OC9{NUCgcm0> NV7Te2RPPzJiaB?= NF60NFNmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NWLpWlNYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlU4QDJpPkK0N|Y2Pzh{PD;hQi=>
MSTO-211H Ml;kR4VtdCCYaXHibYxqfHliQYPzZZk> MXexOVAwOjVyIH7N NHHyRVI4OiCq NX\pWIVO\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NUe4Nkc,OjR|NkW3PFI9N2F-
NCI-H2052 MoT3R4VtdCCYaXHibYxqfHliQYPzZZk> MWCxOVAwOjVyIH7N MknMO|IhcA>? M3rUN4VvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NIK0eHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OVc5Oid-MkSzOlU4QDJ:L3G+
WEE1 M1TEN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TZNWlEPTB;NT6yJI5O MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ7OU[1OUc,OjN4OUm2OVU9N2F-
CDC2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvEb4FKSzVy78{eNVAxOCCwTR?= MlrkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OUm2OVUoRjJ|Nkm5OlU2RC:jPh?=
CDK7 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LUW2lEPTExvK6xNFAxKG6P NVfGdZN6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PVk3PTVpPkKzOlk6PjV3PD;hQi=>
MYT1 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2myOGlEPTB;NUOwJI5O NHfqPVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[5PVY2PSd-MkO2PVk3PTV:L3G+
T98G  Mm[1RZBweHSxc3nzJGF{e2G7 M{fuUlExOC9{NUCgcm0> NFTHZ203KGh? NYG2fJFq\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQh[2WubDDrbYxtcW6p MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl7Mke5N{c,OjF7OUK3PVM9N2F-
A549 MYfBdI9xfG:|aYOgRZN{[Xl? NEXaVlUzODBibl2= MoqyNUBp MmHBdoFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= M3LDOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{m5NFM{Lz5{MUe5PVA{OzxxYU6=
H460 NELIfZJCeG:ydH;zbZMhSXO|YYm= NXrvVZFIOjByIH7N MX[xJIg> M33ndZJi\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXy NITYZXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe5PVA{Oyd-MkG3PVkxOzN:L3G+
H1299 MV7BdI9xfG:|aYOgRZN{[Xl? NFjocFMzODBibl2= M122TVEhcA>? M1zyOJJi\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXy NYnoS|QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO|k6ODN|PD;hQi=>
Calu-6  NVPRSHd1SXCxcITvd4l{KEG|c3H5 M3vxXFIxOCCwTR?= NXPMfWp[OSCq MXPyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= MlLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OUmwN|MoRjJzN{m5NFM{RC:jPh?=
WiDr M2C4ZWtqdmG|ZTDBd5NigXN? MnX0NVAuOTByMECgcm0> M1zuSVghcA>? MYPpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gR2REOiCjdDDUfZIyPSC5aYToJIFvKEWFNUFCpJZidHWnIH;mJFg2KG6vb3yvUEBxemW2cnXheIVlKHerdHig[4Vu[2m2YXLpcoU> NYDHW5JQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PFc2PDVpPkG5PFg4PTR3PD;hQi=>
Function assay MXvFfJBqOjl|Rh?= MljuRolv\GmwZzDh[oZqdmm2eTD0c{Bz\WOxbXLpcoFvfCCqdX3hckBnfWyuLXzlcod1cCCQLYTldo1qdmGuIFjpd|gufGGpZ3XkJHdm\TFiKEGgeI8hPjR4IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hcHWvYX6gSZhxcTJ7M1[gZ4VtdHNiYYPz[ZN{\WRiYYOg[IV{e2:laXH0bY9vKGOxboP0ZY51KGK7IIH1ZY51cXSjdHn2[UBz\WGuLYTpcYUhWEOUIH3leIhw\CxiS3SgQUAxNjByM{Kg{txONg>? NYnZc2E2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
Function assay NVT4d5QyTXiyaUK5N2Y> MoPXRolv\GmwZzDh[oZqdmm2eTD0c{Bz\WOxbXLpcoFvfCCqdX3hckBnfWyuLXzlcod1cCCQLYTldo1qdmGuIFjpd|gufGGpZ3XkJHdm\TJiKEGgeI8hPTZ5IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hcHWvYX6gSZhxcTJ7M1[gZ4VtdHNiYYPz[ZN{\WRiYYOg[IV{e2:laXH0bY9vKGOxboP0ZY51KGK7IIH1ZY51cXSjdHn2[UBz\WGuLYTpcYUhWEOUIH3leIhw\CxiS3SgQUAxNjByM{mg{txONg>? NWDPbm5wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
Antiproliferative assay NUPjfW5xVUSDLV3CMVI{OQ>? NXjINJhTPzJiaILz M2DjR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCvZXHzeZJm\CCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFnDOVAhRSByLkK2JO69VS5? NF7sWXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3OCd-Mki3PVI4PjB:L3G+
Antiproliferative assay NUjqU3cxUEWNMkmzWC=> MoHCO|IhcHK| NXvpZoUzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUt{OUPUJINmdGy|IH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygTWM2OCB;IECuNlkh|ryPLh?= NFXndFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3OCd-Mki3PVI4PjB:L3G+
Antiproliferative assay NFPDPVJOVTGV M1fLRVczKGi{cx?= M1XZeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV2xV{Bk\WyuczDt[YF{fXKnZDDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGlEPTBiPTCwMlMyKM7:TT6= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Function assay MlTRTGVMOjl| Mmi0NUBpeg>? NV7DXoFTUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsJIxmdme2aDDQT21[XDFiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyC3c3nu[{BGTlNiKEK0O{B1dyB{NUmgdoV{cWS3ZYOpJIF{KHO3YoP0doF1\SCjZoTldkAyKGi{IHL5JIZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gbY1ufW6xYYPhfUwhU2liPTCwMlQ4KM7:TT6= Mm\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEGxPVMoRjJ7OUSxNVk{RC:jPh?=
Function assay M4Li[GhGUzJ7Mx?= M2LublEhcHJ? MXnJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxibHXu[5RpKFCNTWnUNUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJJV{cW6pIFXGV{ApOjR5IITvJFI2QSC{ZYPp[JVmeyliYYOgd5Vje3S{YYTlJIFnfGW{IEGgbJIh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCrbX31co9ie2G7LDDJR|UxKD1iND65OEDPxE1w M2Tpb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUSxNVk{Lz5{OUm0NVE6OzxxYU6=
Function assay NV;IT5JOVUSDLV3CMVI{OQ>? NUm2N3hpOC5zIITvJFExKHWP NXe1eJBWPiCqcoO= NYfLdnVvUW6qaXLpeIlwdiCxZjDX[YUyKGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gR2RMOSCyaH;zdIhwenmuYYTpc44h[XRiVInyJFE2KGG2IECuNUB1dyBzMDD1UUBi\nSncjC2JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k Mn7jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5OUK3OlAoRjJ6N{myO|YxRC:jPh?=
Function assay M2rxVmhGUzJ7M2S= MWOwMlEhfG9iMUCgeW0> NFzsV|U3KGi{cx?= NFXZeYlKdmirYnn0bY9vKG:oIGfl[VEhcW5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDDSGsyKHCqb4PwbI9zgWyjdHnvckBifCCWeYKxOUBifCByLkGgeI8hOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Function assay NFexSYZJTUt{OUPU NUfreYpOOC5zIITvJFExKHWP NH;xRYo3KGi{cx?= MXLJcohq[mm2aX;uJI9nKFCOS{GgbY4hUEWNMkmzWEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCWQ2TQJJBpd3OyaH;yfYxifGmxbjDheEAxNjFidH:gNVAhfU1iYX\0[ZIhPiCqcoOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? NXXjfoh4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
Function assay MUjNSGEuVUJvMkO= Mn7BNE4yKHSxIEGwJJVO MoKyOkBpenN? MXPJcohq[mm2aX;uJI9nKFCOS{GgbY4hcHWvYX6gUWRCNU2ELUKzJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKFSFVGCgdIhwe3Cqb4L5cIF1cW:wIHH0JFAvOSC2bzCxNEB2VSCjZoTldkA3KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MoHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5OUK3OlAoRjJ6N{myO|YxRC:jPh?=
qHTS assay NHTPc4hVSzN{ NEPlWINyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?= NHHvTGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M2PucnUuOiCRUx?= MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy| MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NEfmeFJCPjd| M2HndZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NUGzb|VVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NEDUb5NFSU:\ MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? NEfnS5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M4rhWHNid3NvMh?= NU\OU5BveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay MYLCWE0{Pw>? NEHGWpZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= M2f4clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M2rBTXJF NXL1WINneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| NF3HUIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NWLSbGxbW0tvTj3TTC=> M2DWW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz NG\uO|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NFzFU2lDXC1zMh?= M{TBb5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= M1zmTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay MV;ORlE3PDN? M1nGT5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NUn1Xpo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MlLCU2hUNTVy NEOxdVZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz M3GwWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M{XqcmJVNTF{ MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0yOiClZXzsdy=> NHrsdoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MnqxSGFQYQ>? M13ZSZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGRCV1liY3XscJM> NYPG[YoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MXLTT{1PNVOK M3S4V5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? NXG2dGJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MorVVog1OQ>? MkHPdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? NFz3OpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NHLFbYRCPjd| NUD2O|RJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NVrG[5lxVUdiNkOgLFYuXEdiUjm= MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NGqzV|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MUDVMVIhV1N? Mmi4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ MmO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay Mn74U2hUNTVy NH;wb2dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? MoHnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay M{HLd3JpPDF? MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NVjKZ41LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NIjRN2lTTA>? MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSSEBk\Wyucx?= MlXJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay M1XlU3NLNUeETUK= MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M4exWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay MVzTT{1PNU2F Mk\CdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NEe0S2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MWjORk1GSmNz M1zEXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NEPD[Wk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MWPMRW4uPQ>? MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? M17NUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay MX\SbFE5 NFLwWYFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= MlLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NWmyRpp3W0pvR1LNNi=> NWnQOWtieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= NGK5d2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MXnTZY9{NTJ? NECwSHByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBU[W:|LUKgZ4VtdHN? NX;kXGVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-Cdk1(Y15) / Cdk1 p-KAP1(S824) / p-Chk2(T68) / p-Chk1(S345) PARP / CF-PARP / pH3(S10) / p-CDC25c(S216) / p-CDK2(Y15) WEE1 25609063 25458954 27616351
Immunofluorescence tubulin / p-HH3(S10) γH2AX Cleaved caspase-3 / pH3 30755439 25609063 27616351
Growth inhibition assay Cell viability IC50 25458954 25084614
体内研究 MK-1775(~20 mg/kg)单独治疗对WiDr异种移植物表现出最小的抗肿瘤作用,在大鼠体内第3天时T/C为69%。在裸鼠HeLa-luc和TOV21G-shp53异种移植模型中,MK-1775单独的抗肿瘤效能是温和的。[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]

  • 体外激酶试验:

    使用重组人Wee1。激酶反应使用10 μM ATP,1.0 μCi of [γ-33P]ATP,和2.5 μg poly(Lys, Tyr)作为底物,在逐渐增加浓度的MK-1775存在下,在30°C环境中进行30分钟。整合到底物的放射性被捕获到MultiScreen-PH平板,在液体闪烁计数器上计数。

细胞实验:

[1]

  • Cell lines: WiDr,NCI-H1299,TOV21G,和 HeLa细胞
  • Concentrations: 在DMSO中溶解,终浓度为~10 μM
  • Incubation Time: 24小时
  • Method: 细胞在gemcitabine存在或不存在下处理24小时,然后用MK-1775再处理24小时。细胞活性使用SpectraMax通过WST-8试剂盒测定。细胞内caspase-3/7活性使用Caspase-3/7 Glo试剂盒测定。
动物实验:

[1]

  • Animal Models: 负荷WiDr,HeLa-luc,或TOV21G-shp53肿瘤的免疫缺陷裸鼠(F344/NJcl-rnu)
  • Dosages: ~20 mg/kg/day
  • Administration: 口服

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):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O

5mg/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 500.6
化学式

C27H32N8O2

CAS号 955365-80-7
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
NCT03668340 Recruiting Drug: AZD1775 Uterine Cancer Dana-Farber Cancer Institute|AstraZeneca October 22 2018 Phase 2
NCT03028766 Completed Drug: AZD1775|Drug: Cisplatin|Radiation: Radiotherapy Hypopharynx Squamous Cell Carcinoma|Oral Cavity Squamous Cell Carcinoma|Larynx Cancer University of Birmingham|AstraZeneca|Cancer Research UK June 22 2017 Phase 1
NCT03012477 Completed Drug: Cisplatin|Drug: AZD1775 Triple-negative Metastatic Breast Cancer Dana-Farber Cancer Institute|AstraZeneca January 18 2017 Phase 2

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

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常见问题及建议解决方法

问题 1:
How to prepare MK1775 methylcellulose solution? and how to prepare methylcellulose itself? Once make the MK1775 methylcellulose solution, how should i keep it?

回答:
MK1775 in 0.5% methylcellulose is a suspension or emulsion, and it is ok to treat mice orally. It is recommended to dissolve methylcellulose in saline. It will take some time to dissolve methylcellulose, and you can vortex it for a while. The MK1775 methylcellulose solution can be stored at 4°C for a week.

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