Adavosertib (MK-1775)

For research use only.

Catalog No.S1525 Synonyms: AZD1775

155 publications

Adavosertib (MK-1775) Chemical Structure

CAS No. 955365-80-7

Adavosertib (MK-1775, AZD1775) is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.

Selleck's Adavosertib (MK-1775) has been cited by 155 publications

Purity & Quality Control

Choose Selective Wee1 Inhibitors

Biological Activity

Description Adavosertib (MK-1775, AZD1775) is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.
Features The first reported Wee1 inhibitor.
Targets
Wee1 [1]
(Cell-free assay)
5.2 nM
In vitro

MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14). By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ASPC-1 NFXaXnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPjbmVWUUN3ME2xN{4zKMLzIEGuNUDPxE1? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
BxPC-3 NYK0XGl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37kbmlEPTB;MD64JOKyKDBwMEOg{txO M1z2PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEW4PVU1Lz5{NUS1PFk2PDxxYU6=
CFPAC-1 NXzPRVlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLmeGZ4UUN3ME2zMlMhyrFiMD6yJO69VQ>? M1HWbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEW4PVU1Lz5{NUS1PFk2PDxxYU6=
HPAC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnRdXFKSzVyPUCuOUDDuSByLkCxJO69VQ>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
MIAPaCa-2 NWS4bYNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Lze2lEPTB;MD61JOKyKDBwMEWg{txO M3XvRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEW4PVU1Lz5{NUS1PFk2PDxxYU6=
PANC-1 M{jRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zESGlEPTB;MUCuOkDDuSBzLkGg{txO MoHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2NUi5OVQoRjJ3NEW4PVU1RC:jPh?=
SK-N-BE (2) MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnZPJZNUUN3ME2yMlTjiIoEsfMAjVAvOyEQvF2= M{\TVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
SK-N-BE (2), PAN→MK NEOzZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJ4LkdihKnDueLCiUmuOkDPxE1? NH\DO|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPFkyPid-MkWzNFg6OTZ:L3G+
SK-N-BE (2), MK→PAN Mn;pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPNTlBbUUN3ME2yMlTjiIoEsfMAjVAvOyEQvF2= NHPRTYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPFkyPid-MkWzNFg6OTZ:L3G+
SK-N-AS M1vycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXCN2JrUUN3ME2wMlUx6oDLwsJihKkxNjB{IN88US=> MkPWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-DZ NXi3eXhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DaNmlEPTB;MD6zOwKBkcLz4pEJNE4xOSEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOEmxOkc,OjV|MEi5NVY9N2F-
SK-N-AS NYfLb4pjSXCxcITvd4l{KEG|c3H5 NUHsVJI4PTByIH7N NInmdWU1QCCq MW\pcoR2[2W|IHPlcIwh[XCxcITvd4l{ M3nPbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
SK-N-DZ NYO5cGRESXCxcITvd4l{KEG|c3H5 NX2xdoJkPTByIH7N NV;UVlB2PDhiaB?= MorwbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOEmxOkc,OjV|MEi5NVY9N2F-
THP-1 MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHvbppiOTJ3L{K1NE82ODBibl2= NHTUOmM1QCCq NF76UldqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NXX1T4Y5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
MV4-11 NHS3NVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWP3RXJpOTJ3L{K1NE82ODBibl2= MXe0PEBp Mk[5bY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NWX3e3BKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
U937 M1rIW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTYSmtUOTJ3L{K1NE82ODBibl2= MmPrOFghcA>? NEDUVXFqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NFzYUFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
HL-60 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nlelEzPS9{NUCvOVAxKG6P NYS1UWZQPDhiaB?= Mor0bY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NIHINYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
OCI-AML3 NH;KPWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxNlUwOjVyL{WwNEBvVQ>? M1TnflQ5KGh? MlTSbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NGrRW449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
MOLM-13 NWi2WHd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNlUwOjVyL{WwNEBvVQ>? NGXI[2U1QCCq MY\pcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MnfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOES2NVQoRjJ3MEi0OlE1RC:jPh?=
CMK Mn7VR4VtdCCYaXHibYxqfHliQYPzZZk> MkLMNVAuOTByMECgcm0> MoTmO|IhcA>? NYnJd41temWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?= MkfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkKzN|EoRjJ2OU[yN|MyRC:jPh?=
CMY NYrj[G5FS2WubDDWbYFjcWyrdImgRZN{[Xl? MkDXNVAuOTByMECgcm0> NIO3[o44OiCq MXPy[YR2[2W|IHPlcIwhfmmjbHnibZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NFzpOVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NlM{OSd-MkS5OlI{OzF:L3G+
Dayo MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF3MDDuUS=> MlnyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkG5NVAoRjJ2Nk[xPVExRC:jPh?=
UW228 M3jSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnzNmVbUUN3ME2yN|Ihdk1? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ4MUmxNEc,OjR4NkG5NVA9N2F-
IST-MES1 NYTOTpczS2WubDDWbYFjcWyrdImgRZN{[Xl? NFrENIwyPTBxMkWwJI5O Mn3rO|IhcA>? NX\GZohC\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NUnuO|FlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlU4QDJpPkK0N|Y2Pzh{PD;hQi=>
IST-MES2 NUjnS3FPS2WubDDWbYFjcWyrdImgRZN{[Xl? M2DBSVE2OC9{NUCgcm0> M2nDTlczKGh? NXOzdVVw\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NV[yNXpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlU4QDJpPkK0N|Y2Pzh{PD;hQi=>
REN M2\0O2NmdGxiVnnhZoltcXS7IFHzd4F6 NF33OlQyPTBxMkWwJI5O NVTPclZjPzJiaB?= MWPlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NUXXRZNnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlU4QDJpPkK0N|Y2Pzh{PD;hQi=>
NCI-H2452 NYeyPXNJS2WubDDWbYFjcWyrdImgRZN{[Xl? NFPNSocyPTBxMkWwJI5O NHTuT3A4OiCq NIDs[HlmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NVyzdoJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlU4QDJpPkK0N|Y2Pzh{PD;hQi=>
MSTO-211H MorXR4VtdCCYaXHibYxqfHliQYPzZZk> MYmxOVAwOjVyIH7N Mk\SO|IhcA>? MnG0[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NWqzdHdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlU4QDJpPkK0N|Y2Pzh{PD;hQi=>
NCI-H2052 M{fFeWNmdGxiVnnhZoltcXS7IFHzd4F6 NEm5cWwyPTBxMkWwJI5O NVjJenhXPzJiaB?= NWr6N41R\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MmLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkW3PFIoRjJ2M{[1O|gzRC:jPh?=
WEE1 NWnZZ4ZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe4TWM2OD13LkKgcm0> M{LhOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nkm5OlU2Lz5{M{[5PVY2PTxxYU6=
CDC2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITqdYRKSzVy78{eNVAxOCCwTR?= NX7OZ4FSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PVk3PTVpPkKzOlk6PjV3PD;hQi=>
CDK7 NI\iSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|Ux97zgMUCwNEBvVQ>? NG\YOlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[5PVY2PSd-MkO2PVk3PTV:L3G+
MYT1 NWLTWo5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTV|MDDuUS=> NFLOd4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[5PVY2PSd-MkO2PVk3PTV:L3G+
T98G  MW\BdI9xfG:|aYOgRZN{[Xl? Mo\3NVAxNzJ3MDDuUS=> MUS2JIg> NY\GS2RE\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQh[2WubDDrbYxtcW6p MlO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7OUK3PVMoRjJzOUmyO|k{RC:jPh?=
A549 NVf6[WI6SXCxcITvd4l{KEG|c3H5 NVvHfodTOjByIH7N NFi4THYyKGh? MWPyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd7OUCzN{c,OjF5OUmwN|M9N2F-
H460 MkDtRZBweHSxc3nzJGF{e2G7 MXSyNFAhdk1? Moq3NUBp NEnSbXlz[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=> NYjOWos6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO|k6ODN|PD;hQi=>
H1299 M1K3dWFxd3C2b4Ppd{BCe3OjeR?= NX7pSHUxOjByIH7N NEH4WlcyKGh? NX;TT4JNemGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI> NVHC[I9{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO|k6ODN|PD;hQi=>
Calu-6  M4fWWWFxd3C2b4Ppd{BCe3OjeR?= NU\LVmhrOjByIH7N NVPzUGJDOSCq NYfDSIZnemGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI> MnHuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OUmwN|MoRjJzN{m5NFM{RC:jPh?=
WiDr M{PQOGtqdmG|ZTDBd5NigXN? NUXFNWU5OTBvMUCwNFAhdk1? MYm4JIg> M{THWolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBETEN{IHH0JHR6ejF3IIfpeIgh[W5iRVO1NOKhfmGudXWgc4YhQDVibn3vcE9NKHC{ZYTy[YF1\WRid3n0bEBo\W2laYThZolv\Q>? NHLvSoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4O|U1PSd-MUm4PFc2PDV:L3G+
Function assay NHv4bVVGgHCrMkmzSi=> MmLPRolv\GmwZzDh[oZqdmm2eTD0c{Bz\WOxbXLpcoFvfCCqdX3hckBnfWyuLXzlcod1cCCQLYTldo1qdmGuIFjpd|gufGGpZ3XkJHdm\TFiKEGgeI8hPjR4IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hcHWvYX6gSZhxcTJ7M1[gZ4VtdHNiYYPz[ZN{\WRiYYOg[IV{e2:laXH0bY9vKGOxboP0ZY51KGK7IIH1ZY51cXSjdHn2[UBz\WGuLYTpcYUhWEOUIH3leIhw\CxiS3SgQUAxNjByM{Kg{txONg>? M1fWfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Function assay NITWT|BGgHCrMkmzSi=> MVfCbY5lcW6pIHHm[olvcXS7IITvJJJm[2:vYnnuZY51KGi3bXHuJIZ2dGxvbHXu[5RpKE5vdHXycYlv[WxiSHnzPE11[WepZXSgW4VmOiBqMTD0c{A2PjdicnXzbYR2\XNrIHX4dJJme3OnZDDpckBpfW2jbjDFfJBqOjl|RjDj[YxteyCjc4Pld5Nm\CCjczDk[ZN{d2OrYYTpc44h[2:wc4ThcpQh[nlicYXhcpRqfGG2aY\lJJJm[WxvdHnt[UBRS1JibXX0bI9lNCCNZDC9JFAvODB|OTFOwG0v M1r2U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Antiproliferative assay NE\JU5JOTEFvTVKtNlMy MmHXO|IhcHK| NHH5NmFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNibXXhd5Vz\WRiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDJR|UxKD1iMD6yOkDPxE1w NGjqWXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3OCd-Mki3PVI4PjB:L3G+
Antiproliferative assay MWHISWszQTOW NHPJVIY4OiCqcoO= NX\XbYMySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUt{OUPUJINmdGy|IH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygTWM2OCB;IECuNlkh|ryPLh?= M4S4blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Antiproliferative assay NXnWUpROVU1zUx?= MmHXO|IhcHK| NHvR[FNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3NNXMh[2WubIOgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3CcJVmKGG|c3H5MEBKSzVyIE2gNE4{OSEQvF2u MlfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5OUK3OlAoRjJ6N{myO|YxRC:jPh?=
Function assay MVfISWszQTN? NH\QXlAyKGi{ MVjJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxibHXu[5RpKFCNTWnUNUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJJV{cW6pIFXGV{ApOjR5IITvJFI2QSC{ZYPp[JVmeyliYYOgd5Vje3S{YYTlJIFnfGW{IEGgbJIh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCrbX31co9ie2G7LDDLbUA:KDBwNEeg{txONg>? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MUG5N{c,Ojl7NEGxPVM9N2F-
Function assay M33FNGhGUzJ7Mx?= M4rMSlEhcHJ? MYLJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxibHXu[5RpKFCNTWnUNUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJJV{cW6pIFXGV{ApOjR5IITvJFI2QSC{ZYPp[JVmeyliYYOgd5Vje3S{YYTlJIFnfGW{IEGgbJIh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCrbX31co9ie2G7LDDJR|UxKD1iND65OEDPxE1w NYfqVnE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFEyQTNpPkK5PVQyOTl|PD;hQi=>
Function assay MmTlUWRCNU2ELUKzNS=> MWSwMlEhfG9iMUCgeW0> MX:2JIhzew>? MU\Jcohq[mm2aX;uJI9nKFenZUGgbY4hcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCFRFuxJJBpd3OyaH;yfYxifGmxbjDheEBVgXJiMUWgZZQhOC5zIITvJFExKHWPIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? M2TuZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Function assay NXmzNYVqUEWNMkmzWC=> MoPlNE4yKHSxIEGwJJVO MorQOkBpenN? MmqwTY5pcWKrdHnvckBw\iCZZXWxJIlvKEiHS{K5N3Qh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iQ1TLNUBxcG:|cHjvdplt[XSrb36gZZQhXHm{MUWgZZQhOC5zIITvJFExKHWPIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Function assay MVPISWszQTOW MY[wMlEhfG9iMUCgeW0> MUK2JIhzew>? NETDUnJKdmirYnn0bY9vKG:oIGDMT|EhcW5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDUR3RRKHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= MorJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5OUK3OlAoRjJ6N{myO|YxRC:jPh?=
Function assay NXnsW2puVUSDLV3CMVI{ NHzNSowxNjFidH:gNVAhfU1? M2jVSFYhcHK| MoXSTY5pcWKrdHnvckBw\iCSTFuxJIlvKGi3bXHuJG1FSS2PQj2yN{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCWQ2TQJJBpd3OyaH;yfYxifGmxbjDheEAxNjFidH:gNVAhfU1iYX\0[ZIhPiCqcoOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? NYHpc2FIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
qHTS assay M4TQdXREOzJ? NWjQSXRqeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGTDN|Ih[2WubIO= NYHxZ2l1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MWTVMVIhV1N? NIjufZFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVT2yJG9UKGOnbHzz MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay M33MN2E3PzN? MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MlHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NVvVeZRKTEGRWR?= MlLEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? MmW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay M174cHNid3NvMh?= NHLSb3FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz NV;ad3VnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay M2TBeGJVNTN5 M2nJOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MnPvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MVrSSC=> MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> MlTCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MkDyV2suVi2VSB?= NH6x[WVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay MWnCWE0yOg>? M{XLOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= NWrnfol{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay Mo\pUmIyPjR| MkTxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NHqybIJQUFNvNUC= NHLaN|ByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NFXP[5FDXC1zMh?= NITITYVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1zMjDj[Yxtew>? NYTzZ20zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MkTwSGFQYQ>? MlfqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgSGFQYSClZXzsdy=> MkjIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NYT5[odHW0tvTj3TTC=> MmfOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? NHP5O3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MXfSbFQy NXf6VlJQeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= NH;Hb5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M17G[2E3PzN? NXPLRXBLeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? NWTYZnRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay Mn74UWchPjNiKE[tWGchWil? NFn3fnhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? NELhWFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NWj1RnQ4XS1{IF;T M3vmXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? M2jlXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NF25XnZQUFNvNUC= NEfUNo1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? MnrEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MlntVog1OQ>? MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NYLIbollRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NGPlR5VTTA>? MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSSEBk\Wyucx?= NYnjRVM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MVzTTk1ISk1{ MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M3fLb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M2rIXnNMNU5vTVO= NGPHb5ByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NX6yZoxCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay M13aTG5DNUWEY{G= NUXxZXNYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NFPSZ|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M1HwOGxCVi13 NFrVcWFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NFHuT2RTcDF6 NYnYUGpEeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= Mne3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NVS0Wm5bW0pvR1LNNi=> M3;nZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNLNUeETUKgZ4VtdHN? NGnoVGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NEjaOY1U[W:|LUK= MnXwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ MnP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Cdk1(Y15) / Cdk1; 

PubMed: 25609063     


The impact of a 24 hour pre-treatment of MK-1775 on p-Cdk1 was assessed by western blotting. Because of low basal phosphorylation, GBM22 was irradiated (RT) with 10 Gy.

p-KAP1(S824) / p-Chk2(T68) / p-Chk1(S345); 

PubMed: 25609063     


Western blot evaluation of GBM6 and GBM22 short-term explant cultures 24 hours after treatment with either MK-1775 or TMZ or the combination. 

PARP / CF-PARP / pH3(S10) / p-CDC25c(S216) / p-CDK2(Y15); 

PubMed: 25458954     


Pancreatic cancer cells were treated with vehicle control or 500 nM MK-1775 for 48 h. Whole cell lysates were subjected to Western blotting and probed with anti-PARP, -p-H3, -γH2AX, -p-CHK1, -CHK1, -p-CDC25C, -p-CDK1, - CDK1, -p-CDK2, -CDK2, or -β-actin antibody.

WEE1; 

PubMed: 27616351     


MIA PaCa2, PANC-1, Hs 766T, Capan-1 and PL11 cells were treated with MK-1775 (400 nM/L) and/or MMC (150 nM/L) for 24 hours. Whole cell lysates were prepared using RIPA and western blot was performed to assess the protein expression of WEE1 (90 kDa), pCDK1(y15) (34 kDa), CDK1 (34 kDa) and GAPDH (36 kDa) as loading control. 

25609063 25458954 27616351
Immunofluorescence
tubulin / p-HH3(S10); 

PubMed: 30755439     


FaDu and UNC7 cells were treated with adavosertib (500 nM), alisertib (250 nM), or adavosertib + alisertib for 24 hours and followed by immunofluorescent staining with anti-tubulin (Green) and anti-pHH3 (S10; Red). Nucleus was stained with DAPI. (A) Representative images of mitotic cells were captured by confocal microscopy. Scale bar: 10 µm.

γH2AX; 

PubMed: 25609063     


A) γH2AX foci formation in GBM6 and GBM22 were assessed 24 h after a single treatment of 300 nM MK-1775. 

Cleaved caspase-3 / pH3; 

PubMed: 27616351     


MIA PaCa2 cells were treated and dual stained with pH3 to observe mitotic entry; and cleaved caspase 3 (CL-CSP3) to observe caspase 3 activity.

30755439 25609063 27616351
Growth inhibition assay
Cell viability; 

PubMed: 25458954     


Pancreatic cancer cell lines were cultured in 96-well plates at 37℃ for 48 h in complete medium with variable concentrations of MK-1775 and viable cell numbers were determined using MTT reagent and a microplate reader. The data are presented as means ± standard errors from at least 3 independent experiments.

IC50; 

PubMed: 25084614     


AML cell lines were cultured for 72 h in complete medium with variable concentrations of MK-1775 (MK) and viable cell numbers were determined using MTT assays. IC50 values were calculated as drug concentration necessary to inhibit 50% growth compared to untreated control cells.

25458954 25084614
In vivo MK-1775 treatment alone at ~20 mg/kg displays minimal antitumor effects against WiDr xenografts in rats with T/C of 69% at day 3. Antitumor efficacy by MK-1775 alone in the nude rat HeLa-luc and TOV21G-shp53 xenograft models is also moderate. [1]

Protocol

Kinase Assay:

[1]

- Collapse

In vitro kinase assays:

Recombinant human Wee1 is used. Kinase reaction is conducted with 10 μM ATP, 1.0 μCi of [γ-33P]ATP, and 2.5 μg of poly(Lys, Tyr) as a substrate in the presence of increasing concentrations of MK-1775 at 30°C for 30 minutes. Radioactivity incorporated into the substrate is trapped on MultiScreen-PH plates and is counted on a liquid scintillation counter.
Cell Research:

[1]

- Collapse
  • Cell lines: WiDr, NCI-H1299, TOV21G, and HeLa
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 hours
  • Method:

    Cells are treated with or without gemcitabine for 24 hours, then with MK-1775 for an additional 24 hours. Cell viability is determined with a WST-8 kit using SpectraMax. Cellular caspase-3/7 activities are determined with a Caspase-3/7 Glo kit.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Immunodeficient nude rats (F344/NJcl-rnu) bearing WiDr, HeLa-luc, or TOV21G-shp53 tumors
  • Dosages: ~20 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (159.8 mM)
Water 0.0001 mg/mL (0.0 mM)
Ethanol ''10 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 500.6
Formula

C27H32N8O2

CAS No. 955365-80-7
Storage powder
in solvent
Synonyms AZD1775
Smiles CC(C)(C1=NC(=CC=C1)N2C3=NC(=NC=C3C(=O)N2CC=C)NC4=CC=C(C=C4)N5CCN(CC5)C)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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.

Wee1 Signaling Pathway Map

Related Wee1 Products

Tags: buy Adavosertib (MK-1775) | Adavosertib (MK-1775) supplier | purchase Adavosertib (MK-1775) | Adavosertib (MK-1775) cost | Adavosertib (MK-1775) manufacturer | order Adavosertib (MK-1775) | Adavosertib (MK-1775) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID