Adavosertib (MK-1775)

製品コード:S1525 別名:AZD1775

For research use only.

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.

Adavosertib (MK-1775)化学構造

CAS No. 955365-80-7

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 41500
JPY 30200
JPY 80000
JPY 170480

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(167)

製品安全説明書

Wee1阻害剤の選択性比較

相関Wee1製品

生物活性

製品説明 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.
特性 The first reported Wee1 inhibitor.
ターゲット
Wee1 [1]
(Cell-free assay)
5.2 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ASPC-1 NWe0SGhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NESwZXJKSzVyPUGzMlIhyrFiMT6xJO69VQ>? NFLkUYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS1PFk2PCd-MkW0OVg6PTR:L3G+
BxPC-3 Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIe0bXZKSzVyPUCuPEDDuSByLkCzJO69VQ>? NIe4Sm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS1PFk2PCd-MkW0OVg6PTR:L3G+
CFPAC-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXENm5KSzVyPUOuN{DDuSByLkKg{txO NILFcYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS1PFk2PCd-MkW0OVg6PTR:L3G+
HPAC NV7NNmVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvGVoNKUUN3ME2wMlUhyrFiMD6wNUDPxE1? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
MIAPaCa-2 MkHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3OzU2lEPTB;MD61JOKyKDBwMEWg{txO NGS0Xm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS1PFk2PCd-MkW0OVg6PTR:L3G+
PANC-1 M2exOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknCTWM2OD1zMD62JOKyKDFwMTFOwG0> M3PQblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEW4PVU1Lz5{NUS1PFk2PDxxYU6=
SK-N-BE (2) MmXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXxOFlNUUN3ME2yMlTjiIoEsfMAjVAvOyEQvF2= NX3VVmRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFg6OTZpPkK1N|A5QTF4PD;hQi=>
SK-N-BE (2), PAN→MK NVm1eVF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3YTWM2OD1{Nj625qCKyrIkgJm5MlYh|ryP MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOEmxOkc,OjV|MEi5NVY9N2F-
SK-N-BE (2), MK→PAN MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJwNPMAjeKy6oDLMD6zJO69VQ>? NIS0RoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPFkyPid-MkWzNFg6OTZ:L3G+
SK-N-AS NVvxRm5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILFdmZKSzVyPUCuOVDjiIoEsfMAjVAvODJizszN NI\Hepk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPFkyPid-MkWzNFg6OTZ:L3G+
SK-N-DZ NGjrWHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFf1RpJKSzVyPUCuN|bjiIoEsfMAjVAvODFizszN MmjjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-AS MWrBdI9xfG:|aYOgRZN{[Xl? NVvJSlczPTByIH7N NWHvR4pxPDhiaB?= NUS0TVlQcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MnznQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-DZ NHnQOGlCeG:ydH;zbZMhSXO|YYm= M{fx[FUxOCCwTR?= MWG0PEBp NGD4XZVqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MkXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
THP-1 MnLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYexNlUwOjVyL{WwNEBvVQ>? MmfnOFghcA>? MXTpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NHvhNYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
MV4-11 M2XPUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrPVZoyOjVxMkWwM|UxOCCwTR?= NGDUSpE1QCCq NVXEPIh3cW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NVflS4pYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
U937 NIjOSXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrWNHQyOjVxMkWwM|UxOCCwTR?= M4HMSFQ5KGh? NVfFNnZFcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NVzDNJlVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
HL-60 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3lWFYzOTJ3L{K1NE82ODBibl2= MmfOOFghcA>? M{jKd4lv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MnXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOES2NVQoRjJ3MEi0OlE1RC:jPh?=
OCI-AML3 NVLEVmJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkP2NVI2NzJ3MD:1NFAhdk1? MVm0PEBp M{DHe4lv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NWTkd3JGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
MOLM-13 M3[zb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWixNlUwOjVyL{WwNEBvVQ>? M4nIdFQ5KGh? MnXXbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NW\yd4pLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFQ3OTRpPkK1NFg1PjF2PD;hQi=>
CMK MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3u0OlExNTFyMECwJI5O MmPLO|IhcA>? M1HjOZJm\HWlZYOgZ4VtdCC4aXHsbYJqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl4MkOzNUc,OjR7NkKzN|E9N2F-
CMY NVOwR3J2S2WubDDWbYFjcWyrdImgRZN{[Xl? MYCxNE0yODByMDDuUS=> MkH0O|IhcA>? MmCzdoVlfWOnczDj[YxtKH[rYXzpZol1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? Mm\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkKzN|EoRjJ2OU[yN|MyRC:jPh?=
Dayo NInkcoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonkTWM2OD1zNUCgcm0> M1npW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[xPVExLz5{NE[2NVkyODxxYU6=
UW228 M{TNZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS0b5p6UUN3ME2yN|Ihdk1? M4DJZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[xPVExLz5{NE[2NVkyODxxYU6=
IST-MES1 Mmi4R4VtdCCYaXHibYxqfHliQYPzZZk> Mn;ONVUxNzJ3MDDuUS=> MV23NkBp MofH[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M3nkWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[1O|gzLz5{NEO2OVc5OjxxYU6=
IST-MES2 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{flNlE2OC9{NUCgcm0> MljNO|IhcA>? M4G3[oVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NHfPSFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OVc5Oid-MkSzOlU4QDJ:L3G+
REN NFX2U29E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MonxNVUxNzJ3MDDuUS=> MV63NkBp M3;rUIVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NG[x[3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OVc5Oid-MkSzOlU4QDJ:L3G+
NCI-H2452 NGDwV5VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYTyNmhqOTVyL{K1NEBvVQ>? NFz1Rog4OiCq Ml\I[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NIi4elI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OVc5Oid-MkSzOlU4QDJ:L3G+
MSTO-211H MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHH3WWwyPTBxMkWwJI5O MWG3NkBp NWDEd2VL\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NHS1[mQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OVc5Oid-MkSzOlU4QDJ:L3G+
NCI-H2052 MkPaR4VtdCCYaXHibYxqfHliQYPzZZk> NVf0TFhXOTVyL{K1NEBvVQ>? NV\ufZNxPzJiaB?= NWnzfGFV\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MnfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkW3PFIoRjJ2M{[1O|gzRC:jPh?=
WEE1 M3riTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr0T5NpUUN3ME21MlIhdk1? NY\QSWJXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PVk3PTVpPkKzOlk6PjV3PD;hQi=>
CDC2 NUDwXnBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LoOmlEPTExvK6xNFAxKG6P NWDSfHJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PVk3PTVpPkKzOlk6PjV3PD;hQi=>
CDK7 M{fSN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPkTWM2OO,:nkGwNFAhdk1? MkS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OUm2OVUoRjJ|Nkm5OlU2RC:jPh?=
MYT1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfoTWM2OD13M{Cgcm0> NUDTNZR3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PVk3PTVpPkKzOlk6PjV3PD;hQi=>
T98G  NEmxZ2pCeG:ydH;zbZMhSXO|YYm= MXqxNFAwOjVyIH7N NVHnWm11PiCq Mmfn[Y5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgZ4VtdCCtaXzsbY5o NIjNW3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm5Nlc6Oyd-MkG5PVI4QTN:L3G+
A549 NXr1cGRUSXCxcITvd4l{KEG|c3H5 MXeyNFAhdk1? MnK5NUBp MWjyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= M1joO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{m5NFM{Lz5{MUe5PVA{OzxxYU6=
H460 M2HacWFxd3C2b4Ppd{BCe3OjeR?= NYXoXG8{OjByIH7N NGTtd|AyKGh? MknjdoFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= NV3qfIlCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO|k6ODN|PD;hQi=>
H1299 NYXHOlh2SXCxcITvd4l{KEG|c3H5 NEXiWG8zODBibl2= M1\xR|EhcA>? MYfyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd7OUCzN{c,OjF5OUmwN|M9N2F-
Calu-6  M4TCd2Fxd3C2b4Ppd{BCe3OjeR?= MWKyNFAhdk1? NXv4d|h3OSCq NGP0eWlz[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=> NVrYVZd6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO|k6ODN|PD;hQi=>
WiDr MlHPT4lv[XOnIFHzd4F6ew>? M2jEelExNTFyMECwJI5O NXz0dGcyQCCq MVTpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gR2REOiCjdDDUfZIyPSC5aYToJIFvKEWFNUFCpJZidHWnIH;mJFg2KG6vb3yvUEBxemW2cnXheIVlKHerdHig[4Vu[2m2YXLpcoU> M1X6NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEi3OVQ2Lz5zOUi4O|U1PTxxYU6=
Function assay NXfw[XRpTXiyaUK5N2Y> NUPDdJNzSmmwZHnu[{Bi\m[rbnn0fUB1dyC{ZXPvcYJqdmGwdDDoeY1idiCodXzsMYxmdme2aDDOMZRmem2rbnHsJGhqezhvdHHn[4VlKFenZUGgLFEhfG9iNkS2JJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iaIXtZY4hTXiyaUK5N2Yh[2WubIOgZZN{\XO|ZXSgZZMh\GW|c3;jbYF1cW:wIHPvcpN1[W62IHL5JJF2[W62aYTheIl3\SC{ZXHsMZRqdWViUFPSJI1mfGixZDygT4QhRSByLkCwN|Ih|ryPLh?= NFXoeXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3OCd-Mki3PVI4PjB:L3G+
Function assay NFP3NJVGgHCrMkmzSi=> MnTrRolv\GmwZzDh[oZqdmm2eTD0c{Bz\WOxbXLpcoFvfCCqdX3hckBnfWyuLXzlcod1cCCQLYTldo1qdmGuIFjpd|gufGGpZ3XkJHdm\TJiKEGgeI8hPTZ5IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hcHWvYX6gSZhxcTJ7M1[gZ4VtdHNiYYPz[ZN{\WRiYYOg[IV{e2:laXH0bY9vKGOxboP0ZY51KGK7IIH1ZY51cXSjdHn2[UBz\WGuLYTpcYUhWEOUIH3leIhw\CxiS3SgQUAxNjByM{mg{txONg>? M1Hwd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Antiproliferative assay MXPNSGEuVUJvMkOx MliyO|IhcHK| MoKyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuSmy3ZTDhd5NigSxiSVO1NEA:KDBwMk[g{txONg>? M{fFclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Antiproliferative assay MoDsTGVMOjl|VB?= NGP4bIs4OiCqcoO= MnXIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDISWszQTOWIHPlcIx{KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuSmy3ZTDhd5NigSxiSVO1NEA:KDBwMkmg{txONg>? NYjvfFJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
Antiproliferative assay M1XhTW1OOVN? MXW3NkBpenN? NWP1U5A2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNUVFUKGOnbHzzJI1m[XO3cnXkJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhUUN3MDC9JFAvOzFizszNMi=> M3\uU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Function assay NXrWWHgzUEWNMkmz M3\j[FEhcHJ? NYrHW5VlUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsJIxmdme2aDDQT21[XDFiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyC3c3nu[{BGTlNiKEK0O{B1dyB{NUmgdoV{cWS3ZYOpJIF{KHO3YoP0doF1\SCjZoTldkAyKGi{IHL5JIZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gbY1ufW6xYYPhfUwhU2liPTCwMlQ4KM7:TT6= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl2MUG5N{c,Ojl7NEGxPVM9N2F-
Function assay NYXFXplbUEWNMkmz MnKyNUBpeg>? M{X3[WlvcGmkaYTpc44hd2ZiaIXtZY4h\nWubDDs[Y5ofGhiUFvNXXQyKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMhfXOrbnegSWZUKCh{NEegeI8hOjV7IILld4llfWW|KTDhd{B{fWK|dILheIUh[W[2ZYKgNUBpeiCkeTDmcJVwemW|Y3XuZ4UheG:uYYLpfoF1cW:wIHntcZVvd2G|YYmsJGlEPTBiPTC0Mlk1KM7:TT6= NWL4fXBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm5OFEyQTNpPkK5PVQyOTl|PD;hQi=>
Function assay M3LGem1FSS2PQj2yN|E> M2jwfFAvOSC2bzCxNEB2VQ>? NXLOT4ViPiCqcoO= NXTU[4dkUW6qaXLpeIlwdiCxZjDX[YUyKGmwIHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gR2RMOSCyaH;zdIhwenmuYYTpc44h[XRiVInyJFE2KGG2IECuNUB1dyBzMDD1UUBi\nSncjC2JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k NXfoUo5[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
Function assay MkHmTGVMOjl|VB?= MoGzNE4yKHSxIEGwJJVO NXXCeGJ{PiCqcoO= M4TYUWlvcGmkaYTpc44hd2ZiV3XlNUBqdiCKRVuyPVNVKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFPET|EheGixc4Doc5J6dGG2aX;uJIF1KFS7ckG1JIF1KDBwMTD0c{AyOCC3TTDh[pRmeiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Function assay M{W1OWhGUzJ7M2S= NGPJXmgxNjFidH:gNVAhfU1? M2fTelYhcHK| NES3RoFKdmirYnn0bY9vKG:oIGDMT|EhcW5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDUR3RRKHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= M4rUUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|YxLz5{OEe5Nlc3ODxxYU6=
Function assay NInsRZJOTEFvTVKtNlM> MWmwMlEhfG9iMUCgeW0> NWLifYRlPiCqcoO= NXe1XG13UW6qaXLpeIlwdiCxZjDQUGsyKGmwIHj1cYFvKE2GQT3NRk0zOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDUR3RRKHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= NVLpd3pjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O|kzPzZyPD;hQi=>
qHTS assay NXnBXXVUXEN|Mh?= MoXvdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? NIrmW5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NGq2fYRWNTJiT2O= NWXaW3NleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=> M4TWWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NV7lcGJ5STZ5Mx?= MoWxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? M1L6WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NEDKVFFFSU:\ M1rISJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| MoqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MX\TZY9{NTJ? NFLHbZlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay MUTCWE0{Pw>? M1;EdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MorwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay MlLSVmQ> MnHsdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NWG1ZXh3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MmW1V2suVi2VSB?= MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= NU\S[XM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay Mmj4RnQuOTJ? M17LUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= NFjDbWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M2nNeG5DOTZ2Mx?= MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| M3TjNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay MojsU2hUNTVy M4LVPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= MlT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NFfuUHdDXC1zMh?= MnX2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOTJiY3XscJM> NUHFSZFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NX\CXI9bTEGRWR?= NEGzeolyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBFSU:\IHPlcIx{ MmLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NF;JS4tUUy2QLWPI Mn3YdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? Mof3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NHLhOmRTcDRz NGf0fItyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= M{TvNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M2TQNGE3PzN? M2D3SJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq MljsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NYXONndyVUdiNkOgLFYuXEdiUjm= NIXjZnpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>? NI\BfVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M124dHUuOiCRUx?= M4DQW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay MWXPTHMuPTB? NFG0XY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? M1zvOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NULFbFRWWmh2MR?= MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NWXmPGRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay M{PxcHJF NGjUUZdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTTCClZXzsdy=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NIixdZVUUi2JQl2y MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M1GzdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay Ml[5V2suVi2PQx?= NIXjV21yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MlHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NXvFToNWVkJvRVLjNS=> NWnaTHRpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NW\rbJNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NUX5WHRMVEGQLUW= NX6zS45keUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NVL0W486RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NFHXZoxTcDF6 MoHZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NF\wWHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay MV7TTk1ISk1{ NUG5OFdteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M4XzeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay MnvxV4Fwey1{ MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> Mm\hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

  • 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.

細胞試験:

[1]

  • 細胞株:WiDr, NCI-H1299, TOV21G, and HeLa
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間:24 hours
  • 実験の流れ:

    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.

動物試験:

[1]

  • 動物モデル:Immunodeficient nude rats (F344/NJcl-rnu) bearing WiDr, HeLa-luc, or TOV21G-shp53 tumors
  • 投薬量:~20 mg/kg/day
  • 投与方法:Orally

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。

5mg/mL

化学情報

分子量 500.6
化学式

C27H32N8O2

CAS No. 955365-80-7
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CC(C)(C1=NC(=CC=C1)N2C3=NC(=NC=C3C(=O)N2CC=C)NC4=CC=C(C=C4)N5CCN(CC5)C)O

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

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)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

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よくある質問(FAQ)

質問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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