MK-8776 (SCH 900776)

For research use only. Not for use in humans.

目录号：S2735

CAS No. 891494-63-6

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。Phase 2。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1921.21	现货
5mg	RMB 1733.35	现货
10mg	RMB 3015.42	现货
50mg	RMB 7966.05	现货
200mg	RMB 20229.3	现货
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客户使用Selleck生产的MK-8776 (SCH 900776)发表文献41篇：

Nature, 2019, 10.1038/s41586-019-1607-3

PubMed: 31578521 ( click the link to review the publication )

FEBS J, 2021, 10.1111/febs.15747

PubMed: 33529438 ( click the link to review the publication )

DNA Repair (Amst), 2021, 101:103099

PubMed: 33740539 ( click the link to review the publication )

Biochem Pharmacol, 2021, 186:114450

PubMed: 33571504 ( click the link to review the publication )

Sci Rep, 2021, 11(1):10181

PubMed: 33986399 ( click the link to review the publication )

Cell Rep, 2021, 34(4):108680

PubMed: 33503415 ( click the link to review the publication )

Cancer Res, 2020, 80(18):3841-3854

PubMed: 32690724 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(24)E9715

PubMed: 33352723 ( click the link to review the publication )

Sci Rep, 2020, 10(1):18924

PubMed: 33144657 ( click the link to review the publication )

Cell Cycle, 2020, 19(1):84-96

PubMed: 31760882 ( click the link to review the publication )

Diagnostics (Basel), 2020, 10(2)

PubMed: 32098452 ( click the link to review the publication )

Anticancer Res, 2020, 40(3):1315-1323

PubMed: 32132028 ( click the link to review the publication )

Cancer Res, 2020, 80(8):1735-1747

PubMed: 32161100 ( click the link to review the publication )

Leukemia, 2019, 10.1038/s41375-019-0456-2

PubMed: 30967619 ( click the link to review the publication )

Cancer Res, 2019, 79(1):99-113

PubMed: 30361254 ( click the link to review the publication )

Oncogenesis, 2019, 8(7):38

PubMed: 31209198 ( click the link to review the publication )

Mol Cancer Res, 2019, 17(10):1985-1998

PubMed: 31300540 ( click the link to review the publication )

J Virol, 2019, 93(14)

PubMed: 31043526 ( click the link to review the publication )

Chem Res Toxicol, 2019, 32(12):2526-2537

PubMed: 31664825 ( click the link to review the publication )

Nat Commun, 2018, 9(1):764

PubMed: 29472538 ( click the link to review the publication )

Biomaterials, 2018, 182:35-43

PubMed: 30103170 ( click the link to review the publication )

Mol Syst Biol, 2018, 14(8):e8238

PubMed: 30104419 ( click the link to review the publication )

Cancer Res, 2018, 78(11):3054-3066

PubMed: 29735549 ( click the link to review the publication )

Sci Signal, 2018, 11(540)eaat0229

PubMed: 30042127 ( click the link to review the publication )
Mol Cancer Ther, 2018, 17(12):2551-2563

PubMed: 30217967 ( click the link to review the publication )

PLoS One, 2018, 13(4):e0195050

PubMed: 29617433 ( click the link to review the publication )

Neoplasia, 2018, 20(11):1135-1143

PubMed: 30257222 ( click the link to review the publication )

Leuk Res, 2018, 64:17-23

PubMed: 29149649 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(12):3097-3108

PubMed: 27993965 ( click the link to review the publication )

Genes Dev, 2017, 31(3):318-332

PubMed: 28242626 ( click the link to review the publication )

Acta Pharmacol Sin, 2017, 38(4):513-523

PubMed: 28042876 ( click the link to review the publication )

Oncotarget, 2017, 8(7):10966-10979

PubMed: 28030798 ( click the link to review the publication )

Sci Rep, 2017, 7(1):15031

PubMed: 29118324 ( click the link to review the publication )

Oncol Lett, 2017, 14(1):241-249

PubMed: 28693160 ( click the link to review the publication )

JCI Insight, 2017, 2(1):e89760

PubMed: 28097235 ( click the link to review the publication )

Nat Cell Biol, 2016, 18(6):668-75

PubMed: 27136267 ( click the link to review the publication )

Oncotarget, 2016, 7(51):85033-85048

PubMed: 27829224 ( click the link to review the publication )

Cell Death Dis, 2015, 6:e1947

PubMed: 26512957 ( click the link to review the publication )

J Biol Chem, 2015, 290(46):27473-86

PubMed: 26391395 ( click the link to review the publication )

EBioMedicine, 2015, 2(12):1923-31

PubMed: 26844271 ( click the link to review the publication )

Nucleic Acids Res, 2015, 43(20):9776-87

PubMed: 26271993 ( click the link to review the publication )

产品安全说明书

Chk抑制剂选择性比较

生物活性

产品描述

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。Phase 2。

靶点

Chk1 ^[1] (Cell-free assay)	CDK2 ^[1] (Cell-free assay)
3 nM	0.16 μM

体外研究

SCH 900776是Chk2和CDK2的低效抑制剂，IC50分别为1.5 μM 和 0.16 μM。SCH 900776对细胞色素P450人肝微粒体亚型1A2，2C9，2C19，2D6，和3A4没有显著的抑制作用。羟基脲下暴露24小时后，SCH 900776诱导DNA复制能力剂量依赖性损失。SCH 900776增强γ-H2AX对羟基脲，5-氟尿嘧啶，和阿糖孢苷的响应。与抗代谢物结合，SCH 900776在2小时内诱导γ-H2AX的累积，表明复制叉瓦解，并且双链DNA断裂。此外，SCH 900776以剂量依赖的方式抑制Chk1 pS296自磷酸化的积累。增殖的WS1细胞暴露于SCH 900776，与Chk1 pS345快速的，剂量依赖性聚集相关，表明正常细胞的循环群诱导Chk1 pS345在暴露于SCH 900776后，是一部分无效循环，这也许通过AT-家族激酶和DNA-PK驱动。^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
U251	NIfoRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYjJVXJjOjByL{KwNFAhdk1?	NVLQWGpIOjRiaB?=		MVHk[YNz\WG\|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV?	Ml\1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR\|NUm1NlYoRjJ2M{W5OVI3RC:jPh?=
HCT115	NGfPeotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYHCRYliOjByL{KwNFAhdk1?	MnrzNlQhcA>?		NF6yOHdl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW=	NFjDbWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
SW620	NXfsPJBzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Moi3NlAxNzJyMECgcm0>	NF7nXm4zPCCq		Ml7o[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n	NXy5UnJ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVk2OjZpPkK0N\|U6PTJ4PD;hQi=>
IGROV-1	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVuyNFAwOjByMDDuUS=>	M4TNclI1KGh?		NETWZlll\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW=	NIriUVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
HCT116	Mn3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlnyNlAxNzJyMECgcm0>	M17jPVI1KGh?		M4qzT4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=	NWK2[45qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVk2OjZpPkK0N\|U6PTJ4PD;hQi=>
MCF10A	NGfRdXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mne3NlAxNzJyMECgcm0>	NIj4T5ozPCCq		NYDNeFR5\GWlcnXhd4V{KHSqZTDJR\|UxKG:oIFflcYNqfGGkaX7l	M4XvVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
MiaPaCa-2	NEHH[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV6yNFAwOjByMDDuUS=>	M4mzS\|I1KGh?		MUPk[YNz\WG\|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV?	NIPzVYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
MDA-MB-231	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUCxZ2lrOjByL{KwNFAhdk1?	NVHVd4p[OjRiaB?=		NV;hfJo5\GWlcnXhd4V{KHSqZTDJR\|UxKG:oIFflcYNqfGGkaX7l	NUj4fllzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVk2OjZpPkK0N\|U6PTJ4PD;hQi=>
HCC2998	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NInYOGwzODBxMkCwNEBvVQ>?	NH\NcnczPCCq		Ml64[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n	M{TYV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
U87	MlXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUKyNFAwOjByMDDuUS=>	NGq1b\|EzPCCq		MU\k[YNz\WG\|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV?	NHfvenU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
MDA-MB-435	NYHqbGFFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFrWXFkzODBxMkCwNEBvVQ>?	MVKyOEBp		Mofs[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3OUWyOkc,OjR\|NUm1NlY9N2F-
SNB19	M4n5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{PvXlIxOC9{MECwJI5O	MnvTNlQhcA>?		Mljj[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n	M3:4fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
U20S	M3SybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{jmb\|IxOC9{MECwJI5O	NF[w[VgzPCCq		NIfMfJFl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW=	M{XwclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
A498	M3zQNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2DJ[FIxOC9{MECwJI5O	NG\EfWEzPCCq		MVHk[YNz\WG\|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV?	M2XNRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
TK10	NWHWNJRLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYPMZYk5OjByL{KwNFAhdk1?	MYSyOEBp		M1XLc4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=	M2rKblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
AsPC-1	NF32OnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVOyNFAwOjByMDDuUS=>	NVq5dFdbOjRiaB?=		NX;NNHVK\GWlcnXhd4V{KHSqZTDJR\|UxKG:oIFflcYNqfGGkaX7l	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3OUWyOkc,OjR\|NUm1NlY9N2F-
H23	NITDXGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVO1NFAhdk1?	M1vQT\|I1KGh?	M2q4eGROW09?	MYTlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=>	NV3nblE2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVM2PDlpPkK0NVE{PTR7PD;hQi=>
H1437	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYm1NFAhdk1?	NXP0[pB3OjRiaB?=	NVfNclkxTE2VTx?=	NYThd3Zq\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh?	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{W0PUc,OjRzMUO1OFk9N2F-
H1993	NI[5eJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYKxRmRrPTByIH7N	NInoPJczPCCq	MVnEUXNQ	Mkfh[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg>	MmXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMUO1OFkoRjJ2MUGzOVQ6RC:jPh?=
H1299	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWCybFVJPTByIH7N	M{TITVI1KGh?	MljWSG1UVw>?	NIqzdlJmdmijbnPld{B1cGViY3jlcY9{\W6\|aYTpfoF1cW:wIITvJHBOYA>?	NWXhNWZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVM2PDlpPkK0NVE{PTR7PD;hQi=>
AsPC-1	NFfQeGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV6x[Gx7OTBvMUCwNEBvVQ>?	MoriNlQuPDiq		NWnueIo{\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{Bo\W2laYThZolv\Q>?	M1iyO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEC0OFIzLz5{M{iwOFQzOjxxYU6=
MiaPaCa-2	Mmm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mkf0NVAuOTByMDDuUS=>	Mn7QNlQuPDiq		NYLGcGVo\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{Bo\W2laYThZolv\Q>?	M1rvdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEC0OFIzLz5{M{iwOFQzOjxxYU6=
BxPC-3	NHLEOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NH7SRYYyOC1zMECwJI5O	M{PreFI1NTR6aB?=		M3nJPYVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:g[4Vu[2m2YXLpcoU>	MnzLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MES0NlIoRjJ\|OEC0OFIzRC:jPh?=
SKOV3	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MorkNE4{KML3TR?=	NHfK[GE5KGR?		NF;hOmt{\W6\|aYTpfoV{KHSqZTDj[YxtKGyrbnXzJJRwKGenbXPpeIFjcW6nwrC=	NGHWbWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0PFI3QSd-MkO1OFgzPjl:L3G+
OVCAR-8	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnP5NE4{KML3TR?=	MYG4JIQ>		MXzz[Y5{cXSrenXzJJRp\SClZXzsJIxqdmW\|IITvJIdmdWOrdHHibY5myqB?	NYLQeJI2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFgzPjlpPkKzOVQ5OjZ7PD;hQi=>
MV-4-11	M4PLeGFxd3C2b4Ppd{BCe3OjeR?=	Mn25NVAxNTdyMDDuUS=>	MYm0PEBp		MWfpcoR2[2W\|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	NHzEOIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WzOlczOSd-MkO1N\|Y4OjF:L3G+
U937	NWLmZnA{SXCxcITvd4l{KEG\|c3H5	MYqxNFAuPzByIH7N	NFqyOXk1QCCq		NGHvbmNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5	Mof4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3M{[3NlEoRjJ\|NUO2O\|IyRC:jPh?=
MOLM-13	Ml24RZBweHSxc3nzJGF{e2G7	NFPoVpgyODBvN{CwJI5O	MmHGOFghcA>?		NE\MVWJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5	NGW0dnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WzOlczOSd-MkO1N\|Y4OjF:L3G+
A2058	MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NHzsRlk{Py53LUOwNEBvVQ>?	NIn6RW44OiCq	NGDZc3hFVVOR	NEnjSJpz\WS3Y3XzJJRp\SCPSz2xO\|c2KEWFNUFCpIJ6KDVvZn;s[EB1dyCjbjDheoVz[WenIH;mJFQ2KG6P	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF2OE[4OEc,OjNzNEi2PFQ9N2F-
H2009	M4nlRmNmdGxiVnnhZoltcXS7IFHzd4F6	NXLYWlM3PTByIH7N	MVm3NkBp	MUjEUXNQ	NFX1WJpz\XO3bITzJIlvKEdzL2OtdIhie2ViYXPjeY12dGG2aX;uJINwdWKrbnXkJJdqfGhiTVutNVc4PQ>?	M2jxflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|MUS4Olg1Lz5{M{G0PFY5PDxxYU6=
Su.86.86	M17GVWNmdGxiVnnhZoltcXS7IFHzd4F6	NHLoSZc2ODBibl2=	M4\jXVczKGh?	NFLmS\|lFVVOR	MVry[ZN2dHS\|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=>	NF33bYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{G0PFY5PCd-MkOxOFg3QDR:L3G+
HRE	NVXMfVVUS2WubDDWbYFjcWyrdImgRZN{[Xl?	NEnXOGI2ODBibl2=	NVzo[YFTPzJiaB?=	M4XWU2ROW09?	M2HBNpJme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO\|c2	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF2OE[4OEc,OjNzNEi2PFQ9N2F-
HMEC	NInjTXVE\WyuIG\pZYJqdGm2eTDBd5NigQ>?	Mo\mOVAxKG6P	M1;5dFczKGh?	MXjEUXNQ	Mkn2doV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O\|U>	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF2OE[4OEc,OjNzNEi2PFQ9N2F-
U2OS	MoTJSpVv[3Srb36gRZN{[Xl?	NXraOYc2OiEEtV2=	MVmwMVI1KGh?		NWXF[JB7cW6mdXPld{BxcG:\|cHjvdplt[XSrb36gc4YhS2itMTDheEB{\XKrbnWgN\|Q2KGG2IHLveIgh[2:wY3XueJJifGmxboOgZZMh\WG{bImgZZMhOiCqIHHmeIVzKGGmbXnubZN1emG2aX;u	MkjpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{exOFcoRjJ{OUO3NVQ4RC:jPh?=
U2OS	NGLxPXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoraNE0yOCEEtV2=	NXjkdVh1OjRxNEigbC=>		MoKybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:\|ZTDk[ZBmdmSnboTsfS=>	NUG4TmR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N\|cyPDdpPkKyPVM4OTR5PD;hQi=>
U937	M4jkbWZ2dmO2aX;uJGF{e2G7	M3\se\|ExOC13MECgcm0>	NH7SUVM1KGkEoB?=		M4rzeIRm[3KnYYPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIFPob\|Eh[XW2b4Doc5NxcG:{eXzheIlwdiCjdDDT[ZIzQTcEoHHu[EBxemW4ZX70d{BE\GN{NVGg[I94dnKnZ4XsZZRqd25?	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh4OUi2PUc,OjJ6Nkm4Olk9N2F-
U937	M3\Hc2Z2dmO2aX;uJGF{e2G7	M{j0bVExOCCwTR?=	NEn1WVQ1KGkEoB?=		NH:2bIRz\X[ncoPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIHnubIljcXSrb36gc4bDqDOKLYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGmwdH:gSG5C	M2G5WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OE[5PFY6Lz5{Mki2PVg3QTxxYU6=
U937	NUDGXWxSTnWwY4Tpc44hSXO\|YYm=	NFmyXo8yODBvNUCwJI5O	M1vNXFQhcMLi		MX3pcoR2[2W\|IHnuZ5Jm[XOnZDDwbI9{eGixconsZZRqd25ib3[gTFJCYA>?	M1X5XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OE[5PFY6Lz5{Mki2PVg3QTxxYU6=
HL-60	NH[4bIZCeG:ydH;zbZMhSXO\|YYm=	MV:zNE8yODBxM{CwJI5O	NWHKVYFvOjRiaB?=	NGrSeWNFVVOR	MlTh[Y5p[W6lZYOgZ5l1[XKjYnnu[U1qdmS3Y3XkJIFxd3C2b4Ppdy=>	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh4OUi2PUc,OjJ6Nkm4Olk9N2F-
ML-1	NWnwRZdOSXCxcITvd4l{KEG\|c3H5	NWqwO2syOjVxNUCvNVAxKG6P	M1HEd\|I1KGh?	MVTEUXNQ	NF\GTolmdmijbnPld{BkgXSjcnHibY5mNWmwZIXj[YQh[XCxcITvd4l{	NVfsRmN6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4Olk5PjlpPkKyPFY6QDZ7PD;hQi=>
HCT116	NGm2RZpHfW6ldHnvckBCe3OjeR?=	MYGxJOK2VQ>?	NILES20zPCCq		MlLRZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB?	NGj4XWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkWxNFU3OCd-MkK1NVA2PjB:L3G+
U2OS	Mn7hSpVv[3Srb36gRZN{[Xl?	M4XEblEhyrWP	NYT5fWgzOjRiaB?=		MXvhZpJw\2G2ZYOgc4Yh[2WubDDjfYNt\SCjcoLld5TDqA>?	M2j3cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUGwOVYxLz5{MkWxNFU3ODxxYU6=
Sf9	M4TtZWZ2dmO2aX;uJIF{e2G7				NFjEOFlKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JGNFUzJxQ4njcIlvKEFiZYjwdoV{e2WmIHnuJIlve2WldDDT[lkh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDbN\|NRZS2DVGCgbY5kd3Kyb4LheIlwdiCrboTvJIJqd3SrbonsZZRm\CCqaYP0c45mKEhzIHHmeIVzKDFiaIKgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVAhRSByLkG2JO69VS5?	MlLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyOUS2NFcoRjJzMEm0OlA4RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-chk1(ser345) / CDC25A ; PubMed: 27690219 Oncotarget Western blots for H1299 and A549 cells treated with MK-8776 for various times and assessed for expression of p-chk1 (ser345) and CDC25A. Cyclin E / pY15-CDK / γH2AX ; PubMed: 26595527 Oncotarget The indicated cell lines were incubated with 2 μM of each drug for 6 h, then lysed and analyzed by western blotting. The top row reflects cells sensitive to MK-8776. The second row reflects cells that are also sensitive to MK-8776, but which fail to degrade cyclin E. The third row reflects MK-8776-resistant cell lines.	27690219 26595527

体内研究

相对于gemcitabine或SCH 900776单独给药，Gemcitabine给药30分钟后，4 mg/kg SCH 900776足以诱导γ-H2AX生物标志物，而8 mg/kg增强肿瘤药效动力学和退化响应。递增剂量的SCH 900776 (16 mg/kg和32 mg/kg)诱导肿瘤响应持续改进。重要的是，在BALB/c 小鼠体内，SCH 900776的剂量与强的生物标志物活化相关，而提高的肿瘤响应与gemcitabine对血液学指标增强的毒性无关。^[1]

动物实验：^[1]	- 合并 Animal Models: 皮下注射A2780 或 MiaPaCa2细胞的额雌性裸鼠 Dosages: ~50 mg/kg Administration: 腹腔内注射 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	3 mg/mL (7.97 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 4% DMSO+30% propylene glycol	5 mg/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 MK-8776 (SCH 900776) SDF

分子量	376.25
化学式	C₁₅H₁₈BrN₇
CAS号	891494-63-6
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

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、MSDS / 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、MSDS / 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 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00779584	Completed	Drug: MK-8776\|Drug: Gemcitabine	Hodgkin Disease\|Lymphoma Non-Hodgkin\|Neoplasms	Merck Sharp & Dohme Corp.	October 17 2008	Phase 1

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：
I would like to know whether your product S2735 is the optically pure R enantiomer or whether it is a racemic mix.
回答：
Our S2735 MK-8776 (SCH 900776) is R enantiomer.

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

泛CHK抑制剂

AZD7762 : PanCHK inhibitor, Chk1, IC50=5 nM; Chk2, IC50<10 nM.
活性最高的CHK抑制剂

CHIR-124 : Chk1, IC50=0.3 nM.
用于临床的CHK抑制剂

MK-8776 (SCH 900776) : Phase II for Relapsed Acute Myeloid Leukemia.
经典的CHK抑制剂

PF-477736 : Selective, potent and ATP-competitive Chk1 inhibitor with K_i of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes.

研究领域

产品类型

定制您的化合物库

MK-8776 (SCH 900776)

客户使用Selleck生产的MK-8776 (SCH 900776)发表文献41篇：

产品安全说明书

Chk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 MK-8776 (SCH 900776) 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 2021-05-17)

技术支持

常见问题及建议解决方法

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

相关Chk产品