MK-8776 (SCH 900776)

Catalog No.S2735

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.

Price Stock Quantity  
USD 210 In stock
USD 370 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

MK-8776 (SCH 900776) Chemical Structure

MK-8776 (SCH 900776) Chemical Structure
Molecular Weight: 376.25

Validation & Quality Control

1 customer reviews :

Quality Control & MSDS

Related Compound Libraries

MK-8776 (SCH 900776) is available in the following compound libraries:

Chk Inhibitors with Unique Features

  • Pan CHK Inhibitor

    AZD7762 PanCHK inhibitor, Chk1, IC50=5 nM; Chk2, IC50<10 nM.

  • Most Potent CHK Inhibitor

    CHIR-124 Chk1, IC50=0.3 nM.

  • CHK Inhibitor in Clinical Trial

    MK-8776 (SCH 900776) Phase II for Relapsed Acute Myeloid Leukemia.

  • Classic CHK Inhibitor

    PF-477736 Selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes.

Product Information

  • Compare Chk Inhibitors
    Compare Chk Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
U251NVXuToZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWra[G86OjByL{KwNFAhdk1?NULoeWxPOjRiaB?=MVTk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV?M1HsPFI1OzV7NUK2
HCT115NY\TV3F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1HyfVIxOC9{MECwJI5ONXz0[|JEOjRiaB?=M2W0[IRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=MVOyOFM2QTV{Nh?=
SW620MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUfp[Hd4OjByL{KwNFAhdk1?MWSyOEBpNFjrZndl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW=MWGyOFM2QTV{Nh?=
IGROV-1MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NH3XeIYzODBxMkCwNEBvVQ>?MnrqNlQhcA>?MojT[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6nMUSyOFM2QTV{Nh?=
HCT116M2rnSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVuyNFAwOjByMDDuUS=>MXyyOEBpM4DQO4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=MUiyOFM2QTV{Nh?=
MCF10AM13OWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NILScmgzODBxMkCwNEBvVQ>?NWjNNmRtOjRiaB?=NV3RNmZV\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7lM{XYS|I1OzV7NUK2
MiaPaCa-2MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkjMNlAxNzJyMECgcm0>NUPaZ49sOjRiaB?=MojC[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6nNG\5bHUzPDN3OUWyOi=>
MDA-MB-231M3frRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUiyNFAwOjByMDDuUS=>NXvK[XVXOjRiaB?=NHz3T2Zl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW=MX[yOFM2QTV{Nh?=
HCC2998M2\lPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NY\GdZZ3OjByL{KwNFAhdk1?NHfiW2IzPCCqM2DJVIRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=NVjONmhTOjR|NUm1NlY>
U87MkTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mk\WNlAxNzJyMECgcm0>NGrES5MzPCCqMn7G[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6nMojFNlQ{PTl3Mk[=
MDA-MB-435MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1jzdFIxOC9{MECwJI5OM2XSWlI1KGh?NVuw[GJT\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7lNUPXfGtROjR|NUm1NlY>
SNB19MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NX;YPJRSOjByL{KwNFAhdk1?NHzQU|UzPCCqM3zmTIRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=MWeyOFM2QTV{Nh?=
U20SM2D4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4S2eFIxOC9{MECwJI5ONUPnWnlROjRiaB?=Mli1[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6nNYj4d2tHOjR|NUm1NlY>
A498MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MYSyNFAwOjByMDDuUS=>M4PiT|I1KGh?M2TMUYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=NXzVXI9nOjR|NUm1NlY>
TK10MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkTTNlAxNzJyMECgcm0>M17YfFI1KGh?MnjB[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6nMYqyOFM2QTV{Nh?=
AsPC-1Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2nlNFIxOC9{MECwJI5ONUPGfmszOjRiaB?=M{XuT4Rm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?=NGrTVWczPDN3OUWyOi=>
H23MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MYO1NFAhdk1?M3rnRlI1KGh?NETIU|dFVVORMojq[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg>M4Hr[FI1OTF|NUS5
H1437M3zVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NV3KbItPPTByIH7NNXrNN3JGOjRiaB?=M4\sbWROW09?MVzlcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=>NX;jc3ZHOjRzMUO1OFk>
H1993M1jGfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4HtdVUxOCCwTR?=MkHHNlQhcA>?NUfnfXBtTE2VTx?=MoHT[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDQUXg>Mnv2NlQyOTN3NEm=
H1299NIXGNHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mn\UOVAxKG6PNHfVVXczPCCqNH;yTYtFVVORNFrTSHZmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJHBOYA>?MV6yOFEyOzV2OR?=
AsPC-1NWDHfGxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmTJNVAuOTByMDDuUS=>M3rsR|I1NTR6aB?=M3\zWYVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:g[4Vu[2m2YXLpcoU>M1fqNlI{QDB2NEKy
MiaPaCa-2MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkjQNVAuOTByMDDuUS=>NHf0fXozPC12OHi=MmGy[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDn[Y1kcXSjYnnu[S=>MUiyN|gxPDR{Mh?=
BxPC-3NUHzdox1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUf2UHU{OTBvMUCwNEBvVQ>?NEPaZpgzPC12OHi=MYflcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIHflcYNqfGGkaX7lM1HyN|I{QDB2NEKy
SKOV3MknHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIXZVlExNjNiwsXNMWq4JIQ>MVHz[Y5{cXSrenXzJJRp\SClZXzsJIxqdmW|IITvJIdmdWOrdHHibY5myqB?NEnBbFczOzV2OEK2PS=>
OVCAR-8MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3q0S|AvOyEEtV2=NVf0OGM2QCCmNIXoSmd{\W6|aYTpfoV{KHSqZTDj[YxtKGyrbnXzJJRwKGenbXPpeIFjcW6nwrC=M3\TPFI{PTR6Mk[5
MV-4-11M4r2V2Fxd3C2b4Ppd{BCe3OjeR?=M3\0OlExOC15MECgcm0>NVzlWVlVPDhiaB?=M1\PcIlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=MlHFNlM2OzZ5MkG=
U937MnfIRZBweHSxc3nzJGF{e2G7MXmxNFAuPzByIH7NMYW0PEBpMVjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7MlOxNlM2OzZ5MkG=
MOLM-13 M4\Mc2Fxd3C2b4Ppd{BCe3OjeR?=MlO3NVAxNTdyMDDuUS=>MnzCOFghcA>?M1u3RYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=MnXuNlM2OzZ5MkG=
A2058 NFPqZVFE\WyuIG\pZYJqdGm2eTDBd5NigQ>?MYKzO{42NTNyMDDuUS=>NYXuVXV[PzJiaB?=NWLncoxxTE2VTx?=M{TqfpJm\HWlZYOgeIhmKE2NLUG3O|UhTUN3MNMgZpkhPS2ob3zkJJRwKGGwIHH2[ZJi\2Vib3[gOFUhdk1?M1juV|I{OTR6Nki0
H2009MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=>MkCzOVAxKG6PNFHBeJA4OiCqM3rERWROW09?NU\kVnF3emW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV?MVmyN|E1QDZ6NB?=
Su.86.86NHP3dplE\WyuIG\pZYJqdGm2eTDBd5NigQ>?NEjmbIc2ODBibl2=MWe3NkBpMWTEUXNQM4HpepJme3WudIOgbY4hTzFxUz3wbIF{\SCjY3P1cZVt[XSrb36gZ49u[mmwZXSge4l1cCCPSz2xO|c2M3rvRlI{OTR6Nki0
HRENWTEOIVZS2WubDDWbYFjcWyrdImgRZN{[Xl?NWfsSIs{PTByIH7NNUHQNIZ4PzJiaB?=MnH5SG1UVw>?MmPadoV{fWy2czDpckBIOS:VLYDoZZNmKGGlY4XteYxifGmxbjDjc41jcW6nZDD3bZRpKE2NLUG3O|U>M1jYd|I{OTR6Nki0
HMECM1H4dWNmdGxiVnnhZoltcXS7IFHzd4F6NFO0fIU2ODBibl2=MXu3NkBpMoeySG1UVw>?MXfy[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=>M{WxOlI{OTR6Nki0
U2OS MlrQSpVv[3Srb36gRZN{[Xl?NETOXo0zKML3TR?=M3LxU|AuOjRiaB?=NWjBTVhFcW6mdXPld{BxcG:|cHjvdplt[XSrb36gc4YhS2itMTDheEB{\XKrbnWgN|Q2KGG2IHLveIgh[2:wY3XueJJifGmxboOgZZMh\WG{bImgZZMhOiCqIHHmeIVzKGGmbXnubZN1emG2aX;uMWmyNlk{PzF2Nx?=
U2OS MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWSwMVExKML3TR?=NGm0OnAzPC92ODDoMoSybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=>NUPpSI9POjJ7M{exOFc>
U937M2qxWGZ2dmO2aX;uJGF{e2G7NUC3RlZCOTByLUWwNEBvVQ>?MoXJOEBpyqB?MUTk[YNz\WG|ZYOgeIhmKGO7dHHyZYJqdmVvaX7keYNm\CCFaHuxJIF2fG:yaH;zdIhwenmuYYTpc44h[XRiU3XyNlk3yqCjbnSgdJJmfmWwdIOgR4RkOjWDIHTve45z\We3bHH0bY9vNFTL[3czOjh4OUi2PS=>
U937MnHvSpVv[3Srb36gRZN{[Xl?NETNbYUyODBibl2=MV20JIjDqA>?NHfTfW5z\X[ncoPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIHnubIljcXSrb36gc4bDqDOKLYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGmwdH:gSG5CNXPJSmFVOjJ6Nkm4Olk>
U937NEXoWGRHfW6ldHnvckBCe3OjeR?=MnK1NVAxNTVyMDDuUS=>NUTkTlBrPCCqwrC=M33MVolv\HWlZYOgbY5kemWjc3XkJJBpd3OyaH;yfYxifGmxbjDv[kBJOkG[MljhNlI5Pjl6Nkm=
HL-60M4TTSmFxd3C2b4Ppd{BCe3OjeR?=NWGwRm5rOzBxMUCwM|MxOCCwTR?=NWi4NllYOjRiaB?=MoOwSG1UVw>?MX7lcohidmOnczDjfZRiemGkaX7lMYlv\HWlZXSgZZBweHSxc3nzMX2yNlg3QTh4OR?=
ML-1M3HUR2Fxd3C2b4Ppd{BCe3OjeR?=MYKyOU82OC9zMECgcm0>NXjNUINFOjRiaB?=NG\zOZdFVVORNH33bZhmdmijbnPld{BkgXSjcnHibY5mNWmwZIXj[YQh[XCxcITvd4l{MlTNNlI5Pjl6Nkm=
HCT116MVXGeY5kfGmxbjDBd5NigQ>?M{iyV|EhyrWPMWWyOEBpMkfvZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB?MXmyNlUyODV4MB?=
U2OSNVnodFZSTnWwY4Tpc44hSXO|YYm=MkLjNUDDvU1?M2\5b|I1KGh?NIDGT4ti[nKxZ3H0[ZMhd2ZiY3XscEBkgWOuZTDhdpJme3UEoB?=M3\OTlIzPTFyNU[w

... 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Chk1 SPA assay An in vitro assay utilizing recombinant His-Chk1 expressed in the baculovirus expression system as an enzyme source and biotinylated peptide based upon CDC25C as substrate. His-Chk1 is diluted to 32 nM in kinase buffer containing 50 mM Tris pH 8.0, 10 mM MgCl2, and 1 mM DTT. CDC25C (CDC25 Ser216 C-term biotinylated peptide) peptide is diluted to 1.93 μM in kinase buffer. For each kinase reaction, 20 μL of 32 nM Chk1 enzyme solution and 20 μL of 1.926 μM CDC25C are mixed and combined with 10 μL of SCH 900776 diluted in 10% DMSO, making final reaction concentrations of 6.2 nM Chk1, 385 nM CDC25C and 1% DMSO after addition of start solution. The reaction is started by addition of 50 μL of start solution consisting of 2 μM ATP and 0.2 μCi of 33P-ATP, making a final reaction concentration of 1 μM ATP, with 0.2 μCi of 33P-ATP per reaction. Kinase reactions run for 2 hours at room temperature and are stopped by the addition of 100 μL of stop solution consisting of 2 M NaCl, 1% H3PO4, and 5 mg/mL Streptavidin-coated SPA beads. SPA beads are captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads are washed twice with 2 M NaCl and twice with 2 M NaCl with 1% phosphoric acid. Signal is then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves are generated from duplicate 8 point serial dilutions of SCH 900776. IC50 values are derived by nonlinear regression analysis.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Guzi TJ, et al. Mol Cancer Ther, 2011, 10(4), 591-602.

[2] Montano R, et al. Mol Cancer Ther, 2012, 11(2), 427-438.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01870596 Active, not recruiting Adult Acute Megakaryoblastic Leukemia|Adult Acute Monoblastic Leukemia|Adult Acute Monocytic Leukemia|Adult Acute Myeloid Leukemia With Inv(16)(p13  ...more 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, Aggre  ...more 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

Chemical Information

Download MK-8776 (SCH 900776) SDF
Molecular Weight (MW) 376.25
Formula

C15H18BrN7

CAS No. 891494-63-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 3 mg/mL (7.97 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name 6-bromo-3-(1-methyl-1H-pyrazol-4-yl)-5-((R)-piperidin-3-yl)pyrazolo[1,5-a]pyrimidin-7-amine

Customer Product Validation(1)


Click to enlarge
Rating
Source MK-8776 (SCH 900776) purchased from Selleck
Method Western blot
Cell Lines HeLa cells
Concentrations 1-10 uM
Incubation Time 24 h
Results CHK1 phosphorylation increased at 1uM of MK-8776 (SCH900776), possibly due to a negative feedback, or to prevention of phosphatase proximity. At 10uM, CHK1 phosphorylation was inhibited.

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.

Tel: +1-832-582-8158 Ext:3

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

* Indicates a Required Field

Related Chk Products

  • Ro-3306

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • CCG-1423

    CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

  • ML141

    ML141 is a potent, selective and reversible non-competitive inhibitor of Rho family GTPase cdc42 with IC50 of 200 nM.

  • AZD7762

    AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.

  • LY2603618

    LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. Phase 2.

  • CHIR-124

    CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.

  • PF-477736

    PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM in a cell-free assay and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2. Phase 1.

  • Y-27632 2HCl

    Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

    Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).

  • Alisertib (MLN8237)

    Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.

    Features:First orally available inhibitor of Aurora A.

Recently Viewed Items

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
Contact Us