MK-8776 (SCH 900776)

Catalog No.S2735

For research use only.

MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.

MK-8776 (SCH 900776) Chemical Structure

CAS No. 891494-63-6

Selleck's MK-8776 (SCH 900776) has been cited by 53 publications

Purity & Quality Control

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Biological Activity

Description MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
Targets
Chk1 [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
3 nM 0.16 μM
In vitro

SCH 900776 is a less potent inhibitor of Chk2 and CDK2 with IC50 of 1.5 μM and 0.16 μM, respectively. SCH 900776 shows no significant inhibition of cytochrome P450 human liver microsomal isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. SCH 900776 induces a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. SCH 900776 enhances the γ-H2AX response of hydroxyurea, 5-fluoruracil, and cytarabine. In combination with an antimetabolite, SCH 900776 induces accumulation of γ-H2AX within 2 hours, indicative of replication fork collapse and double stranded DNA breaks. Additionally, SCH 900776 suppresses accumulation of the Chk1 pS296 autophosphorylation in a dose-dependent manner. Exposure of proliferating WS1 cells to SCH 900776 is associated with rapid, dose-dependent accumulation of Chk1 pS345, indicating that cycling populations of normal cells induce Chk1 pS345 following exposure to SCH 900776 as part of a futile cycle, perhaps driven by AT-family kinases and DNA-PK.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U251 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWyNFAwOjByMDDuUS=> M2fwOVI1KGh? NEfye3hl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NUTy[XdbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVk2OjZpPkK0N|U6PTJ4PD;hQi=>
HCT115 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDrNJozODBxMkCwNEBvVQ>? NITXT2kzPCCq M32xfYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3OUWyOkc,OjR|NUm1NlY9N2F-
SW620 NYG2dVRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvoNlAxNzJyMECgcm0> M3fyR|I1KGh? MmHq[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n Ml[yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NUm1NlYoRjJ2M{W5OVI3RC:jPh?=
IGROV-1 M4fBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXBd5Z1OjByL{KwNFAhdk1? M4jhfFI1KGh? M1;sZYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3OUWyOkc,OjR|NUm1NlY9N2F-
HCT116 M3OzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuyNFAwOjByMDDuUS=> M4q1bFI1KGh? NYnJSohx\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NYPWOVg6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVk2OjZpPkK0N|U6PTJ4PD;hQi=>
MCF10A M3PXWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Dkc|IxOC9{MECwJI5O M2O0TFI1KGh? Mn3l[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n Moj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NUm1NlYoRjJ2M{W5OVI3RC:jPh?=
MiaPaCa-2 M4nEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLzT5NrOjByL{KwNFAhdk1? NGKxUlgzPCCq Mnrx[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MmfUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NUm1NlYoRjJ2M{W5OVI3RC:jPh?=
MDA-MB-231 M{T3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\ONlAxNzJyMECgcm0> NX;zTmhGOjRiaB?= NUPUUnZC\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NYOwfHJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVk2OjZpPkK0N|U6PTJ4PD;hQi=>
HCC2998 NWD1O483T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPheFRvOjByL{KwNFAhdk1? NYjsZVljOjRiaB?= Mm\S[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3OUWyOkc,OjR|NUm1NlY9N2F-
U87 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT1bYJQOjByL{KwNFAhdk1? Ml7lNlQhcA>? NGLlW21l\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NFPoT4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
MDA-MB-435 NEfsZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuyNFAwOjByMDDuUS=> NImxVVgzPCCq MW\k[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NES3eWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
SNB19 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGyNFAwOjByMDDuUS=> NVHTWmc2OjRiaB?= MUPk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NHGzXIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
U20S M32xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1flVFIxOC9{MECwJI5O NVjsWXhpOjRiaB?= MX;k[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MoX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NUm1NlYoRjJ2M{W5OVI3RC:jPh?=
A498 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHro[HAzODBxMkCwNEBvVQ>? NYPtfYNWOjRiaB?= NHT3Vnhl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= M3\yNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
TK10 NGGwVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHINlAxNzJyMECgcm0> M1jiOVI1KGh? M1P5eoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= M4W3TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W5OVI3Lz5{NEO1PVUzPjxxYU6=
AsPC-1 M{HO[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TpbVIxOC9{MECwJI5O MkPpNlQhcA>? Mn;p[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NFPZOm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1PVUzPid-MkSzOVk2OjZ:L3G+
H23 M17yc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[wRYVnPTByIH7N NXLT[GtFOjRiaB?= MojlSG1UVw>? MXPlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> NYT3cWdrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVM2PDlpPkK0NVE{PTR7PD;hQi=>
H1437 NXrEOYMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO1NFAhdk1? MYmyOEBp M2i0T2ROW09? NGDne5BmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJHBOYA>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFzM{W0PUc,OjRzMUO1OFk9N2F-
H1993 MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWe1NFAhdk1? NG\mXWEzPCCq MV;EUXNQ Ml;K[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg> M3zHRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUGzOVQ6Lz5{NEGxN|U1QTxxYU6=
H1299 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTKSGZIPTByIH7N MYWyOEBp NXfKb5ZMTE2VTx?= NVK5d413\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? NXzn[oE2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVM2PDlpPkK0NVE{PTR7PD;hQi=>
AsPC-1 NWr6TpVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGxNE0yODByIH7N Ml;ZNlQuPDiq NEXIOGxmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m M33HclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEC0OFIzLz5{M{iwOFQzOjxxYU6=
MiaPaCa-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHoRmdDOTBvMUCwNEBvVQ>? NEW4RoYzPC12OHi= M4PDUYVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:g[4Vu[2m2YXLpcoU> M1jLVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEC0OFIzLz5{M{iwOFQzOjxxYU6=
BxPC-3 NH3zPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfxNVAuOTByMDDuUS=> NXPzWFhROjRvNEjo NInBfnZmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m NHHtOHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iwOFQzOid-MkO4NFQ1OjJ:L3G+
SKOV3 M1HPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzwUmgxNjNiwsXN NU[3bpp3QCCm MYfz[Y5{cXSrenXzJJRp\SClZXzsJIxqdmW|IITvJIdmdWOrdHHibY5myqB? NXyz[Yd7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFgzPjlpPkKzOVQ5OjZ7PD;hQi=>
OVCAR-8 NF7qS41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmwMlMhyrWP MnXLPEBl NEjoV5d{\W6|aYTpfoV{KHSqZTDj[YxtKGyrbnXzJJRwKGenbXPpeIFjcW6nwrC= NH7DPGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0PFI3QSd-MkO1OFgzPjl:L3G+
MV-4-11 NH7XcZRCeG:ydH;zbZMhSXO|YYm= NYn0[49lOTByLUewNEBvVQ>? M4\melQ5KGh? NIDidZVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV|NkeyNUc,OjN3M{[3NlE9N2F-
U937 NYfkSY5uSXCxcITvd4l{KEG|c3H5 M13HSFExOC15MECgcm0> MlnXOFghcA>? M2DaXolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NGnqR4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WzOlczOSd-MkO1N|Y4OjF:L3G+
MOLM-13  NH;TUnRCeG:ydH;zbZMhSXO|YYm= MWSxNFAuPzByIH7N MVq0PEBp NYXnSldTcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M2HJWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUO2O|IyLz5{M{WzOlczOTxxYU6=
A2058  NVfab4VVS2WubDDWbYFjcWyrdImgRZN{[Xl? NUXkenM1OzdwNT2zNFAhdk1? MY[3NkBp MV\EUXNQ MVjy[YR2[2W|IITo[UBOUy1zN{e1JGVEPTEEoHL5JFUu\m:uZDD0c{BidiCjdnXyZYdmKG:oIES1JI5O M3TJdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MUS4Olg1Lz5{M{G0PFY5PDxxYU6=
H2009 Ml3TR4VtdCCYaXHibYxqfHliQYPzZZk> NGfYWFA2ODBibl2= M3zjblczKGh? NVXmcnlzTE2VTx?= MW\y[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> NU\5cW5kRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxOFg3QDRpPkKzNVQ5Pjh2PD;hQi=>
Su.86.86 M3XhSmNmdGxiVnnhZoltcXS7IFHzd4F6 MXu1NFAhdk1? Ml75O|IhcA>? NWHHPFZ7TE2VTx?= MkL1doV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O|U> M{jCdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MUS4Olg1Lz5{M{G0PFY5PDxxYU6=
HRE MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{n5eVUxOCCwTR?= MYK3NkBp MnvJSG1UVw>? MX;y[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF2OE[4OEc,OjNzNEi2PFQ9N2F-
HMEC M4mxemNmdGxiVnnhZoltcXS7IFHzd4F6 MU[1NFAhdk1? MUC3NkBp MnXYSG1UVw>? MV\y[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> MlLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNEi2PFQoRjJ|MUS4Olg1RC:jPh?=
U2OS  NHeyUHZHfW6ldHnvckBCe3OjeR?= MmjYNkDDvU1? NWjqWJdZOC1{NDDo NGThUVVqdmS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFUh[XRiYn;0bEBkd26lZX70doF1cW:wczDhd{Bm[XKueTDhd{AzKGhiYX\0[ZIh[WSvaX7pd5Rz[XSrb36= M3nXfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO3NVQ4Lz5{MkmzO|E1PzxxYU6=
U2OS  NHX3OY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljuNE0yOCEEtV2= NW\BV4M3OjRxNEigbC=> MVPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWLkNpVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|cyPDdpPkKyPVM4OTR5PD;hQi=>
U937 MmXkSpVv[3Srb36gRZN{[Xl? M2DsTFExOC13MECgcm0> M3O4[|QhcMLi MYjk[YNz\WG|ZYOgeIhmKGO7dHHyZYJqdmVvaX7keYNm\CCFaHuxJIF2fG:yaH;zdIhwenmuYYTpc44h[XRiU3XyNlk3yqCjbnSgdJJmfmWwdIOgR4RkOjWDIHTve45z\We3bHH0bY9v NHrNc5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki2PVg3QSd-MkK4Olk5Pjl:L3G+
U937 MU\GeY5kfGmxbjDBd5NigQ>? NFzMVFcyODBibl2= MUS0JIjDqA>? NU\z[XltemW4ZYLz[ZMhfGinIHP5eIFz[WKrbnWtbY5lfWOnZDDpcohq[mm2aX;uJI9nyqB|SD30bJlucWSrbnWgbY5kd3Kyb4LheIlwdiCrboTvJGRPSQ>? NHjSSJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki2PVg3QSd-MkK4Olk5Pjl:L3G+
U937 NUDMNFE6TnWwY4Tpc44hSXO|YYm= Mn\mNVAxNTVyMDDuUS=> NV\zVGV4PCCqwrC= NFK4UHhqdmS3Y3XzJIlv[3KnYYPl[EBxcG:|cHjvdplt[XSrb36gc4YhUDKDWB?= MkThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6Nkm4OlkoRjJ{OE[5PFY6RC:jPh?=
HL-60 MnLtRZBweHSxc3nzJGF{e2G7 NHO2boE{OC9zMECvN|AxKG6P NIrjWXQzPCCq NGLO[JpFVVOR NXzBW5hS\W6qYX7j[ZMh[3m2YYLhZolv\S2rbnT1Z4VlKGGyb4D0c5Nqew>? NEHzbYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki2PVg3QSd-MkK4Olk5Pjl:L3G+
ML-1 MWTBdI9xfG:|aYOgRZN{[Xl? NH:xdWUzPS93MD:xNFAhdk1? Moj6NlQhcA>? MUXEUXNQ NW\mPXpL\W6qYX7j[ZMh[3m2YYLhZolv\S2rbnT1Z4VlKGGyb4D0c5Nqew>? NUTmfZhsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4Olk5PjlpPkKyPFY6QDZ7PD;hQi=>
HCT116 NIX4XYtHfW6ldHnvckBCe3OjeR?= NWDNfnhzOSEEtV2= M3G0cVI1KGh? NHvC[pli[nKxZ3H0[ZMhd2ZiY3XscEBkgWOuZTDhdpJme3UEoB?= MlLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3MUC1OlAoRjJ{NUGwOVYxRC:jPh?=
U2OS M4\MTGZ2dmO2aX;uJGF{e2G7 MoqyNUDDvU1? NIn1UG4zPCCq MknUZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB? NIjPTpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkWxNFU3OCd-MkK1NVA2PjB:L3G+
Sf9 M{TtOGZ2dmO2aX;uJIF{e2G7 M1fvZmlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgR2RMOi:FeXPsbY4hSSCneIDy[ZN{\WRiaX6gbY5{\WO2IGPmPUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuzN3BeNUGWUDDpcoNwenCxcnH0bY9vKGmwdH:gZolwfGmweXzheIVlKGirc4TvcoUhUDFiYX\0[ZIhOSCqcjDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMU[g{txONg>? NXX1bHFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwPVQ3ODdpPkKxNFk1PjB5PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-chk1(ser345) / CDC25A ; Cyclin E / pY15-CDK / γH2AX 27690219 26595527
In vivo Administered 30 minutes after gemcitabine, 4 mg/kg SCH 900776 is sufficient to induce the γ-H2AX biomarker while 8 mg/kg leads to enhanced tumor pharmacodynamic and regression responses relative to gemcitabine or SCH 900776 alone. Dose escalation of SCH 900776 (16 mg/kg and 32 mg/kg) induces incremental improvements in tumor response. Importantly, doses of SCH 900776 associate with robust biomarker activation and improved tumor response are not associated with enhanced toxicity of gemcitabine on hematological parameters in BALB/c mice. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Female nude mice injected subcutaneously with A2780 or MiaPaCa2 cells
  • Dosages: ~50 mg/kg
  • Administration: Administered intraperitoneally

Solubility (25°C)

In vitro

DMSO 3 mg/mL
(7.97 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% propylene glycol
For best results, use promptly after mixing.

5 mg/mL

Chemical Information

Molecular Weight 376.25
Formula

C15H18BrN7

CAS No. 891494-63-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C=N1)C2=C3N=C(C(=C(N3N=C2)N)Br)C4CCCNC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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Frequently Asked Questions

Question 1:
I would like to know whether your product S2735 is the optically pure R enantiomer or whether it is a racemic mix.

Answer:
Our S2735 MK-8776 (SCH 900776) is R enantiomer.

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