MK-8776 (SCH 900776)

For research use only.

Catalog No.S2735

32 publications

MK-8776 (SCH 900776) Chemical Structure

CAS No. 891494-63-6

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) RMB 1921.21 In stock
RMB 1733.35 In stock
RMB 3015.42 In stock
RMB 7966.05 In stock
RMB 20229.30 In stock
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Selleck's MK-8776 (SCH 900776) has been cited by 32 publications

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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 M3TROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[yNFAwOjByMDDuUS=> NHvWdJIzPCCq MlPO[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MVmyOFM2QTV{Nh?=
HCT115 NUHWTZA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2yNFAwOjByMDDuUS=> NVrkSo93OjRiaB?= M1e3XoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= M3zYfFI1OzV7NUK2
SW620 MknuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PNXFIxOC9{MECwJI5O M3rueVI1KGh? NYTocZNG\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MkjsNlQ{PTl3Mk[=
IGROV-1 MnX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjNUFNLOjByL{KwNFAhdk1? M1\IeFI1KGh? M4rTNoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MX:yOFM2QTV{Nh?=
HCT116 NVPCNHJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[yNFAwOjByMDDuUS=> M4Xnc|I1KGh? NXfWUJo2\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l M{DGNlI1OzV7NUK2
MCF10A Moe0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7u[2kzODBxMkCwNEBvVQ>? MlTINlQhcA>? NHr6To5l\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= M2POblI1OzV7NUK2
MiaPaCa-2 NIKxeXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\UVVIxOC9{MECwJI5O NWLBW5YzOjRiaB?= NEHRVmll\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NYDOSFM2OjR|NUm1NlY>
MDA-MB-231 M2TQOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX1NlAxNzJyMECgcm0> M{fuUlI1KGh? MVXk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? Ml3sNlQ{PTl3Mk[=
HCC2998 M{XuT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF23NIQzODBxMkCwNEBvVQ>? NYjrSIhOOjRiaB?= M1nOXIRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MmW0NlQ{PTl3Mk[=
U87 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle3NlAxNzJyMECgcm0> M3rGdlI1KGh? NFXB[oll\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= MoLMNlQ{PTl3Mk[=
MDA-MB-435 NELiS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4L3eFIxOC9{MECwJI5O MlOzNlQhcA>? MUnk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MoH4NlQ{PTl3Mk[=
SNB19 NYPSVI9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorvNlAxNzJyMECgcm0> Mm\6NlQhcA>? NGr1PIZl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= MYiyOFM2QTV{Nh?=
U20S MmC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmyNFAwOjByMDDuUS=> NEL4fIUzPCCq MkLT[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MnHlNlQ{PTl3Mk[=
A498 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnWNlAxNzJyMECgcm0> M1;USlI1KGh? Mk\4[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MniwNlQ{PTl3Mk[=
TK10 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\hWVIxOC9{MECwJI5O Mly2NlQhcA>? Mn7i[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MmnaNlQ{PTl3Mk[=
AsPC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\KdlIxOC9{MECwJI5O M1K4O|I1KGh? MoPv[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NVLDcIFOOjR|NUm1NlY>
H23 Mk\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrvS2Y2ODBibl2= MorINlQhcA>? NG\Ve45FVVOR NUDqfos4\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? MlT0NlQyOTN3NEm=
H1437 NXLYXIhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvuOVAxKG6P MV:yOEBp NXK3So5TTE2VTx?= MWXlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> NEPRcoMzPDFzM{W0PS=>
H1993 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUP2clZPPTByIH7N M2O3NFI1KGh? MmT3SG1UVw>? MkXL[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg> NWHC[5oyOjRzMUO1OFk>
H1299 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFmzS2c2ODBibl2= MoHnNlQhcA>? NGDPXmZFVVOR MYDlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> MVqyOFEyOzV2OR?=
AsPC-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLzVlAyOC1zMECwJI5O MWqyOE01QGh? NX;LRYFE\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{Bo\W2laYThZolv\Q>? NEjtZnIzOzhyNESyNi=>
MiaPaCa-2 Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTHeVlzOTBvMUCwNEBvVQ>? NW\jd4JGOjRvNEjo M4DPS4VvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:g[4Vu[2m2YXLpcoU> MXuyN|gxPDR{Mh?=
BxPC-3 M1HHWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPOPXAzOTBvMUCwNEBvVQ>? M{nac|I1NTR6aB?= NUnYR4JU\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{Bo\W2laYThZolv\Q>? NHPIeYwzOzhyNESyNi=>
SKOV3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XqXVAvOyEEtV2= M13qUVgh\A>? NUTTbYVXe2Wwc3n0bZpmeyC2aHWgZ4VtdCCuaX7ld{B1dyCpZX3jbZRi[mmwZdMg M2rod|I{PTR6Mk[5
OVCAR-8 NVvSSYVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV2wMlMhyrWP NWD4XlFZQCCm NV3VS3Aye2Wwc3n0bZpmeyC2aHWgZ4VtdCCuaX7ld{B1dyCpZX3jbZRi[mmwZdMg M2LORlI{PTR6Mk[5
MV-4-11 NHHwU5lCeG:ydH;zbZMhSXO|YYm= NELCOFYyODBvN{CwJI5O M2niWFQ5KGh? MXvpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MlXYNlM2OzZ5MkG=
U937 MX;BdI9xfG:|aYOgRZN{[Xl? NEi5eZQyODBvN{CwJI5O MX[0PEBp M{[0VIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MV:yN|U{Pjd{MR?=
MOLM-13  NYjjZ5ZvSXCxcITvd4l{KEG|c3H5 MojLNVAxNTdyMDDuUS=> NUnSRm9SPDhiaB?= NEXJc4VqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NGPRemwzOzV|NkeyNS=>
A2058  Mmr1R4VtdCCYaXHibYxqfHliQYPzZZk> MV2zO{42NTNyMDDuUS=> M{\ncVczKGh? MlXESG1UVw>? NIq3TJdz\WS3Y3XzJJRp\SCPSz2xO|c2KEWFNUFCpIJ6KDVvZn;s[EB1dyCjbjDheoVz[WenIH;mJFQ2KG6P MlXrNlMyPDh4OES=
H2009 M3TZ[GNmdGxiVnnhZoltcXS7IFHzd4F6 NF20b5U2ODBibl2= NU\lSIdyPzJiaB?= M{\TfmROW09? NFHJdmdz\XO3bITzJIlvKEdzL2OtdIhie2ViYXPjeY12dGG2aX;uJINwdWKrbnXkJJdqfGhiTVutNVc4PQ>? M1uyV|I{OTR6Nki0
Su.86.86 M4i3TWNmdGxiVnnhZoltcXS7IFHzd4F6 MX61NFAhdk1? MknaO|IhcA>? NFHzW4VFVVOR NXrLW|J1emW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? NE\DfGkzOzF2OE[4OC=>
HRE M4LwO2NmdGxiVnnhZoltcXS7IFHzd4F6 MlvJOVAxKG6P NXfjT|BnPzJiaB?= M{\CSGROW09? M{\6[pJme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO|c2 Mn7LNlMyPDh4OES=
HMEC NHrxZ2FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYjROYh5PTByIH7N NYGyZ2JmPzJiaB?= M3e3RmROW09? MlfndoV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O|U> MUCyN|E1QDZ6NB?=
U2OS  NVf2dIZQTnWwY4Tpc44hSXO|YYm= NI\xRnkzKML3TR?= MVywMVI1KGh? NH;ve4tqdmS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFUh[XRiYn;0bEBkd26lZX70doF1cW:wczDhd{Bm[XKueTDhd{AzKGhiYX\0[ZIh[WSvaX7pd5Rz[XSrb36= NF;5OGczOjl|N{G0Oy=>
U2OS  MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGwMVExKML3TR?= NUO1WZRsOjRxNEigbC=> NW\6dWg2cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MkPkNlI6OzdzNEe=
U937 NHnGU|RHfW6ldHnvckBCe3OjeR?= MlL1NVAxNTVyMDDuUS=> M4nJUlQhcMLi M4rXWIRm[3KnYYPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIFPob|Eh[XW2b4Doc5NxcG:{eXzheIlwdiCjdDDT[ZIzQTcEoHHu[EBxemW4ZX70d{BE\GN{NVGg[I94dnKnZ4XsZZRqd25? NIjPTJYzOjh4OUi2PS=>
U937 NESzeFZHfW6ldHnvckBCe3OjeR?= NEjBelgyODBibl2= M{niTVQhcMLi M2T1Z5JmfmW{c3XzJJRp\SCleYThdoFjcW6nLXnu[JVk\WRiaX7obYJqfGmxbjDv[uKhO0hvdHj5cYllcW6nIHnuZ49zeG:{YYTpc44hcW62bzDEUmE> NEPwd4YzOjh4OUi2PS=>
U937 NXPCVo1NTnWwY4Tpc44hSXO|YYm= NVTXSHcxOTByLUWwNEBvVQ>? NXziXoN6PCCqwrC= NIj2Z4tqdmS3Y3XzJIlv[3KnYYPl[EBxcG:|cHjvdplt[XSrb36gc4YhUDKDWB?= MYiyNlg3QTh4OR?=
HL-60 Mnf2RZBweHSxc3nzJGF{e2G7 Mk[5N|AwOTByL{OwNEBvVQ>? MmfnNlQhcA>? NE\ENHBFVVOR NWjje2po\W6qYX7j[ZMh[3m2YYLhZolv\S2rbnT1Z4VlKGGyb4D0c5Nqew>? NF7aV28zOjh4OUi2PS=>
ML-1 MULBdI9xfG:|aYOgRZN{[Xl? NVXKSnRZOjVxNUCvNVAxKG6P M{\McFI1KGh? MljvSG1UVw>? M1y3WIVvcGGwY3XzJIN6fGG{YXLpcoUucW6mdXPl[EBieG:ydH;zbZM> NWLjeGtGOjJ6Nkm4Olk>
HCT116 NX7SPG5STnWwY4Tpc44hSXO|YYm= NF\N[mYyKML3TR?= MVyyOEBp NXjrboFR[WK{b3fheIV{KG:oIHPlcIwh[3mlbHWgZZJz\XO2wrC= MYGyNlUyODV4MB?=
U2OS NF7KUGRHfW6ldHnvckBCe3OjeR?= M3jkTlEhyrWP M{W3TVI1KGh? MoPYZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB? MmPXNlI2OTB3NkC=

... 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

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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