MK-8776 (SCH 900776)

Catalog No.S2735

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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Cited by 26 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 M4HuTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXUNlAxNzJyMECgcm0> MmXINlQhcA>? NHXkbXVl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NF7pVoEzPDN3OUWyOi=>
HCT115 NX:4N|NpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWyNFAwOjByMDDuUS=> MXSyOEBp MYXk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NIS3b5ozPDN3OUWyOi=>
SW620 M2m3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjsc20zODBxMkCwNEBvVQ>? NYPS[ZlCOjRiaB?= NXLPSHR4\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MX2yOFM2QTV{Nh?=
IGROV-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3JRnYzODBxMkCwNEBvVQ>? M2DaUFI1KGh? NWDxXGpM\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NVvhSmRPOjR|NUm1NlY>
HCT116 NUSxWIM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVyyNFAwOjByMDDuUS=> NETkVpMzPCCq Ml7u[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NFLSOWgzPDN3OUWyOi=>
MCF10A NWX6dllJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3uxSFIxOC9{MECwJI5O MofyNlQhcA>? M3Pod4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MVqyOFM2QTV{Nh?=
MiaPaCa-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;QTYYzODBxMkCwNEBvVQ>? MYmyOEBp MXPk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MYCyOFM2QTV{Nh?=
MDA-MB-231 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTQbHgzODBxMkCwNEBvVQ>? M{nRXlI1KGh? Mnnq[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NUPaVY1rOjR|NUm1NlY>
HCC2998 MlfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jBfVIxOC9{MECwJI5O NYfCcoV6OjRiaB?= MkTm[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n M120U|I1OzV7NUK2
U87 NHPRR4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7yNlAxNzJyMECgcm0> NETOfY0zPCCq NXrZdHI4\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NU\KcoF{OjR|NUm1NlY>
MDA-MB-435 M3\aOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle0NlAxNzJyMECgcm0> NXjTR2FSOjRiaB?= MYfk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M3TQelI1OzV7NUK2
SNB19 MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjVNlAxNzJyMECgcm0> NH;qTXQzPCCq NV;0encx\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MXqyOFM2QTV{Nh?=
U20S NXz1OlhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vkblIxOC9{MECwJI5O NXrLclFqOjRiaB?= NYO4WmVP\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MnnsNlQ{PTl3Mk[=
A498 NGH1VmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXYNlAxNzJyMECgcm0> MX:yOEBp M{Gx[IRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NV3Sc|dSOjR|NUm1NlY>
TK10 NE\BdWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLxVWkzODBxMkCwNEBvVQ>? M{GxSVI1KGh? MWnk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NHzGclIzPDN3OUWyOi=>
AsPC-1 M2fqemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\CTlIxOC9{MECwJI5O NEfYbmczPCCq NH\mXodl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= M3fmUlI1OzV7NUK2
H23 NUnMO3JQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rWRVUxOCCwTR?= MoGyNlQhcA>? MnXLSG1UVw>? MYrlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> MXqyOFEyOzV2OR?=
H1437 NHP0fmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj2OVAxKG6P MWeyOEBp MY\EUXNQ NVO0[W5u\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? MknWNlQyOTN3NEm=
H1993 M4TTfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LVWlUxOCCwTR?= M3uzR|I1KGh? M3nBSmROW09? MnPo[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg> NVPHNmZxOjRzMUO1OFk>
H1299 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkm0OVAxKG6P MlvyNlQhcA>? NH3xboNFVVOR M{i0dYVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:gVG1Z NH2z[okzPDFzM{W0PS=>
AsPC-1 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLQNVAuOTByMDDuUS=> M1\4UFI1NTR6aB?= MY\lcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIHflcYNqfGGkaX7l MVWyN|gxPDR{Mh?=
MiaPaCa-2 NVGyb4hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHwNVAuOTByMDDuUS=> NXXofZVqOjRvNEjo NHuwZXRmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m NGG4bnIzOzhyNESyNi=>
BxPC-3 NUDGWWJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL0NVAuOTByMDDuUS=> MnrzNlQuPDiq NIrXc4JmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m NEjWbpAzOzhyNESyNi=>
SKOV3 NEDMNpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HIVVAvOyEEtV2= NX32d5lMQCCm NHjXRll{\W6|aYTpfoV{KHSqZTDj[YxtKGyrbnXzJJRwKGenbXPpeIFjcW6nwrC= MoDaNlM2PDh{Nkm=
OVCAR-8 NX7jOVVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWD4PJRDOC5|INM1US=> NXnjVFh6QCCm NHn0Nll{\W6|aYTpfoV{KHSqZTDj[YxtKGyrbnXzJJRwKGenbXPpeIFjcW6nwrC= NYHDN|FVOjN3NEiyOlk>
MV-4-11 MYTBdI9xfG:|aYOgRZN{[Xl? MW[xNFAuPzByIH7N MXS0PEBp MnPBbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NHi0N5gzOzV|NkeyNS=>
U937 NYfU[ld3SXCxcITvd4l{KEG|c3H5 M1;pVVExOC15MECgcm0> MV:0PEBp NIn5flBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NUHLWVJJOjN3M{[3NlE>
MOLM-13  MlTSRZBweHSxc3nzJGF{e2G7 MUSxNFAuPzByIH7N NYrrZpVxPDhiaB?= MmGybY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NXnpUWFXOjN3M{[3NlE>
A2058  NH\GWWVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWGzO{42NTNyMDDuUS=> M1nhdFczKGh? NFizV4JFVVOR MVTy[YR2[2W|IITo[UBOUy1zN{e1JGVEPTEEoHL5JFUu\m:uZDD0c{BidiCjdnXyZYdmKG:oIES1JI5O MUOyN|E1QDZ6NB?=
H2009 M3\Kc2NmdGxiVnnhZoltcXS7IFHzd4F6 Mn\XOVAxKG6P M4W1WFczKGh? MV7EUXNQ Ml;rdoV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O|U> NV[xbXk{OjNzNEi2PFQ>
Su.86.86 MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1zIb|UxOCCwTR?= MVm3NkBp MWTEUXNQ MUny[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> M2XjUlI{OTR6Nki0
HRE NXXpOI4xS2WubDDWbYFjcWyrdImgRZN{[Xl? MnG0OVAxKG6P MWG3NkBp M3frOmROW09? MnfBdoV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O|U> M1[1elI{OTR6Nki0
HMEC NHLSWY1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MoPFOVAxKG6P M2DtOlczKGh? MV7EUXNQ MVvy[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> NWCwflF{OjNzNEi2PFQ>
U2OS  MWPGeY5kfGmxbjDBd5NigQ>? NWTneGFROiEEtV2= Mlr2NE0zPCCq MWTpcoR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIsyKGG2IIPldolv\SB|NEWgZZQh[m:2aDDjc45k\W62cnH0bY9veyCjczDlZZJtgSCjczCyJIgh[W[2ZYKgZYRucW6rc4TyZZRqd25? M1f4SFIzQTN5MUS3
U2OS  NH\4U5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnNNE0yOCEEtV2= MV:yOE81QCCq MoqxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MWmyNlk{PzF2Nx?=
U937 NGXqTWZHfW6ldHnvckBCe3OjeR?= NGnFboIyODBvNUCwJI5O M3i2ZVQhcMLi NV;1Z2FW\GWlcnXhd4V{KHSqZTDjfZRiemGkaX7lMYlv\HWlZXSgR4hsOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHH0JHNmejJ7NtMgZY5lKHC{ZY\lcpR{KEOmY{K1RUBld3ewcnXneYxifGmxbh?= M2jhVVIzQDZ7OE[5
U937 MXLGeY5kfGmxbjDBd5NigQ>? NWKwV2RLOTByIH7N M13RRVQhcMLi Mni0doV3\XK|ZYOgeIhmKGO7dHHyZYJqdmVvaX7keYNm\CCrbnjpZol1cW:wIH;mxsA{UC22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBqdnSxIFTORS=> MXuyNlg3QTh4OR?=
U937 NI\adYFHfW6ldHnvckBCe3OjeR?= MnO2NVAxNTVyMDDuUS=> MVO0JIjDqA>? M1vBSolv\HWlZYOgbY5kemWjc3XkJJBpd3OyaH;yfYxifGmxbjDv[kBJOkG[ M{HC[VIzQDZ7OE[5
HL-60 MoD1RZBweHSxc3nzJGF{e2G7 MkHMN|AwOTByL{OwNEBvVQ>? NELrWWkzPCCq NHrXcYVFVVOR M1H0eYVvcGGwY3XzJIN6fGG{YXLpcoUucW6mdXPl[EBieG:ydH;zbZM> NWXCZoNLOjJ6Nkm4Olk>
ML-1 MV7BdI9xfG:|aYOgRZN{[Xl? MnP1NlUwPTBxMUCwJI5O NX3MUFVzOjRiaB?= NXvNXm0xTE2VTx?= M{\tdIVvcGGwY3XzJIN6fGG{YXLpcoUucW6mdXPl[EBieG:ydH;zbZM> NGLPe4MzOjh4OUi2PS=>
HCT116 NFzxOHRHfW6ldHnvckBCe3OjeR?= MUGxJOK2VQ>? NHzjXoozPCCq MXvhZpJw\2G2ZYOgc4Yh[2WubDDjfYNt\SCjcoLld5TDqA>? Mo\ONlI2OTB3NkC=
U2OS MljoSpVv[3Srb36gRZN{[Xl? MkexNUDDvU1? MV6yOEBp MVThZpJw\2G2ZYOgc4Yh[2WubDDjfYNt\SCjcoLld5TDqA>? MVOyNlUyODV4MB?=

... 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
  • Formulation: Formulated in 20% hydroxypropyl β-cyclodextrin
  • 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

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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

If you have any other enquiries, please leave a message.

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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