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.

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.

2 Customer Reviews

  • MCF7 cells were seeded in 60 mm dishes and were pretreated with the specified inhibitor 1 h before stimulation with either vehicle or doxorubicin. Twenty-four hours after treatment, cells were collected and immunoblotted for nSMase2 and actin.

    Cell Death Dis, 2015, 6:e1947.. MK-8776 (SCH 900776) purchased from Selleck.

    Hela cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, MK-8776 (SCH900776) was added at final concentrations of 0, 5, 10 and 25uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- CHK1, pS345-CHK1 and beta-actin (internal control) antibodies.

    MK-8776 (SCH 900776) purchased from Selleck.

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)
Chk2 [1]
(Cell-free assay)
3 nM 0.16 μM 1.5 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 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG3O3IzODBxMkCwNEBvVQ>? NIj5[nczPCCq NFy3RWxl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= MVOyOFM2QTV{Nh?=
HCT115 NVP6RpN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjKNJgzODBxMkCwNEBvVQ>? MX6yOEBp M16zeoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NHvvOmszPDN3OUWyOi=>
SW620 NWj0blI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13xSlIxOC9{MECwJI5O NWHNVm53OjRiaB?= NUnOSHhF\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MmrNNlQ{PTl3Mk[=
IGROV-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6yNFAwOjByMDDuUS=> NVfmZ|M1OjRiaB?= MUHk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NF3sVoYzPDN3OUWyOi=>
HCT116 NYflbIZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\EOFIxOC9{MECwJI5O MWeyOEBp MXrk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NFrSbIMzPDN3OUWyOi=>
MCF10A NXy3b5lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW2NlAxNzJyMECgcm0> NYHuTphROjRiaB?= Mkmy[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NVLSfo06OjR|NUm1NlY>
MiaPaCa-2 NWnJWWFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVeyNFAwOjByMDDuUS=> MUOyOEBp MWTk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? Ml7GNlQ{PTl3Mk[=
MDA-MB-231 MorVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnZVo5OOjByL{KwNFAhdk1? NITuSpczPCCq Mo\2[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n NI\yXW8zPDN3OUWyOi=>
HCC2998 M2nXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yzRVIxOC9{MECwJI5O MorUNlQhcA>? MWjk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NFrRVVMzPDN3OUWyOi=>
U87 Mnr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HaV|IxOC9{MECwJI5O MW[yOEBp MVPk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MkHLNlQ{PTl3Mk[=
MDA-MB-435 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXlRm0zODBxMkCwNEBvVQ>? NVHib4kyOjRiaB?= MYnk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NHv0cWszPDN3OUWyOi=>
SNB19 M{LyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HZTFIxOC9{MECwJI5O MmnTNlQhcA>? NVrjOGhN\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NUK5e2JDOjR|NUm1NlY>
U20S NYTHZXZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m3bVIxOC9{MECwJI5O NFraNnMzPCCq MlPU[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n M1XBUFI1OzV7NUK2
A498 M3[yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnv2NlAxNzJyMECgcm0> NY\uOZlKOjRiaB?= MWjk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? MmqzNlQ{PTl3Mk[=
TK10 NVzEN|FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT2b3ozODBxMkCwNEBvVQ>? NYPkU4ZCOjRiaB?= NXjWcpZE\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NWnEXJIyOjR|NUm1NlY>
AsPC-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHRNlAxNzJyMECgcm0> MYqyOEBp NGfEbGpl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NVrybFF{OjR|NUm1NlY>
H23 M4jLcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPLZmQ2ODBibl2= M2XKNVI1KGh? MlzoSG1UVw>? NULrTY9s\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? NV3MN3ZkOjRzMUO1OFk>
H1437 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTCS5ZLPTByIH7N NHyycWQzPCCq NULXOndrTE2VTx?= NV3uelNE\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? NV\YNFNGOjRzMUO1OFk>
H1993 MnfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULmUZJWPTByIH7N NEHDOIwzPCCq NIfXd5lFVVOR NInjfpFmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJHBOYA>? NU\GNpQzOjRzMUO1OFk>
H1299 MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi5blc2ODBibl2= MkHRNlQhcA>? NEjvNo1FVVOR MWjlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> NHi4Om4zPDFzM{W0PS=>
AsPC-1 NWXm[28xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexNE0yODByIH7N Mo\GNlQuPDiq M{G0WYVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:g[4Vu[2m2YXLpcoU> MmfwNlM5ODR2MkK=
MiaPaCa-2 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TE[FExNTFyMECgcm0> MY[yOE01QGh? NX;Lcolp\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{Bo\W2laYThZolv\Q>? MXuyN|gxPDR{Mh?=
BxPC-3 MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPES3IyOC1zMECwJI5O M{PQWVI1NTR6aB?= MmXW[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDn[Y1kcXSjYnnu[S=> MnfWNlM5ODR2MkK=
SKOV3 MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPrN5k2OC5|INM1US=> MX64JIQ> Mleyd4Vve2m2aYrld{B1cGViY3XscEBtcW6nczD0c{Bo\W2laYThZolv\cLi Mmn3NlM2PDh{Nkm=
OVCAR-8 NEGzdYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXVUYIxNjNiwsXN MmjIPEBl MoDzd4Vve2m2aYrld{B1cGViY3XscEBtcW6nczD0c{Bo\W2laYThZolv\cLi MY[yN|U1QDJ4OR?=
MV-4-11 NYTi[otuSXCxcITvd4l{KEG|c3H5 NUjEVHEzOTByLUewNEBvVQ>? NHHjU5k1QCCq NInBblVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 Ml3lNlM2OzZ5MkG=
U937 NGnzcG9CeG:ydH;zbZMhSXO|YYm= NX3DfHFMOTByLUewNEBvVQ>? NWPkdVdwPDhiaB?= NV\FU4NDcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M{TFVVI{PTN4N{Kx
MOLM-13  MV;BdI9xfG:|aYOgRZN{[Xl? M3f0XlExOC15MECgcm0> MUK0PEBp MYHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NFjhN3kzOzV|NkeyNS=>
A2058  MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUL0c242OzdwNT2zNFAhdk1? M4e2W|czKGh? NYWwcFhJTE2VTx?= M1jkVpJm\HWlZYOgeIhmKE2NLUG3O|UhTUN3MNMgZpkhPS2ob3zkJJRwKGGwIHH2[ZJi\2Vib3[gOFUhdk1? NYHrOop6OjNzNEi2PFQ>
H2009 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlL6OVAxKG6P NWfWOHFmPzJiaB?= NFf1enpFVVOR NUWyeIljemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? M3PvSlI{OTR6Nki0
Su.86.86 MlLKR4VtdCCYaXHibYxqfHliQYPzZZk> M4X0VVUxOCCwTR?= NVjzV|hmPzJiaB?= MVrEUXNQ NW[0ZYVvemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? MkC2NlMyPDh4OES=
HRE NW\oZW1lS2WubDDWbYFjcWyrdImgRZN{[Xl? MV61NFAhdk1? NI[0d|A4OiCq MYDEUXNQ MV7y[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> NXvSfphYOjNzNEi2PFQ>
HMEC NWi3T4c3S2WubDDWbYFjcWyrdImgRZN{[Xl? NWHwWJFrPTByIH7N NVjacGV1PzJiaB?= M1HKbWROW09? NHPHN|Zz\XO3bITzJIlvKEdzL2OtdIhie2ViYXPjeY12dGG2aX;uJINwdWKrbnXkJJdqfGhiTVutNVc4PQ>? NVzY[HBZOjNzNEi2PFQ>
U2OS  NGrHXJFHfW6ldHnvckBCe3OjeR?= NH21e2MzKML3TR?= MWewMVI1KGh? M1zXT4lv\HWlZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGNpczFiYYSgd4VzcW6nIEO0OUBifCCkb4ToJINwdmOnboTyZZRqd26|IHHzJIViemy7IHHzJFIhcCCjZoTldkBi\G2rbnnzeJJifGmxbh?= MVOyNlk{PzF2Nx?=
U2OS  MmjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDl[WsxNTFyINM1US=> NHPrb3EzPC92ODDo MlLxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MmHVNlI6OzdzNEe=
U937 M{fvdWZ2dmO2aX;uJGF{e2G7 M2LaVFExOC13MECgcm0> M2nmRlQhcMLi M1fYNIRm[3KnYYPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIFPob|Eh[XW2b4Doc5NxcG:{eXzheIlwdiCjdDDT[ZIzQTcEoHHu[EBxemW4ZX70d{BE\GN{NVGg[I94dnKnZ4XsZZRqd25? NXrsOYxHOjJ6Nkm4Olk>
U937 MorwSpVv[3Srb36gRZN{[Xl? M2jxW|ExOCCwTR?= NIS1RXk1KGkEoB?= MWny[ZZmenOnczD0bIUh[3m2YYLhZolv\S2rbnT1Z4VlKGmwaHnibZRqd25ib3dCpFNJNXSqeX3p[Ilv\SCrbnPvdpBwemG2aX;uJIlvfG9iRF7B M37HZlIzQDZ7OE[5
U937 NV\TS4p7TnWwY4Tpc44hSXO|YYm= MVyxNFAuPTByIH7N MmTmOEBpyqB? NUm5RWtmcW6mdXPld{BqdmO{ZXHz[YQheGixc4Doc5J6dGG2aX;uJI9nKEh{QWi= M1viPFIzQDZ7OE[5
HL-60 NX\JfVgySXCxcITvd4l{KEG|c3H5 M4LPSVMxNzFyMD:zNFAhdk1? M{T6XFI1KGh? NFPN[HNFVVOR MX3lcohidmOnczDjfZRiemGkaX7lMYlv\HWlZXSgZZBweHSxc3nz MoDhNlI5Pjl6Nkm=
ML-1 M4P2SGFxd3C2b4Ppd{BCe3OjeR?= MnGxNlUwPTBxMUCwJI5O MnjQNlQhcA>? M3rJ[GROW09? MnG1[Y5p[W6lZYOgZ5l1[XKjYnnu[U1qdmS3Y3XkJIFxd3C2b4Ppdy=> NYPKVGZlOjJ6Nkm4Olk>
HCT116 NI\hOZhHfW6ldHnvckBCe3OjeR?= MmTTNUDDvU1? MkfVNlQhcA>? NUfDTWti[WK{b3fheIV{KG:oIHPlcIwh[3mlbHWgZZJz\XO2wrC= M1jtZ|IzPTFyNU[w
U2OS NHX3VZZHfW6ldHnvckBCe3OjeR?= NVvYcHdmOSEEtV2= MoXCNlQhcA>? MWjhZpJw\2G2ZYOgc4Yh[2WubDDjfYNt\SCjcoLld5TDqA>? MVGyNlUyODV4MB?=

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% propylene glycol 5 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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 (g) = Concentration (mol/L) × Volume (L) × 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

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01870596 Completed Adult Acute Megakaryoblastic Leukemia|Adult Acute Monoblastic Leukemia|Adult Acute Monocytic Leukemia|Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With Maturation|Adult Acute Myeloid Leukemia With Minimal Differentiation|Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22); RUNX1-RUNX1T1|Adult Acute Myeloid Leukemia With t(9;11)(p22;q23); MLLT3-MLL|Adult Acute Myeloid Leukemia Without Maturation|Adult Acute Myelomonocytic Leukemia|Adult Erythroleukemia|Adult Pure Erythroid Leukemia|Alkylating Agent-Related Acute Myeloid Leukemia|Recurrent Adult Acute Myeloid Leukemia National Cancer Institute (NCI) May 2013 Phase 2
NCT00907517 Terminated Myelogenous Leukemia, Acute|Leukemia, Lymphocytic, Acute|Leukemia, Lymphoblastic, Acute, Philadelphia-Positive|Myelogenous Leukemia, Chronic, Aggressive Phase Merck Sharp & Dohme Corp. July 2009 Phase 1
NCT00779584 Completed Hodgkin Disease|Lymphoma, Non-Hodgkin|Neoplasms Merck Sharp & Dohme Corp. October 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

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

  • * Indicates a Required Field

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