Adavosertib (MK-1775)

For research use only. Not for use in humans.

目录号：S1525 别名： AZD1775

Adavosertib (MK-1775) Chemical Structure

CAS No. 955365-80-7

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。

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库存

购买数量

10mM (1mL in DMSO)	RMB 1960.96	现货
5mg	RMB 1376.38	现货
10mg	RMB 2226.67	现货
25mg	RMB 3835.28	现货
50mg	RMB 6297.29	现货
100mg	RMB 9582.3	现货
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客户使用Selleck生产的Adavosertib (MK-1775)发表文献163篇：

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产品安全说明书

Wee1抑制剂选择性比较

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	Activity Description	PMID
ASPC-1	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NF\UUHZKSzVyPUGzMlIhyrFiMT6xJO69VQ>?	NET5T4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS1PFk2PCd-MkW0OVg6PTR:L3G+
BxPC-3	M3fsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NGLMdXBKSzVyPUCuPEDDuSByLkCzJO69VQ>?	NXfJRpFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0OVg6PTRpPkK1OFU5QTV2PD;hQi=>
CFPAC-1	NXnDVYZVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NH3COmNKSzVyPUOuN{DDuSByLkKg{txO	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
HPAC	MmXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NH\iN4tKSzVyPUCuOUDDuSByLkCxJO69VQ>?	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
MIAPaCa-2	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MlPjTWM2OD1yLkWgxtEhOC5yNTFOwG0>	M{j3dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEW4PVU1Lz5{NUS1PFk2PDxxYU6=
PANC-1	NF20XWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M2PQZ2lEPTB;MUCuOkDDuSBzLkGg{txO	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR3OEm1OEc,OjV2NUi5OVQ9N2F-
SK-N-BE (2)	NFj0U3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MYDJR\|UxRTJwNPMAjeKy6oDLMD6zJO69VQ>?	MkPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-BE (2), PAN→MK	MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M{[1OmlEPTB;Mk[uOwKBkcLz4pEJPU43KM7:TR?=	MorzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-BE (2), MK→PAN	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NHfMeVJKSzVyPUKuOQKBkcLz4pEJNE4{KM7:TR?=	Ml;mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|MEi5NVYoRjJ3M{C4PVE3RC:jPh?=
SK-N-AS	M1H1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M{TCPWlEPTB;MD61NQKBkcLz4pEJNE4xOiEQvF2=	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOEmxOkc,OjV\|MEi5NVY9N2F-
SK-N-DZ	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M1rx[mlEPTB;MD6zOwKBkcLz4pEJNE4xOSEQvF2=	NFP1Ro49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPFkyPid-MkWzNFg6OTZ:L3G+
SK-N-AS	M1XMTWFxd3C2b4Ppd{BCe3OjeR?=	NX;lNI1iPTByIH7N	NH\zSHQ1QCCq	MonsbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>?	M3XFRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
SK-N-DZ	M1nYemFxd3C2b4Ppd{BCe3OjeR?=	NITOcWM2ODBibl2=	M3PlR\|Q5KGh?	MULpcoR2[2W\|IHPlcIwh[XCxcITvd4l{	M1fTd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C4PVE3Lz5{NUOwPFkyPjxxYU6=
THP-1	Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYKxNlUwOjVyL{WwNEBvVQ>?	MoLYOFghcA>?	MUTpcoNz\WG\|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=>	M1\qWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEi0OlE1Lz5{NUC4OFYyPDxxYU6=
MV4-11	M1y1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1yzW\|EzPS9{NUCvOVAxKG6P	NVK1dnoxPDhiaB?=	MVPpcoNz\WG\|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=>	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB6NE[xOEc,OjVyOES2NVQ9N2F-
U937	MoLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NYLwSGFzOTJ3L{K1NE82ODBibl2=	NYKwXYtpPDhiaB?=	NFLs[4NqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>?	Mke5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOES2NVQoRjJ3MEi0OlE1RC:jPh?=
HL-60	M2jYWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M170XlEzPS9{NUCvOVAxKG6P	M3jxVVQ5KGh?	MUHpcoNz\WG\|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=>	NELyXYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
OCI-AML3	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEKzbIIyOjVxMkWwM\|UxOCCwTR?=	MoL0OFghcA>?	NVu1V2pycW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ?	NFvMSGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4OFYyPCd-MkWwPFQ3OTR:L3G+
MOLM-13	NFPuVphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVfkb\|BYOTJ3L{K1NE82ODBibl2=	MknpOFghcA>?	M1i4[Ilv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz	M1u3[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEi0OlE1Lz5{NUC4OFYyPDxxYU6=
CMK	M1rKSmNmdGxiVnnhZoltcXS7IFHzd4F6	MV6xNE0yODByMDDuUS=>	NXXmfVhYPzJiaB?=	MUHy[YR2[2W\|IHPlcIwhfmmjbHnibZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz	NF3ZcVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm2NlM{OSd-MkS5OlI{OzF:L3G+
CMY	NEe5[pdE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NG\VOVYyOC1zMECwNEBvVQ>?	NXv0[ZA5PzJiaB?=	NFToXnpz\WS3Y3XzJINmdGxidnnhcIljcXS7IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{	MmnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7NkKzN\|EoRjJ2OU[yN\|MyRC:jPh?=
Dayo	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M3m2[WlEPTB;MUWwJI5O	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ4MUmxNEc,OjR4NkG5NVA9N2F-
UW228	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NHLYZZJKSzVyPUKzNkBvVQ>?	NV\NeIlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OlE6OTBpPkK0OlYyQTFyPD;hQi=>
IST-MES1	MnfRR4VtdCCYaXHibYxqfHliQYPzZZk>	Mke2NVUxNzJ3MDDuUS=>	MUW3NkBp	MnfJ[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NUe4Nkc,OjR\|NkW3PFI9N2F-
IST-MES2	M4ixV2NmdGxiVnnhZoltcXS7IFHzd4F6	Mo[4NVUxNzJ3MDDuUS=>	MXu3NkBp	M1z4V4VvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>?	MlrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR\|NkW3PFIoRjJ2M{[1O\|gzRC:jPh?=
REN	MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NUXxV4Z7OTVyL{K1NEBvVQ>?	NXjxSXV[PzJiaB?=	MmPT[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NUe4Nkc,OjR\|NkW3PFI9N2F-
NCI-H2452	NGnDcWRE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	NFKwfWUyPTBxMkWwJI5O	NXKzeINwPzJiaB?=	Mn30[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz	Mn3RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR\|NkW3PFIoRjJ2M{[1O\|gzRC:jPh?=
MSTO-211H	MoL6R4VtdCCYaXHibYxqfHliQYPzZZk>	NEPTdHgyPTBxMkWwJI5O	MX63NkBp	Mlvq[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz	MkD2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR\|NkW3PFIoRjJ2M{[1O\|gzRC:jPh?=
NCI-H2052	MmXIR4VtdCCYaXHibYxqfHliQYPzZZk>	MV2xOVAwOjVyIH7N	NHv2V3U4OiCq	M33Bc4VvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>?	M33GTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[1O\|gzLz5{NEO2OVc5OjxxYU6=
WEE1	NHHJc\|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MUHJR\|UxRTVwMjDuUS=>	M4npUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|Nkm5OlU2Lz5{M{[5PVY2PTxxYU6=
CDC2	Mn\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MW\JR\|Ux97zgMUCwNEBvVQ>?	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ7OU[1OUc,OjN4OUm2OVU9N2F-
CDK7	NXLXWpNUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M17oWmlEPTExvK6xNFAxKG6P	MkO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OUm2OVUoRjJ\|Nkm5OlU2RC:jPh?=
MYT1	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M{W1fGlEPTB;NUOwJI5O	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ7OU[1OUc,OjN4OUm2OVU9N2F-
T98G	MX;BdI9xfG:\|aYOgRZN{[Xl?	M4jUfFExOC9{NUCgcm0>	M{XFXlYhcA>?	MmG0[Y5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgZ4VtdCCtaXzsbY5o	NUnxSnNuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5PVI4QTNpPkKxPVkzPzl\|PD;hQi=>
A549	MYnBdI9xfG:\|aYOgRZN{[Xl?	NXm4O5VkOjByIH7N	M1zLblEhcA>?	NWXR[mxUemGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI>	NUG2NHhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO\|k6ODN\|PD;hQi=>
H460	MYjBdI9xfG:\|aYOgRZN{[Xl?	NUXmd3VwOjByIH7N	NUfxOJNQOSCq	NHezdG1z[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=>	NHHIZYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUe5PVA{Oyd-MkG3PVkxOzN:L3G+
H1299	M1XXc2Fxd3C2b4Ppd{BCe3OjeR?=	Mnz2NlAxKG6P	MmHuNUBp	Mkf4doFlcW:\|ZX7zbZRqgmW\|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK=	MoDZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF5OUmwN\|MoRjJzN{m5NFM{RC:jPh?=
Calu-6	M4HQSmFxd3C2b4Ppd{BCe3OjeR?=	NGXFWJIzODBibl2=	MX6xJIg>	MYPyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?=	NVu2V4x{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3PVkxOzNpPkKxO\|k6ODN\|PD;hQi=>
WiDr	MUnLbY5ie2ViQYPzZZl{	Moi5NVAuOTByMECgcm0>	MXq4JIg>	M4\Pc4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBETEN{IHH0JHR6ejF3IIfpeIgh[W5iRVO1NOKhfmGudXWgc4YhQDVibn3vcE9NKHC{ZYTy[YF1\WRid3n0bEBo\W2laYThZolv\Q>?	NFfrUo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi4O\|U1PSd-MUm4PFc2PDV:L3G+
Function assay	Mnr5SZhxcTJ7M1[=			M2\xc2JqdmSrbnegZYZncW6rdImgeI8hemWlb33ibY5idnRiaIXtZY4h\nWubD3s[Y5ofGhiTj30[ZJucW6jbDDIbZM5NXSjZ3fl[EBY\WVzIDixJJRwKDZ2NjDy[ZNq\HWnczmg[ZhxemW\|c3XkJIlvKGi3bXHuJGV5eGl{OUPGJINmdGy\|IHHzd4V{e2WmIHHzJIRme3OxY3nheIlwdiClb37zeIFvfCCkeTDxeYFvfGm2YYTpeoUhemWjbD30bY1mKFCFUjDt[ZRpd2RuIFvkJF0hOC5yMEOyJO69VS5?	M122T\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO\|YxLz5{OEe5Nlc3ODxxYU6=
Function assay	MXPFfJBqOjl\|Rh?=			NEfzWnlDcW6maX7nJIFn\mmwaYT5JJRwKHKnY3;tZolv[W62IHj1cYFvKG[3bHytcIVv\3SqIF6teIVzdWmwYXygTIl{QC22YXfn[YQhX2WnMjCoNUB1dyB3NkegdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCqdX3hckBGgHCrMkmzSkBk\WyuczDhd5Nme3OnZDDhd{Bl\XO\|b3PpZZRqd25iY3;ud5RidnRiYomgdZVidnSrdHH0bZZmKHKnYXyteIlu\SCSQ2KgcYV1cG:mLDDL[EA:KDBwMECzPUDPxE1w	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Antiproliferative assay	MVvNSGEuVUJvMkOx		M3nH[\|czKGi{cx?=	NGr4THBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNibXXhd5Vz\WRiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDJR\|UxKD1iMD6yOkDPxE1w	M3\GdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO\|YxLz5{OEe5Nlc3ODxxYU6=
Antiproliferative assay	NYDpT3NKUEWNMkmzWC=>		M{jFcVczKGi{cx?=	NVjrUlB[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUt{OUPUJINmdGy\|IH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygTWM2OCB;IECuNlkh\|ryPLh?=	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Antiproliferative assay	M{LiOG1OOVN?		MYC3NkBpenN?	NFXiN3JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3NNXMh[2WubIOgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3CcJVmKGG\|c3H5MEBKSzVyIE2gNE4{OSEQvF2u	NH\RVo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3OCd-Mki3PVI4PjB:L3G+
Function assay	NWXl[41OUEWNMkmz		NEXIOXQyKGi{	MmLXTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCSS13ZWFEh\XiycnXzd4VlKGmwIFjFT\|I6OyClZXzsd{B2e2mwZzDFSnMhMDJ2NzD0c{AzPTlicnXzbYR2\XNrIHHzJJN2[nO2cnH0[UBi\nSncjCxJIhzKGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iaX3teY5w[XOjeTygT4khRSByLkS3JO69VS5?	NGnsTYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm0NVE6Oyd-Mkm5OFEyQTN:L3G+
Function assay	MVnISWszQTN?		MXOxJIhz	MXXJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxibHXu[5RpKFCNTWnUNUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJJV{cW6pIFXGV{ApOjR5IITvJFI2QSC{ZYPp[JVmeyliYYOgd5Vje3S{YYTlJIFnfGW{IEGgbJIh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCrbX31co9ie2G7LDDJR\|UxKD1iND65OEDPxE1w	MkfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEGxPVMoRjJ7OUSxNVk{RC:jPh?=
Function assay	MlTvUWRCNU2ELUKzNS=>	MkTWNE4yKHSxIEGwJJVO	NHnaO3A3KGi{cx?=	MY\Jcohq[mm2aX;uJI9nKFenZUGgbY4hcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCFRFuxJJBpd3OyaH;yfYxifGmxbjDheEBVgXJiMUWgZZQhOC5zIITvJFExKHWPIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R?	M1PMZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO\|YxLz5{OEe5Nlc3ODxxYU6=
Function assay	MY\ISWszQTOW	NYfSXoNvOC5zIITvJFExKHWP	MoPEOkBpenN?	M{XwemlvcGmkaYTpc44hd2ZiV3XlNUBqdiCKRVuyPVNVKGOnbHzzJIF{e2W\|c3XkJIF{KGSnY4LlZZNmKGmwIFPET\|EheGixc4Doc5J6dGG2aX;uJIF1KFS7ckG1JIF1KDBwMTD0c{AyOCC3TTDh[pRmeiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd7Mke2NEc,Ojh5OUK3OlA9N2F-
Function assay	MYrISWszQTOW	M4fqVlAvOSC2bzCxNEB2VQ>?	NHv1bIg3KGi{cx?=	NGe0VFRKdmirYnn0bY9vKG:oIGDMT\|EhcW5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDUR3RRKHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?=	M33ndVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO\|YxLz5{OEe5Nlc3ODxxYU6=
Function assay	NVfVSoJrVUSDLV3CMVI{	MWewMlEhfG9iMUCgeW0>	M4PE[FYhcHK\|	NX7OZ2VnUW6qaXLpeIlwdiCxZjDQUGsyKGmwIHj1cYFvKE2GQT3NRk0zOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDUR3RRKHCqb4PwbI9zgWyjdHnvckBifCByLkGgeI8hOTBidV2gZYZ1\XJiNjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?=	NX\JV4lQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjBpPkK4O\|kzPzZyPD;hQi=>
qHTS assay	MoXiWGM{Og>?			M1\VcZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy\|	MmfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NYS1[JZDXS1{IF;T			MkfJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFVvMjDPV{Bk\Wyucx?=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	NHjHdGJCPjd\|			MnG2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	NFLKc4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	MnTvSGFQYQ>?			NXPzcYFieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO=	MkXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NUHhRoVHW2Gxcz2y			M2fHepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	M{HzfmJVNTN5			NGHjUGFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN\|ch[2WubIO=	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	NWfRUWxDWkR?			NILCdpNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN?	M4\6bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay	MmnFV2suVi2VSB?=			Ml;NdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO=	M2ToNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay	M2LmfWJVNTF{			MkLXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy\|	NEnTTGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	NHryeWlPSjF4NEO=			M{HleJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	NH;0O3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	M1LaTG9JWy13MB?=			NFj3V3lyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	NGS5OIVDXC1zMh?=			NUn0ZXJxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	NXS0ZVZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	MYPERW9[			M3TtWZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGRCV1liY3XscJM>	M2n0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay	M2TMVHNMNU5vU1i=			NIfBeFRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLWPIJINmdGy\|	M3vReVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay	MmHZVog1OQ>?			MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>?	NW\pcpBERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	NHvFPJpCPjd\|			Mn30dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k>	MnnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	NHnHRmFOTyB4MzCoOk1VTyCUKR?=			NHTqfYVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>?	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	MUXVMVIhV1N?			NX\2[YhQeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy\|	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	MYPPTHMuPTB?			MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDPTHMuPTBiY3XscJM>	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	NV[xTnJvWmh2MR?=			MX;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz	NVT1SpdtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	MXPSSC=>			NH;DZoxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTTCClZXzsdy=>	NX;vcZJmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay	MoPlV2ouT0KPMh?=			MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	NHfLe2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	M1e0OnNMNU5vTVO=			MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	MnTPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay	MnLsUmIuTUKlMR?=			NEj1R4lyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=>	NIDieYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	MUPMRW4uPQ>?			NGe5SHVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO=	NGX5eVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
qHTS assay	NVTqZng6WmhzOB?=			M3TTN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy\|	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	MYXTTk1ISk1{			Ml\LdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2ouT0KPMjDj[Yxtew>?	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
qHTS assay	MnTvV4Fwey1{			M{Pa[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>?	M3fld\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

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Assay

Methods	Test Index	PMID
Western blot	p-Cdk1(Y15) / Cdk1; PubMed: 25609063 Clin Cancer Res 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 Clin Cancer Res 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 Cancer Lett 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 Sci Rep 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 Clin Cancer Res 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 Clin Cancer Res 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 Sci Rep 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 Cancer Lett 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 J Hematol Oncol 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

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]

激酶实验： ^[1]	- 合并体外激酶试验: 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]	- 合并 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。 (Only for Reference)
动物实验： ^[1]	- 合并 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 (Only for Reference)

参考文献

[1] Hirai H, et al. Mol Cancer Ther, 2009, 8(11), 2992-3000.

溶解度 (25°C)

体外	DMSO	80 mg/mL (159.8 mM)
	Water	0.0001 mg/mL (0.0 mM)
	Ethanol	''10 mg/mL warmed
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 Download Adavosertib (MK-1775) SDF

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
别名	AZD1775

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

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

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
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.

研究领域

产品类型

定制您的化合物库

Adavosertib (MK-1775)

客户使用Selleck生产的Adavosertib (MK-1775)发表文献163篇：

产品安全说明书

Wee1抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Adavosertib (MK-1775) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

常见问题及建议解决方法

Wee1 Signaling Pathway Map

相关Wee1产品