MK-8776 (SCH 900776)

For research use only. Not for use in humans.

Catalog No.S2735

27 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  
USD 210 In stock
USD 370 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's MK-8776 (SCH 900776) has been cited by 27 publications

Purity & Quality Control

Choose Selective Chk Inhibitors

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 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXKyNFAwOjByMDDuUS=> MWeyOEBp Mnrj[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NV\YSmJpOjR|NUm1NlY>
HCT115 NXfPT3J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojhNlAxNzJyMECgcm0> NISyXlkzPCCq MlWw[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MlfqNlQ{PTl3Mk[=
SW620 NUDPZZhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTJNlAxNzJyMECgcm0> NWPFUYdkOjRiaB?= MWLk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NXXsdlBiOjR|NUm1NlY>
IGROV-1 M2G0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuyNFAwOjByMDDuUS=> NFvifHUzPCCq MYrk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M1u3RlI1OzV7NUK2
HCT116 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLaV5ZCOjByL{KwNFAhdk1? MXqyOEBp Mo\1[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MYKyOFM2QTV{Nh?=
MCF10A MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHKc|YzODBxMkCwNEBvVQ>? M{TSR|I1KGh? M{fRc4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NW\PTmhNOjR|NUm1NlY>
MiaPaCa-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD3NlAxNzJyMECgcm0> M4nDS|I1KGh? M{\hTIRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= M1ywT|I1OzV7NUK2
MDA-MB-231 NH;PSGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\vRmozODBxMkCwNEBvVQ>? NEm4PJozPCCq MVTk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M2XwWlI1OzV7NUK2
HCC2998 NHzLVWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofkNlAxNzJyMECgcm0> MUOyOEBp NYLMOGtW\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MofDNlQ{PTl3Mk[=
U87 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mof1NlAxNzJyMECgcm0> NHjFd3IzPCCq MknC[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NHXlXFMzPDN3OUWyOi=>
MDA-MB-435 Ml\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LH[lIxOC9{MECwJI5O NVLlfGh1OjRiaB?= MkT0[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MXGyOFM2QTV{Nh?=
SNB19 NVm1XWZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jlRVIxOC9{MECwJI5O MoLVNlQhcA>? NWPOdpE6\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MVyyOFM2QTV{Nh?=
U20S NVHBeJE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH24clQzODBxMkCwNEBvVQ>? MUSyOEBp NITMVWZl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NHyxWJYzPDN3OUWyOi=>
A498 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HO[VIxOC9{MECwJI5O Moj5NlQhcA>? MUPk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MojJNlQ{PTl3Mk[=
TK10 NG\HW2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnwfGx{OjByL{KwNFAhdk1? MUCyOEBp M1W5V4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= M2\VU|I1OzV7NUK2
AsPC-1 MmXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHz[YIzODBxMkCwNEBvVQ>? M{XHbVI1KGh? M4nRdYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= MmPlNlQ{PTl3Mk[=
H23 NVT0bVJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnSVZgzPTByIH7N NXfKSoE4OjRiaB?= M{L4PGROW09? MoS0[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg> NIrre5gzPDFzM{W0PS=>
H1437 NYPsdJhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLYPGRxPTByIH7N MUWyOEBp M4K0RWROW09? M4[wU4VvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:gVG1Z Mmn0NlQyOTN3NEm=
H1993 MkHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7jPIQ2ODBibl2= M2DMOFI1KGh? NHzjbG1FVVOR NXX3e4dT\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? NXvvWVV4OjRzMUO1OFk>
H1299 NGHrd45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrHSG1yPTByIH7N M1HaeVI1KGh? NG\TOXBFVVOR M4fjTIVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:gVG1Z MkjtNlQyOTN3NEm=
AsPC-1 NHrS[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rh[|ExNTFyMECgcm0> NYPEboJTOjRvNEjo MYXlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIHflcYNqfGGkaX7l Ml:xNlM5ODR2MkK=
MiaPaCa-2 NU\CXGhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixNE0yODByIH7N M{jkVlI1NTR6aB?= NEnkS|RmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m NEHKc|YzOzhyNESyNi=>
BxPC-3 NU\RZYt5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[xNE0yODByIH7N NWHZelJQOjRvNEjo NFHIRY1mdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m NFrjbJUzOzhyNESyNi=>
SKOV3 MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWwMlMhyrWP MnLWPEBl M1u2TJNmdnOrdHn6[ZMhfGinIHPlcIwhdGmwZYOgeI8h\2WvY3n0ZYJqdmYEoB?= MV:yN|U1QDJ4OR?=
OVCAR-8 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfqcot2OC5|INM1US=> MW[4JIQ> M2H4e5NmdnOrdHn6[ZMhfGinIHPlcIwhdGmwZYOgeI8h\2WvY3n0ZYJqdmYEoB?= MnTkNlM2PDh{Nkm=
MV-4-11 MW\BdI9xfG:|aYOgRZN{[Xl? MUWxNFAuPzByIH7N MlGwOFghcA>? M1rPOIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MlrZNlM2OzZ5MkG=
U937 MWLBdI9xfG:|aYOgRZN{[Xl? NIfMVWIyODBvN{CwJI5O M3WwOVQ5KGh? M2LXdolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NF60[JAzOzV|NkeyNS=>
MOLM-13  MUPBdI9xfG:|aYOgRZN{[Xl? M3nVZlExOC15MECgcm0> MnzQOFghcA>? M2DsR4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MWOyN|U{Pjd{MR?=
A2058  NGP4NXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4XFb|M4NjVvM{CwJI5O M2Hn[lczKGh? MYrEUXNQ NIfWXnRz\WS3Y3XzJJRp\SCPSz2xO|c2KEWFNUFCpIJ6KDVvZn;s[EB1dyCjbjDheoVz[WenIH;mJFQ2KG6P M1\m[|I{OTR6Nki0
H2009 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M136dVUxOCCwTR?= NXHtblh[PzJiaB?= NVT4eoRxTE2VTx?= NUDCdXZxemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? M1jGOFI{OTR6Nki0
Su.86.86 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2S5WVUxOCCwTR?= NFXvTIc4OiCq M3Oxb2ROW09? M4P3W5Jme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO|c2 MnLoNlMyPDh4OES=
HRE MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mnv0OVAxKG6P MnPDO|IhcA>? MUTEUXNQ NUfIV|VFemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? NHPIXJIzOzF2OE[4OC=>
HMEC Mn35R4VtdCCYaXHibYxqfHliQYPzZZk> MoiwOVAxKG6P NXHlcXl5PzJiaB?= MUfEUXNQ MnnvdoV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O|U> MorONlMyPDh4OES=
U2OS  M1nqcGZ2dmO2aX;uJGF{e2G7 M4GycVIhyrWP MW[wMVI1KGh? MUfpcoR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIsyKGG2IIPldolv\SB|NEWgZZQh[m:2aDDjc45k\W62cnH0bY9veyCjczDlZZJtgSCjczCyJIgh[W[2ZYKgZYRucW6rc4TyZZRqd25? MWeyNlk{PzF2Nx?=
U2OS  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:5bWgxNTFyINM1US=> MVqyOE81QCCq M3vUW4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NFPlSY4zOjl|N{G0Oy=>
U937 MlfqSpVv[3Srb36gRZN{[Xl? MUSxNFAuPTByIH7N NXPwU2pNPCCqwrC= M2fIe4Rm[3KnYYPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIFPob|Eh[XW2b4Doc5NxcG:{eXzheIlwdiCjdDDT[ZIzQTcEoHHu[EBxemW4ZX70d{BE\GN{NVGg[I94dnKnZ4XsZZRqd25? NYnhVHFkOjJ6Nkm4Olk>
U937 MUDGeY5kfGmxbjDBd5NigQ>? MkfmNVAxKG6P NFXOS5g1KGkEoB?= MlL0doV3\XK|ZYOgeIhmKGO7dHHyZYJqdmVvaX7keYNm\CCrbnjpZol1cW:wIH;mxsA{UC22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBqdnSxIFTORS=> MkjyNlI5Pjl6Nkm=
U937 NUTl[JBHTnWwY4Tpc44hSXO|YYm= NH7pRZUyODBvNUCwJI5O MUS0JIjDqA>? MVvpcoR2[2W|IHnuZ5Jm[XOnZDDwbI9{eGixconsZZRqd25ib3[gTFJCYA>? MXSyNlg3QTh4OR?=
HL-60 NEO0bItCeG:ydH;zbZMhSXO|YYm= NGLoS3Q{OC9zMECvN|AxKG6P NHfSfFkzPCCq NYDWWlZNTE2VTx?= Mk\a[Y5p[W6lZYOgZ5l1[XKjYnnu[U1qdmS3Y3XkJIFxd3C2b4Ppdy=> NWfsXI4zOjJ6Nkm4Olk>
ML-1 MmLHRZBweHSxc3nzJGF{e2G7 NYHLS4RQOjVxNUCvNVAxKG6P NE\sRZczPCCq MWXEUXNQ NIm3S4JmdmijbnPld{BkgXSjcnHibY5mNWmwZIXj[YQh[XCxcITvd4l{ NH\HPVEzOjh4OUi2PS=>
HCT116 NWHDU3M4TnWwY4Tpc44hSXO|YYm= M2nwWVEhyrWP MUGyOEBp MkTrZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB? MYqyNlUyODV4MB?=
U2OS MYjGeY5kfGmxbjDBd5NigQ>? MUCxJOK2VQ>? NV\sTGROOjRiaB?= MnPGZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB? NUfYWYp5OjJ3MUC1OlA>

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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

  • * Indicates a Required Field

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.

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

Related Chk Products

Tags: buy MK-8776 (SCH 900776) | MK-8776 (SCH 900776) supplier | purchase MK-8776 (SCH 900776) | MK-8776 (SCH 900776) cost | MK-8776 (SCH 900776) manufacturer | order MK-8776 (SCH 900776) | MK-8776 (SCH 900776) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID