MK-8776 (SCH 900776)

For research use only.

Catalog No.S2735

31 publications

MK-8776 (SCH 900776) Chemical Structure

Molecular Weight(MW): 376.25

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 230 In stock
EUR 206 In stock
EUR 363 In stock
EUR 953 In stock
EUR 2427 In stock
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Selleck's MK-8776 (SCH 900776) has been cited by 31 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 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3kcm5GOjByL{KwNFAhdk1? Mn23NlQhcA>? M{\j[IRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MmPINlQ{PTl3Mk[=
HCT115 NYXHO4JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rNeVIxOC9{MECwJI5O NFnieWgzPCCq Mnrq[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n M2PidlI1OzV7NUK2
SW620 NXn0eWRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfPOpYzODBxMkCwNEBvVQ>? NXy1W2NFOjRiaB?= NF30W49l\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= MXuyOFM2QTV{Nh?=
IGROV-1 NYrxRXZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXpemEzODBxMkCwNEBvVQ>? MVOyOEBp M1z4VYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MVGyOFM2QTV{Nh?=
HCT116 NFH4NGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPJNlAxNzJyMECgcm0> NXjae3lLOjRiaB?= MXjk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NVrIR4JpOjR|NUm1NlY>
MCF10A MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrpbFczODBxMkCwNEBvVQ>? NYfFT|ZsOjRiaB?= MWHk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M{m0blI1OzV7NUK2
MiaPaCa-2 NHm1S|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrnc2p{OjByL{KwNFAhdk1? NWHlWIdpOjRiaB?= NGXSSW9l\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NHjpfVIzPDN3OUWyOi=>
MDA-MB-231 MknCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[3NlAxNzJyMECgcm0> NIW3fHEzPCCq NFrMUVFl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NHjvSGUzPDN3OUWyOi=>
HCC2998 NIrzdmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfrTHJyOjByL{KwNFAhdk1? MYCyOEBp M3nnSIRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NYfJXpVpOjR|NUm1NlY>
U87 NV3nWm5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH24TZEzODBxMkCwNEBvVQ>? M3\YRlI1KGh? MVTk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M4rIeVI1OzV7NUK2
MDA-MB-435 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjjSIQ4OjByL{KwNFAhdk1? MkTmNlQhcA>? NX;VSGlw\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NV;2PVBCOjR|NUm1NlY>
SNB19 NH;MOnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrkbJEzODBxMkCwNEBvVQ>? M1;ZPVI1KGh? NIjKeFNl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NFfNelMzPDN3OUWyOi=>
U20S M4DO[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3CNlAxNzJyMECgcm0> NFLrcFUzPCCq NXv4bFdC\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NXjzfI5vOjR|NUm1NlY>
A498 MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPaVpczODBxMkCwNEBvVQ>? M2W0TFI1KGh? Mmjn[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n M2iydFI1OzV7NUK2
TK10 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jUOVIxOC9{MECwJI5O MmrINlQhcA>? MUHk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NHfqNVQzPDN3OUWyOi=>
AsPC-1 MojpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;tbFIxOC9{MECwJI5O NGTsfokzPCCq MVzk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NVHGSldyOjR|NUm1NlY>
H23 NV;1bpM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m0eFUxOCCwTR?= MnTMNlQhcA>? NYD0dWNZTE2VTx?= NYrV[Y16\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? MWGyOFEyOzV2OR?=
H1437 NFjE[JJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofvOVAxKG6P NYXSfIRUOjRiaB?= Mke5SG1UVw>? M1\iT4VvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:gVG1Z M2jHelI1OTF|NUS5
H1993 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj0OVAxKG6P NFq1e5EzPCCq NUfUbWgyTE2VTx?= MXTlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> MYSyOFEyOzV2OR?=
H1299 NXTRO44xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWK4XnpMPTByIH7N NYjaTYJNOjRiaB?= MXnEUXNQ MnTP[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg> M2jzWVI1OTF|NUS5
AsPC-1 MlLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInQbYQyOC1zMECwJI5O NHPZTG8zPC12OHi= MlPq[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDn[Y1kcXSjYnnu[S=> NELaSlAzOzhyNESyNi=>
MiaPaCa-2 NIPzTZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:xNE0yODByIH7N MYKyOE01QGh? NF3SUopmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m NUHMd44zOjN6MES0NlI>
BxPC-3 M3GzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2WzTFExNTFyMECgcm0> NFjpVYwzPC12OHi= NELkRYhmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m M{LSPFI{QDB2NEKy
SKOV3 M3jHTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[0NVQxNjNiwsXN NITJZ4E5KGR? MXnz[Y5{cXSrenXzJJRp\SClZXzsJIxqdmW|IITvJIdmdWOrdHHibY5myqB? NXLaeFNmOjN3NEiyOlk>
OVCAR-8 M4PZbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[2ZZY1OC5|INM1US=> MWG4JIQ> M2jmZpNmdnOrdHn6[ZMhfGinIHPlcIwhdGmwZYOgeI8h\2WvY3n0ZYJqdmYEoB?= MmfmNlM2PDh{Nkm=
MV-4-11 NWDocHB7SXCxcITvd4l{KEG|c3H5 M1z1clExOC15MECgcm0> NYPWZ3RsPDhiaB?= MWrpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MlzhNlM2OzZ5MkG=
U937 NIrXNZdCeG:ydH;zbZMhSXO|YYm= NITVXGUyODBvN{CwJI5O M4PCS|Q5KGh? MWTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MkS2NlM2OzZ5MkG=
MOLM-13  M{Xjb2Fxd3C2b4Ppd{BCe3OjeR?= MkH5NVAxNTdyMDDuUS=> M4L5[|Q5KGh? NH7WTW9qdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NHq0XIgzOzV|NkeyNS=>
A2058  MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIPvc4k{Py53LUOwNEBvVQ>? NXWwc4s6PzJiaB?= Ml;iSG1UVw>? M4PucJJm\HWlZYOgeIhmKE2NLUG3O|UhTUN3MNMgZpkhPS2ob3zkJJRwKGGwIHH2[ZJi\2Vib3[gOFUhdk1? MmfZNlMyPDh4OES=
H2009 M1T2TGNmdGxiVnnhZoltcXS7IFHzd4F6 NXv1[2piPTByIH7N M3HS[VczKGh? NWWzdYpZTE2VTx?= MWXy[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> M4TFcVI{OTR6Nki0
Su.86.86 MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmfBOVAxKG6P NV7sfGhlPzJiaB?= NWHlN3dVTE2VTx?= M1vUNZJme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO|c2 M{XvZVI{OTR6Nki0
HRE MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NU\M[3NTPTByIH7N NFvMV4c4OiCq NYf4TW1[TE2VTx?= NVvHOItGemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? NGj6enEzOzF2OE[4OC=>
HMEC MnjrR4VtdCCYaXHibYxqfHliQYPzZZk> NIPnS3A2ODBibl2= NIjmOIQ4OiCq M3fITWROW09? NVrIWWc3emW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? M2HFXVI{OTR6Nki0
U2OS  MUfGeY5kfGmxbjDBd5NigQ>? MXmyJOK2VQ>? NFv1eJkxNTJ2IHi= NGL3S4xqdmS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFUh[XRiYn;0bEBkd26lZX70doF1cW:wczDhd{Bm[XKueTDhd{AzKGhiYX\0[ZIh[WSvaX7pd5Rz[XSrb36= NE\DdpYzOjl|N{G0Oy=>
U2OS  NX75W281T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHvNE0yOCEEtV2= MlvqNlQwPDhiaB?= M2DtZolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NEf2WlczOjl|N{G0Oy=>
U937 MofOSpVv[3Srb36gRZN{[Xl? MmXyNVAxNTVyMDDuUS=> MYe0JIjDqA>? MoLX[IVkemWjc3XzJJRp\SCleYThdoFjcW6nLXnu[JVk\WRiQ3jrNUBifXSxcHjvd5Bpd3K7bHH0bY9vKGG2IGPldlI6PsLiYX7kJJBz\X[nboTzJGNl[zJ3QTDkc5dvemWpdXzheIlwdg>? NYHlPY1VOjJ6Nkm4Olk>
U937 NFrqdnNHfW6ldHnvckBCe3OjeR?= MlnLNVAxKG6P MlqyOEBpyqB? MYfy[ZZmenOnczD0bIUh[3m2YYLhZolv\S2rbnT1Z4VlKGmwaHnibZRqd25ib3dCpFNJNXSqeX3p[Ilv\SCrbnPvdpBwemG2aX;uJIlvfG9iRF7B NV3Wb2o3OjJ6Nkm4Olk>
U937 MVnGeY5kfGmxbjDBd5NigQ>? M2DoU|ExOC13MECgcm0> MV20JIjDqA>? M3fpNYlv\HWlZYOgbY5kemWjc3XkJJBpd3OyaH;yfYxifGmxbjDv[kBJOkG[ MWqyNlg3QTh4OR?=
HL-60 NIOzSWxCeG:ydH;zbZMhSXO|YYm= NEPIZYg{OC9zMECvN|AxKG6P NGnuXnIzPCCq M1\VeWROW09? NGDCeJBmdmijbnPld{BkgXSjcnHibY5mNWmwZIXj[YQh[XCxcITvd4l{ Mm[0NlI5Pjl6Nkm=
ML-1 NHX2eoZCeG:ydH;zbZMhSXO|YYm= M{jhV|I2NzVyL{GwNEBvVQ>? NFr5[mgzPCCq NFzXOWJFVVOR M1fXe4VvcGGwY3XzJIN6fGG{YXLpcoUucW6mdXPl[EBieG:ydH;zbZM> NUfZU25pOjJ6Nkm4Olk>
HCT116 Ml22SpVv[3Srb36gRZN{[Xl? NVXOOmhEOSEEtV2= NH\GSmczPCCq NVy3N2l[[WK{b3fheIV{KG:oIHPlcIwh[3mlbHWgZZJz\XO2wrC= NVLFe5JMOjJ3MUC1OlA>
U2OS NETQTVZHfW6ldHnvckBCe3OjeR?= NX[1WHNvOSEEtV2= Moi4NlQhcA>? MXThZpJw\2G2ZYOgc4Yh[2WubDDjfYNt\SCjcoLld5TDqA>? NUSwVZBiOjJ3MUC1OlA>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-chk1(ser345) / CDC25A ; 

PubMed: 27690219     


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     


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
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

Animal Research:[1]
- Collapse
  • Animal Models: Female nude mice injected subcutaneously with A2780 or MiaPaCa2 cells
  • Dosages: ~50 mg/kg
  • Administration: Administered intraperitoneally
    (Only for Reference)

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

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

Chemical Information

Molecular Weight 376.25
Formula

C15H18BrN7

CAS No. 891494-63-6
Storage powder
in solvent
Synonyms N/A
Smiles CN1C=C(C=N1)C2=C3N=C(C(=C(N3N=C2)N)Br)C4CCCNC4

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID