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.

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Selleck's MK-8776 (SCH 900776) has been cited by 31 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 NFmwNXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDPUHczODBxMkCwNEBvVQ>? MnjoNlQhcA>? M{LafYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NXLPR5M5OjR|NUm1NlY>
HCT115 MkLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDONlAxNzJyMECgcm0> Mn\vNlQhcA>? MYLk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MoLiNlQ{PTl3Mk[=
SW620 MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVeyNFAwOjByMDDuUS=> NHTGN5gzPCCq M1jhTYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MV2yOFM2QTV{Nh?=
IGROV-1 NULEfIw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofhNlAxNzJyMECgcm0> MnOzNlQhcA>? M1rFXoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MYSyOFM2QTV{Nh?=
HCT116 M1z2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXK0eI5{OjByL{KwNFAhdk1? Mn\ONlQhcA>? NIrRc2hl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= MoiyNlQ{PTl3Mk[=
MCF10A M4jqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X1blIxOC9{MECwJI5O MoC3NlQhcA>? MkfD[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NFTOc4QzPDN3OUWyOi=>
MiaPaCa-2 NYrZdFRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fte|IxOC9{MECwJI5O MmXPNlQhcA>? M1;jXoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NUnmUYQzOjR|NUm1NlY>
MDA-MB-231 NGrDUJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;sS|IxOC9{MECwJI5O M1vRTFI1KGh? MnXT[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NUTZV4xLOjR|NUm1NlY>
HCC2998 M2H6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnuZ44zOjByL{KwNFAhdk1? M4LmZ|I1KGh? NYLGb2RN\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l M36zRVI1OzV7NUK2
U87 NIPkXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCyNFAwOjByMDDuUS=> NHqzO5AzPCCq MoPB[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n M1;GfVI1OzV7NUK2
MDA-MB-435 NYXWZpRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHsNlAxNzJyMECgcm0> MlXjNlQhcA>? NFPxR|Vl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NWf6Z4JoOjR|NUm1NlY>
SNB19 NFHTV5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\GSWZFOjByL{KwNFAhdk1? NHLCZ4UzPCCq MWDk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NIjmZoozPDN3OUWyOi=>
U20S MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUeyNFAwOjByMDDuUS=> NYLidWtmOjRiaB?= NXXo[4JT\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MmjrNlQ{PTl3Mk[=
A498 NX;vSpNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPMNlAxNzJyMECgcm0> NGnDWIMzPCCq M{f3NYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MYGyOFM2QTV{Nh?=
TK10 NEfYd4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPaUo8zODBxMkCwNEBvVQ>? NWjkfXc6OjRiaB?= Mli0[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n Ml;KNlQ{PTl3Mk[=
AsPC-1 NVroWHl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXj1XI5tOjByL{KwNFAhdk1? NIPYZVgzPCCq NUPpPZZy\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MWOyOFM2QTV{Nh?=
H23 NUDaeWN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXG1NFAhdk1? MVSyOEBp NXHOS5VXTE2VTx?= MXPlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> MoLoNlQyOTN3NEm=
H1437 MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVe1NFAhdk1? NUDhSnFDOjRiaB?= NXXObG5OTE2VTx?= NYSwZnNb\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? NVO3cIpxOjRzMUO1OFk>
H1993 M1XofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPEelZyPTByIH7N MmTINlQhcA>? NUfpZpF{TE2VTx?= MmTy[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg> M3H1bFI1OTF|NUS5
H1299 M3ztTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfKOVAxKG6P MWOyOEBp NYnXUZFETE2VTx?= NUPNR2NI\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? MXOyOFEyOzV2OR?=
AsPC-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvZNVAuOTByMDDuUS=> M1LaZ|I1NTR6aB?= NWnnfolR\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{Bo\W2laYThZolv\Q>? M{\oUFI{QDB2NEKy
MiaPaCa-2 NYrRe5l4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rVflExNTFyMECgcm0> NVPZ[pNPOjRvNEjo NEftd|hmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m M1XzclI{QDB2NEKy
BxPC-3 NYfDXJhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jXW|ExNTFyMECgcm0> MVWyOE01QGh? MV\lcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIHflcYNqfGGkaX7l MlXENlM5ODR2MkK=
SKOV3 M{\heWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjWNJBwOC5|INM1US=> MWq4JIQ> M1;HUJNmdnOrdHn6[ZMhfGinIHPlcIwhdGmwZYOgeI8h\2WvY3n0ZYJqdmYEoB?= NH3lNYQzOzV2OEK2PS=>
OVCAR-8 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrD[4ZXOC5|INM1US=> NH;Gco05KGR? NFi0ZpB{\W6|aYTpfoV{KHSqZTDj[YxtKGyrbnXzJJRwKGenbXPpeIFjcW6nwrC= MYGyN|U1QDJ4OR?=
MV-4-11 M3LKS2Fxd3C2b4Ppd{BCe3OjeR?= MWGxNFAuPzByIH7N MlzSOFghcA>? M{DaRolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NUm4SGZTOjN3M{[3NlE>
U937 NHzqTFZCeG:ydH;zbZMhSXO|YYm= Ml;TNVAxNTdyMDDuUS=> NXrVZodZPDhiaB?= MnPabY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NF30PIkzOzV|NkeyNS=>
MOLM-13  MVrBdI9xfG:|aYOgRZN{[Xl? MWGxNFAuPzByIH7N M4nvS|Q5KGh? NFOxd2NqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NHT5SY4zOzV|NkeyNS=>
A2058  MmfTR4VtdCCYaXHibYxqfHliQYPzZZk> NEXaTG4{Py53LUOwNEBvVQ>? M1HGb|czKGh? MnixSG1UVw>? NEHjZWNz\WS3Y3XzJJRp\SCPSz2xO|c2KEWFNUFCpIJ6KDVvZn;s[EB1dyCjbjDheoVz[WenIH;mJFQ2KG6P M1\2WlI{OTR6Nki0
H2009 NIDpenJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3HBTVUxOCCwTR?= M{DvflczKGh? M4XFUWROW09? M3fNUZJme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO|c2 NVLsRXE4OjNzNEi2PFQ>
Su.86.86 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUe1NFAhdk1? MlTDO|IhcA>? MYPEUXNQ M{OwOpJme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO|c2 NFrneWgzOzF2OE[4OC=>
HRE NXjae2c4S2WubDDWbYFjcWyrdImgRZN{[Xl? M2rlR|UxOCCwTR?= NEj1ZXk4OiCq NVnOZXROTE2VTx?= MWDy[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> MXOyN|E1QDZ6NB?=
HMEC NXjYOI5ZS2WubDDWbYFjcWyrdImgRZN{[Xl? MmDrOVAxKG6P MlXkO|IhcA>? NI\BRXhFVVOR NFrTXIVz\XO3bITzJIlvKEdzL2OtdIhie2ViYXPjeY12dGG2aX;uJINwdWKrbnXkJJdqfGhiTVutNVc4PQ>? MX6yN|E1QDZ6NB?=
U2OS  MlTkSpVv[3Srb36gRZN{[Xl? MVGyJOK2VQ>? MWOwMVI1KGh? NH[xUYFqdmS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFUh[XRiYn;0bEBkd26lZX70doF1cW:wczDhd{Bm[XKueTDhd{AzKGhiYX\0[ZIh[WSvaX7pd5Rz[XSrb36= NIL3RpczOjl|N{G0Oy=>
U2OS  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXiwMVExKML3TR?= M4jWeVI1NzR6IHi= MmP3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NUWzTmlLOjJ7M{exOFc>
U937 MnPYSpVv[3Srb36gRZN{[Xl? NULLZWRZOTByLUWwNEBvVQ>? M1rUVVQhcMLi MWDk[YNz\WG|ZYOgeIhmKGO7dHHyZYJqdmVvaX7keYNm\CCFaHuxJIF2fG:yaH;zdIhwenmuYYTpc44h[XRiU3XyNlk3yqCjbnSgdJJmfmWwdIOgR4RkOjWDIHTve45z\We3bHH0bY9v Mn[4NlI5Pjl6Nkm=
U937 NYXPfVJnTnWwY4Tpc44hSXO|YYm= NInkd4YyODBibl2= NH\JeG41KGkEoB?= NFTDUlNz\X[ncoPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIHnubIljcXSrb36gc4bDqDOKLYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGmwdH:gSG5C M2LPNFIzQDZ7OE[5
U937 NFGz[GNHfW6ldHnvckBCe3OjeR?= M{DYN|ExOC13MECgcm0> M4nnZlQhcMLi M1j6W4lv\HWlZYOgbY5kemWjc3XkJJBpd3OyaH;yfYxifGmxbjDv[kBJOkG[ MnzTNlI5Pjl6Nkm=
HL-60 M1rqTWFxd3C2b4Ppd{BCe3OjeR?= M4[xPFMxNzFyMD:zNFAhdk1? MV[yOEBp NVPnUY1sTE2VTx?= NUCwXXhp\W6qYX7j[ZMh[3m2YYLhZolv\S2rbnT1Z4VlKGGyb4D0c5Nqew>? NIjYPIMzOjh4OUi2PS=>
ML-1 M{PnXGFxd3C2b4Ppd{BCe3OjeR?= NIXST2szPS93MD:xNFAhdk1? MmjxNlQhcA>? M4H0R2ROW09? M2rLOoVvcGGwY3XzJIN6fGG{YXLpcoUucW6mdXPl[EBieG:ydH;zbZM> MWiyNlg3QTh4OR?=
HCT116 M{PPbWZ2dmO2aX;uJGF{e2G7 NHLKZokyKML3TR?= MYGyOEBp NWD4XY5N[WK{b3fheIV{KG:oIHPlcIwh[3mlbHWgZZJz\XO2wrC= MoPJNlI2OTB3NkC=
U2OS M3LyO2Z2dmO2aX;uJGF{e2G7 M1vTRVEhyrWP NFLYUY0zPCCq MUDhZpJw\2G2ZYOgc4Yh[2WubDDjfYNt\SCjcoLld5TDqA>? NFO4RVIzOjVzMEW2NC=>

... 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 C[N]1C=C(C=N1)C2=C3N=C(C4CCCNC4)C(=C(N)[N]3N=C2)Br

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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