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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6 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.

  • 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.

    (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.

  • 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.

    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.

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 NX;WUlh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M334[GlEPTB;MUOuNkDDuSBzLkGg{txO M4nT[FI2PDV6OUW0
BxPC-3 NX[wfphWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nVUWlEPTB;MD64JOKyKDBwMEOg{txO MmrINlU1PTh7NUS=
CFPAC-1 NEeyVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3z[Gl2UUN3ME2zMlMhyrFiMD6yJO69VQ>? Ml7ONlU1PTh7NUS=
HPAC MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwNTFCtUAxNjBzIN88US=> MmXYNlU1PTh7NUS=
MIAPaCa-2 NUHLdnVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDEWYV2UUN3ME2wMlUhyrFiMD6wOUDPxE1? NGHiU5EzPTR3OEm1OC=>
PANC-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFyLk[gxtEhOS5zIN88US=> MUKyOVQ2QDl3NB?=
SK-N-BE (2) NVzBfm82T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkizTWM2OD1{LkVihKnDueLCiUCuN{DPxE1? M3nodFI2OzB6OUG2
SK-N-BE (2), PAN→MK NWPYZm9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPDe4ppUUN3ME2yOk436oDLwsJihKk6NjZizszN MYWyOVMxQDlzNh?=
SK-N-BE (2), MK→PAN M{fjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rxdGlEPTB;Mj605qCKyrIkgJmwMlMh|ryP M1LLelI2OzB6OUG2
SK-N-AS NELIbpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDXWpJKSzVyPUCuOVDjiIoEsfMAjVAvODJizszN Ml7NNlU{ODh7MU[=
SK-N-DZ M13Icmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe1d4ZKSzVyPUCuN|bjiIoEsfMAjVAvODFizszN M{PxPVI2OzB6OUG2
SK-N-AS NXzCTZRYSXCxcITvd4l{KEG|c3H5 M3e2SlUxOCCwTR?= Mn:xOFghcA>? M4nTWYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M1PadVI2OzB6OUG2
SK-N-DZ MnvwRZBweHSxc3nzJGF{e2G7 MYK1NFAhdk1? NYDZTHlyPDhiaB?= M4\u[4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M17p[VI2OzB6OUG2
THP-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLkfGNnOTJ3L{K1NE82ODBibl2= MYO0PEBp MVHpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MWWyOVA5PDZzNB?=
MV4-11 M2Tye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHzeWF{OTJ3L{K1NE82ODBibl2= NVLCSpJiPDhiaB?= M{\aXIlv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M2\jXlI2ODh2NkG0
U937 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTOUGoyOjVxMkWwM|UxOCCwTR?= MkfMOFghcA>? NGDMeFJqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NIrB[WEzPTB6NE[xOC=>
HL-60 MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWqxNlUwOjVyL{WwNEBvVQ>? M1q4RlQ5KGh? NVzZdGhzcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MoHQNlUxQDR4MUS=
OCI-AML3 M{PWd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHPXVJ4OTJ3L{K1NE82ODBibl2= M2q2TFQ5KGh? NVL5T5M{cW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MX:yOVA5PDZzNB?=
MOLM-13 Mlv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKxNlUwOjVyL{WwNEBvVQ>? M4DTSFQ5KGh? MlnQbY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NVXuTHFbOjVyOES2NVQ>
CMK M1H6XmNmdGxiVnnhZoltcXS7IFHzd4F6 MWmxNE0yODByMDDuUS=> M{H1[FczKGh? NIrNZmFz\WS3Y3XzJINmdGxidnnhcIljcXS7IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NV;MfIR6OjR7NkKzN|E>
CMY MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M122UlExNTFyMECwJI5O NXPVSldUPzJiaB?= NW\UNXlYemWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?= M4nGOVI1QTZ{M{Ox
Dayo M{LHT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTF3MDDuUS=> NGn2WowzPDZ4MUmxNC=>
UW228 MlfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fCTmlEPTB;MkOyJI5O MYqyOFY3OTlzMB?=
IST-MES1 M4rheGNmdGxiVnnhZoltcXS7IFHzd4F6 NFrkfmcyPTBxMkWwJI5O M2L1d|czKGh? MX3lcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NF;QS4EzPDN4NUe4Ni=>
IST-MES2 M3XMPGNmdGxiVnnhZoltcXS7IFHzd4F6 M2fwO|E2OC9{NUCgcm0> MoTiO|IhcA>? M1\WVoVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NUT2dJBCOjR|NkW3PFI>
REN MlHRR4VtdCCYaXHibYxqfHliQYPzZZk> M2fKc|E2OC9{NUCgcm0> NFLHSpA4OiCq MYnlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> M2ftSlI1OzZ3N{iy
NCI-H2452 NX\oUVBlS2WubDDWbYFjcWyrdImgRZN{[Xl? NWnPU3hyOTVyL{K1NEBvVQ>? MUK3NkBp MUnlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NYPKUY43OjR|NkW3PFI>
MSTO-211H NXfYe3QyS2WubDDWbYFjcWyrdImgRZN{[Xl? NEnJXlkyPTBxMkWwJI5O M3TBO|czKGh? MUnlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NU\MUZlVOjR|NkW3PFI>
NCI-H2052 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXixOVAwOjVyIH7N NVH6R3Z5PzJiaB?= M2rCfIVvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NYCzUmdlOjR|NkW3PFI>
WEE1 M4Labmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIH3cY1KSzVyPUWuNkBvVQ>? Moe2NlM3QTl4NUW=
CDC2 NF\Jb|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|Ux97zgMUCwNEBvVQ>? M4O0UFI{Pjl7NkW1
CDK7 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHi3RldKSzVy78{eNVAxOCCwTR?= M4jmUlI{Pjl7NkW1
MYT1 Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTV|MDDuUS=> NELSeYozOzZ7OU[1OS=>
T98G  MWDBdI9xfG:|aYOgRZN{[Xl? MlzmNVAxNzJ3MDDuUS=> MoqyOkBp M3nSV4VvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJINmdGxia3nscIlv\w>? MmXFNlE6QTJ5OUO=
A549 MV3BdI9xfG:|aYOgRZN{[Xl? NU\yNpZLOjByIH7N M2H6WlEhcA>? M2L6d5Ji\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXy Mn\tNlE4QTlyM{O=
H460 NEP2TZVCeG:ydH;zbZMhSXO|YYm= NY\TOIhiOjByIH7N Ml3JNUBp MmDvdoFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= MVKyNVc6QTB|Mx?=
H1299 MmLKRZBweHSxc3nzJGF{e2G7 Ml:yNlAxKG6P NHHQSFIyKGh? M1nvR5Ji\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXy MV[yNVc6QTB|Mx?=
Calu-6  NHPQWlBCeG:ydH;zbZMhSXO|YYm= MWiyNFAhdk1? M2PUbVEhcA>? MYXyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= MlzBNlE4QTlyM{O=
WiDr NHXRXWdMcW6jc3WgRZN{[Xm| MV[xNE0yODByMDDuUS=> MWe4JIg> MX3pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gR2REOiCjdDDUfZIyPSC5aYToJIFvKEWFNUFCpJZidHWnIH;mJFg2KG6vb3yvUEBxemW2cnXheIVlKHerdHig[4Vu[2m2YXLpcoU> NUPIZWRROTl6OEe1OFU>

... 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:
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
NCT02037230 Recruiting Adenocarcinoma of the Pancreas University of Michigan Cancer Center January 2014 Phase 1|Phase 2
NCT01357161 Completed Ovarian Cancer Merck Sharp & Dohme Corp. July 2011 Phase 2
NCT01164995 Unknown status 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
NCT00648648 Completed Solid Tumors Merck Sharp & Dohme Corp. February 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.

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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