MK-1775

Catalog No.S1525

MK-1775 Chemical Structure

Molecular Weight(MW): 500.6

MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.

Size Price Stock Quantity  
In DMSO USD 238 In stock
USD 170 In stock
USD 270 In stock
USD 470 In stock
USD 770 In stock

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5 Customer Reviews

  • Panobinostat enhances the antitumor activity of MK-1775 in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 μM-thick slides for H&E staining.

    Cancer Letters, 2015, 356(200): 656–668 . MK-1775 purchased from Selleck.

    Diagnostic AML blasts from patients either at first diagnosis or at relapse are equally sensitive to MK-1775. Freshly isolated cells from patient AML#10 were purified by standard Ficoll-Hypaque density centrifugation. AML#10, HL-60, and HL-60/Ara-C cells were treated with MK-1775 for 48 h. Whole cell lysates were subjected to Western blotting and probed with anti-p-CDK1, -CDK1, -p-CDK2, -CDK2, -γH2AX, or -β-actin antibody.

    J Hematol Oncol 2014 7:53. MK-1775 purchased from Selleck.

  • GH activates STAT5 and ERK in breast cancer cells. T47D cells were pretreated for 2 hours with vehicle (dimethylsulfoxide) or inhibitors for EGFR (AG1478, 15 uM) or JAK2 (AZD1480, 1 uM), followed by treatment with GH+E2 for 30 minutes.

    Endocrinology 2013 154(9), 3219-27. MK-1775 purchased from Selleck.

    Histopathological assessment of tumor response to MK-1775 alone and in combination with gemcitabine in a patient-derived osteosarcoma mouse model. A. H&E-stained paraffin sections were prepared to assess microscopic features of cell death and differentiation representative micrographs of B. Ki67 shows high immunoreactivity in the control, MK-1775, and combination treatments compared to gemcitabine treatment. C. Cleaved-caspase 3 images show high immunoreactivity in the MK-1775 and combination treatments compared to vehicle and gemcitabine treatment. D. Slides stained for γH2AX show high immunoreactivity in gemcitabine, MK-1775, and combination treatments compared to controls. E. Slides stained for Cyclin A show higher immunoreactivity in gemcitabine but not in control, MK-1775 alone or in combination treatments.

    PLoS One 2013 8(3), e57523. MK-1775 purchased from Selleck.

  • AZD1480 inhibits the JAK2/STAT3 pathway in vitro. HT29 cells were cultured in 24-well plates overnight and then treated with 1 uM AZD1480 for 2 h followed by 4 ng/ml, IL-6 for 2 h and the distribution of phosphorylated STAT3 was analyzed by immunofluorescence.

    Oncol Rep 2014 32(5), 1991-8. MK-1775 purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.
Features The first reported Wee1 inhibitor.
Targets
Wee1 [1]
(Cell-free assay)
5.2 nM
In vitro

MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14). By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ASPC-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXETWM2OD1zMz6yJOKyKDFwMTFOwG0> M4HGdlI2PDV6OUW0
BxPC-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\qRnJRUUN3ME2wMlghyrFiMD6wN{DPxE1? Ml3wNlU1PTh7NUS=
CFPAC-1 NGTQOXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTNwMzFCtUAxNjJizszN MmjJNlU1PTh7NUS=
HPAC NIXkU4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\3V2lEPTB;MD61JOKyKDBwMEGg{txO NXLYXXdpOjV2NUi5OVQ>
MIAPaCa-2 NFPkcIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfQTWM2OD1yLkWgxtEhOC5yNTFOwG0> NGrDe4QzPTR3OEm1OC=>
PANC-1 M1rZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmG2TWM2OD1zMD62JOKyKDFwMTFOwG0> M{jISlI2PDV6OUW0
SK-N-BE (2) MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTJwNPMAjeKy6oDLMD6zJO69VQ>? NFToRnMzPTNyOEmxOi=>
SK-N-BE (2), PAN→MK MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDTNodKSzVyPUK2MlbjiIoEsfMAjVkvPiEQvF2= M13rN|I2OzB6OUG2
SK-N-BE (2), MK→PAN M13Ed2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrXVIV6UUN3ME2yMlTjiIoEsfMAjVAvOyEQvF2= M2LmdFI2OzB6OUG2
SK-N-AS MmTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYqzOGFHUUN3ME2wMlUx6oDLwsJihKkxNjB{IN88US=> MkiyNlU{ODh7MU[=
SK-N-DZ M3\lbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX6dZdSUUN3ME2wMlM36oDLwsJihKkxNjBzIN88US=> NGC5VmozPTNyOEmxOi=>
SK-N-AS NV\kPGFTSXCxcITvd4l{KEG|c3H5 NYX0OIREPTByIH7N NIDLPXM1QCCq M2TDRYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MUKyOVMxQDlzNh?=
SK-N-DZ M1\WT2Fxd3C2b4Ppd{BCe3OjeR?= MkLOOVAxKG6P MnXqOFghcA>? MlrlbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NHPLS5AzPTNyOEmxOi=>
THP-1 NX;IeIpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzxcJAyOjVxMkWwM|UxOCCwTR?= NHH4Vmg1QCCq NHv5foVqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M3TXfVI2ODh2NkG0
MV4-11 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPCNVI2NzJ3MD:1NFAhdk1? NVWwZmtZPDhiaB?= MUPpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NYHv[45GOjVyOES2NVQ>
U937 NGfhZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljkNVI2NzJ3MD:1NFAhdk1? M3nFRVQ5KGh? M3XYcolv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NH25VlIzPTB6NE[xOC=>
HL-60 M16we2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIm3cowyOjVxMkWwM|UxOCCwTR?= NGHsWGM1QCCq NYHSSFBIcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MV2yOVA5PDZzNB?=
OCI-AML3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3roRlEzPS9{NUCvOVAxKG6P MUO0PEBp NH\iOoVqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NIPBV|YzPTB6NE[xOC=>
MOLM-13 NVnJbZk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojKNVI2NzJ3MD:1NFAhdk1? NE\IN4U1QCCq M2fIbIlv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MlvSNlUxQDR4MUS=
CMK MojxR4VtdCCYaXHibYxqfHliQYPzZZk> NUnqdmpUOTBvMUCwNFAhdk1? NXnkV3F[PzJiaB?= NXHo[mNiemWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?= NWH2eog3OjR7NkKzN|E>
CMY NXHYS3hXS2WubDDWbYFjcWyrdImgRZN{[Xl? M{K3[lExNTFyMECwJI5O NGG0ZZg4OiCq NHjEWoRz\WS3Y3XzJINmdGxidnnhcIljcXS7IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NYPUU21uOjR7NkKzN|E>
Dayo NGjIfZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmzenZKSzVyPUG1NEBvVQ>? NUfpcJFDOjR4NkG5NVA>
UW228 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTJ|MjDuUS=> NIHwS5UzPDZ4MUmxNC=>
IST-MES1 NV3qOVNtS2WubDDWbYFjcWyrdImgRZN{[Xl? NHOybmwyPTBxMkWwJI5O M4Pzc|czKGh? NUPRVoox\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NWLHdotuOjR|NkW3PFI>
IST-MES2 NF36SoNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MoTmNVUxNzJ3MDDuUS=> NGH4OlA4OiCq M4SyUYVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MmTYNlQ{PjV5OEK=
REN NHixWlZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlLONVUxNzJ3MDDuUS=> NWfPOolrPzJiaB?= Ml;z[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NEjoW3gzPDN4NUe4Ni=>
NCI-H2452 NYWweVFKS2WubDDWbYFjcWyrdImgRZN{[Xl? NY\zTol2OTVyL{K1NEBvVQ>? NFTqSnE4OiCq MkPw[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz Mlu3NlQ{PjV5OEK=
MSTO-211H MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUOxOVAwOjVyIH7N NX7lZY96PzJiaB?= NGrLRYtmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MUeyOFM3PTd6Mh?=
NCI-H2052 M{XX[2NmdGxiVnnhZoltcXS7IFHzd4F6 M33yd|E2OC9{NUCgcm0> NVvRdZVOPzJiaB?= NWCy[3ZQ\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ M{Ha[lI1OzZ3N{iy
WEE1 NXTaSotDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmruTWM2OD13LkKgcm0> NXjWS5BJOjN4OUm2OVU>
CDC2 M2eyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PYfmlEPTExvK6xNFAxKG6P M2T2blI{Pjl7NkW1
CDK7 NHy4cYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK3PGlNUUN3MP-8olExODBibl2= MoXqNlM3QTl4NUW=
MYT1 M2jSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTV|MDDuUS=> M1X5OlI{Pjl7NkW1
T98G  MkLFRZBweHSxc3nzJGF{e2G7 NIKx[YIyODBxMkWwJI5O MnnkOkBp NX7JVpVu\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQh[2WubDDrbYxtcW6p MlnrNlE6QTJ5OUO=
A549 MVnBdI9xfG:|aYOgRZN{[Xl? M1LvVVIxOCCwTR?= M{DjW|EhcA>? MXvyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= NH31bXUzOTd7OUCzNy=>
H460 Mme4RZBweHSxc3nzJGF{e2G7 M3y4W|IxOCCwTR?= NHHucocyKGh? NWPKbI1semGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI> NVXXb4FIOjF5OUmwN|M>
H1299 M4OxTGFxd3C2b4Ppd{BCe3OjeR?= NFPxd5AzODBibl2= Mn[2NUBp NH;rcHVz[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=> NGrBPHUzOTd7OUCzNy=>
Calu-6  MWfBdI9xfG:|aYOgRZN{[Xl? MlzHNlAxKG6P NWnLOmxiOSCq MYnyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= NYX5WVRqOjF5OUmwN|M>
WiDr NVrXRo9kU2mwYYPlJGF{e2G7cx?= NUHLS2t2OTBvMUCwNFAhdk1? NXXYU|ZvQCCq NVXF[XBRcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEOGQ{KgZZQhXHm{MUWge4l1cCCjbjDFR|UxyqC4YXz1[UBw\iB6NTDucY9tN0xicILleJJm[XSnZDD3bZRpKGenbXPpeIFjcW6n MnTYNVk5QDd3NEW=

... Click to View More Cell Line Experimental Data

In vivo MK-1775 treatment alone at ~20 mg/kg displays minimal antitumor effects against WiDr xenografts in rats with T/C of 69% at day 3. Antitumor efficacy by MK-1775 alone in the nude rat HeLa-luc and TOV21G-shp53 xenograft models is also moderate. [1]

Protocol

Kinase Assay
+ Expand

In vitro kinase assays:

Recombinant human Wee1 is used. Kinase reaction is conducted with 10 μM ATP, 1.0 μCi of [γ-33P]ATP, and 2.5 μg of poly(Lys, Tyr) as a substrate in the presence of increasing concentrations of MK-1775 at 30°C for 30 minutes. Radioactivity incorporated into the substrate is trapped on MultiScreen-PH plates and is counted on a liquid scintillation counter.
Cell Research
+ Expand
  • Cell lines: WiDr, NCI-H1299, TOV21G, and HeLa
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 hours
  • Method:

    Cells are treated with or without gemcitabine for 24 hours, then with MK-1775 for an additional 24 hours. Cell viability is determined with a WST-8 kit using SpectraMax. Cellular caspase-3/7 activities are determined with a Caspase-3/7 Glo kit.


    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: Immunodeficient nude rats (F344/NJcl-rnu) bearing WiDr, HeLa-luc, or TOV21G-shp53 tumors
  • Formulation: Prepared in a vehicle of 0.5% methylcellulose solution
  • Dosages: ~20 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (159.8 mM)
Ethanol <1 mg/mL
Water 0.0001 mg/mL (0.0 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween+ddH2O 5mg/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 500.6
Formula

C27H32N8O2

CAS No. 955365-80-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02037230 Recruiting Adenocarcinoma of the Pancreas University of Michigan Cancer Center January 2014 Phase 1|Phase 2
NCT01748825 Recruiting Neoplasms|Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) November 2012 Phase 1
NCT01357161 Active, not recruiting Ovarian Cancer Merck Sharp & Dohme Corp. July 2011 Phase 2
NCT01164995 Recruiting Epithelial Ovarian Cancer The Netherlands Cancer Institute|Merck Sharp & Dohme Corp. July 2010 Phase 2
NCT01076400 Terminated Cervical Cancer Merck Sharp & Dohme Corp. May 2010 Phase 1|Phase 2
NCT01047007 Terminated Solid Tumors Merck Sharp & Dohme Corp. January 2010 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.

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Frequently Asked Questions

  • Question 1:

    How to prepare MK1775 methylcellulose solution? and how to prepare methylcellulose itself? Once make the MK1775 methylcellulose solution, how should i keep it?

  • Answer:

    MK1775 in 0.5% methylcellulose is a suspension or emulsion, and it is ok to treat mice orally. It is recommended to dissolve methylcellulose in saline. It will take some time to dissolve methylcellulose, and you can vortex it for a while. The MK1775 methylcellulose solution can be stored at 4°C for a week.

Wee1 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID