Adavosertib (MK-1775)

Catalog No.S1525

Adavosertib (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.

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In DMSO USD 238 In stock
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7 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 . Adavosertib (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. Adavosertib (MK-1775) purchased from Selleck.

  • Front Oncol, 2018, 8:143. Adavosertib (MK-1775) purchased from Selleck.

    (C) Nude mice bearing MDA-MB-231 xenograft tumors were treated with vehicle, MK-1775, cisplatin, or a combination of cisplatin and MK-1775 for 28 days and tumor volumes were measured. Data are presented as the mean of 8 tumors for each group ± SEM.

    Sci Rep, 2017, 7:43517. Adavosertib (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. Adavosertib (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. Adavosertib (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. Adavosertib (MK-1775) purchased from Selleck.

Purity & Quality Control

Choose Selective Wee1 Inhibitors

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 MnrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XHd2lEPTB;MUOuNkDDuSBzLkGg{txO M4HBbVI2PDV6OUW0
BxPC-3 NWDZOVFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TqRmlEPTB;MD64JOKyKDBwMEOg{txO M4[ySlI2PDV6OUW0
CFPAC-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkWwTWM2OD1|LkOgxtEhOC5{IN88US=> NH35TFgzPTR3OEm1OC=>
HPAC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonOTWM2OD1yLkWgxtEhOC5yMTFOwG0> M1LGW|I2PDV6OUW0
MIAPaCa-2 M{LOR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwNTFCtUAxNjB3IN88US=> M4\4OVI2PDV6OUW0
PANC-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnnbnNKSzVyPUGwMlYhyrFiMT6xJO69VQ>? NFPXZnIzPTR3OEm1OC=>
SK-N-BE (2) MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe4dVRKSzVyPUKuOQKBkcLz4pEJNE4{KM7:TR?= M1zsWVI2OzB6OUG2
SK-N-BE (2), PAN→MK NH3yPZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ4LkdihKnDueLCiUmuOkDPxE1? NVLONZZ{OjV|MEi5NVY>
SK-N-BE (2), MK→PAN MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPITWM2OD1{LkVihKnDueLCiUCuN{DPxE1? M2TLbFI2OzB6OUG2
SK-N-AS M4LZSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwNUFihKnDueLCiUCuNFIh|ryP M2LBdFI2OzB6OUG2
SK-N-DZ M1LaOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLiTWM2OD1yLkO25qCKyrIkgJmwMlAyKM7:TR?= Ml\tNlU{ODh7MU[=
SK-N-AS NUSzbodISXCxcITvd4l{KEG|c3H5 MWS1NFAhdk1? M1HCcVQ5KGh? MVnpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M1rZN|I2OzB6OUG2
SK-N-DZ NIjyeJlCeG:ydH;zbZMhSXO|YYm= MnLuOVAxKG6P NFvOW401QCCq M1viSIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NVrV[|JiOjV|MEi5NVY>
THP-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrGVJk5OTJ3L{K1NE82ODBibl2= NUXDXXJqPDhiaB?= MojGbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NXrJOJNnOjVyOES2NVQ>
MV4-11 M{L0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq3NVI2NzJ3MD:1NFAhdk1? MXS0PEBp MULpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MUeyOVA5PDZzNB?=
U937 NHXtc5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLmbY9{OTJ3L{K1NE82ODBibl2= MXu0PEBp M{nuVIlv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NXTNflA4OjVyOES2NVQ>
HL-60 NGDaV|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWxNlUwOjVyL{WwNEBvVQ>? MYi0PEBp M1PsXolv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NYjuN3FpOjVyOES2NVQ>
OCI-AML3 M1nreGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX2xNlUwOjVyL{WwNEBvVQ>? NGDjbYU1QCCq M{LsSolv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NHHSVI8zPTB6NE[xOC=>
MOLM-13 NV;keohbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHoWm4yOjVxMkWwM|UxOCCwTR?= NInJclQ1QCCq MlzhbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NHnlSGkzPTB6NE[xOC=>
CMK MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYDtbIttOTBvMUCwNFAhdk1? M2PjSlczKGh? M37pXZJm\HWlZYOgZ4VtdCC4aXHsbYJqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MmrVNlQ6PjJ|M{G=
CMY MnvZR4VtdCCYaXHibYxqfHliQYPzZZk> NEfTUXMyOC1zMECwNEBvVQ>? MUi3NkBp NF3TdIpz\WS3Y3XzJINmdGxidnnhcIljcXS7IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NWDDVlhzOjR7NkKzN|E>
Dayo NH3S[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrad4ZFUUN3ME2xOVAhdk1? Mmq2NlQ3PjF7MUC=
UW228 Mo\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e1RmlEPTB;MkOyJI5O MYWyOFY3OTlzMB?=
IST-MES1 MnzXR4VtdCCYaXHibYxqfHliQYPzZZk> NWLmS2hpOTVyL{K1NEBvVQ>? NHPJVXU4OiCq M2O2dIVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NV7ITHFkOjR|NkW3PFI>
IST-MES2 MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUexOVAwOjVyIH7N NXOybXJwPzJiaB?= MoLH[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NFfLb4ozPDN4NUe4Ni=>
REN NXr4VYg3S2WubDDWbYFjcWyrdImgRZN{[Xl? NFXBU5kyPTBxMkWwJI5O Mm\IO|IhcA>? M2TQd4VvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NHzTSIwzPDN4NUe4Ni=>
NCI-H2452 Mnj0R4VtdCCYaXHibYxqfHliQYPzZZk> MVqxOVAwOjVyIH7N NWnNVnRUPzJiaB?= NHHOWotmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NEfpUFczPDN4NUe4Ni=>
MSTO-211H NHLaeohE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUi1Z|ZOOTVyL{K1NEBvVQ>? NEXRco44OiCq MU\lcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NVjNPFZVOjR|NkW3PFI>
NCI-H2052 MlHlR4VtdCCYaXHibYxqfHliQYPzZZk> M4rtUFE2OC9{NUCgcm0> MlOwO|IhcA>? M1G5dYVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M2PUU|I1OzZ3N{iy
WEE1 MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfPcoJzUUN3ME21MlIhdk1? MkDINlM3QTl4NUW=
CDC2 M2nWbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ja[mlEPTExvK6xNFAxKG6P M{KxZVI{Pjl7NkW1
CDK7 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnMWGNvUUN3MP-8olExODBibl2= M4\5fVI{Pjl7NkW1
MYT1 MlPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTyeZFQUUN3ME21N|Ahdk1? M{jrW|I{Pjl7NkW1
T98G  MmrFRZBweHSxc3nzJGF{e2G7 MnfhNVAxNzJ3MDDuUS=> M3fRe|YhcA>? NF\qRY5mdmijbnPld{Bz[WSrYYTpc44ucW6mdXPl[EBk\WyuIHvpcIxqdmd? NFv2N3kzOTl7Mke5Ny=>
A549 Mny1RZBweHSxc3nzJGF{e2G7 MlvJNlAxKG6P NGrhT2gyKGh? MlfIdoFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= M3;TSVIyPzl7MEOz
H460 NIfnSHlCeG:ydH;zbZMhSXO|YYm= MXiyNFAhdk1? MYexJIg> NW[3bG9memGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI> M2XwUFIyPzl7MEOz
H1299 NFzDVJRCeG:ydH;zbZMhSXO|YYm= NUTqN2oyOjByIH7N MVexJIg> Mmi2doFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= NWTCWXJ3OjF5OUmwN|M>
Calu-6  NUDmXld2SXCxcITvd4l{KEG|c3H5 MlnvNlAxKG6P MoqzNUBp NHvRfYVz[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=> NFzrO5AzOTd7OUCzNy=>
WiDr NVK5bGpQU2mwYYPlJGF{e2G7cx?= M4\0fVExNTFyMECwJI5O MUe4JIg> MUjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gR2REOiCjdDDUfZIyPSC5aYToJIFvKEWFNUFCpJZidHWnIH;mJFg2KG6vb3yvUEBxemW2cnXheIVlKHerdHig[4Vu[2m2YXLpcoU> M{mxclE6QDh5NUS1

... 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:

[1]

+ 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:

[1]

+ 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:

[1]

+ 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 10 mg/mL (19.97 mM)
Water 0.0001 mg/mL (0.0 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/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 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
NCT01076400 Terminated Cervical Cancer Merck Sharp & Dohme Corp. May 31 2010 Phase 1|Phase 2
NCT01357161 Completed Ovarian Cancer Merck Sharp & Dohme Corp. July 26 2011 Phase 2
NCT02037230 Recruiting Adenocarcinoma of the Pancreas University of Michigan Cancer Center January 2014 Phase 1|Phase 2
NCT01164995 Unknown status Epithelial Ovarian Cancer The Netherlands Cancer Institute|Merck Sharp & Dohme Corp. July 2010 Phase 2
NCT00648648 Completed Solid Tumors Merck Sharp & Dohme Corp. February 2008 Phase 1
NCT01748825 Active not recruiting Neoplasms|Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 19 2012 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