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

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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

Choose Selective Wee1 Inhibitors

Click to view more

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 NEnTWmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjsfYFKSzVyPUGzMlIhyrFiMT6xJO69VQ>? M3[xNVI2PDV6OUW0
BxPC-3 NUK4dGhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTBwODFCtUAxNjB|IN88US=> MkHtNlU1PTh7NUS=
CFPAC-1 MnP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHMOYc2UUN3ME2zMlMhyrFiMD6yJO69VQ>? NH2zW|EzPTR3OEm1OC=>
HPAC NYDX[GZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e4[WlEPTB;MD61JOKyKDBwMEGg{txO MV[yOVQ2QDl3NB?=
MIAPaCa-2 NHrmeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjuZVNKSzVyPUCuOUDDuSByLkC1JO69VQ>? NF2wU28zPTR3OEm1OC=>
PANC-1 NHP5W5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTrZY1WUUN3ME2xNE43KMLzIEGuNUDPxE1? M{O3ZVI2PDV6OUW0
SK-N-BE (2) NI\nSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJwNPMAjeKy6oDLMD6zJO69VQ>? M2ThRVI2OzB6OUG2
SK-N-BE (2), PAN→MK MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HPcWlEPTB;Mk[uOwKBkcLz4pEJPU43KM7:TR?= Mn\nNlU{ODh7MU[=
SK-N-BE (2), MK→PAN MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\SbJJKSzVyPUKuOQKBkcLz4pEJNE4{KM7:TR?= MYGyOVMxQDlzNh?=
SK-N-AS NXHQT5Q6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHKTWM2OD1yLkWw5qCKyrIkgJmwMlAzKM7:TR?= NUnvTFN6OjV|MEi5NVY>
SK-N-DZ MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\ZO2lEPTB;MD6zOwKBkcLz4pEJNE4xOSEQvF2= NWjXXHdxOjV|MEi5NVY>
SK-N-AS M{\DNmFxd3C2b4Ppd{BCe3OjeR?= NYWxd5FDPTByIH7N NIrGW5A1QCCq MmG1bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MYeyOVMxQDlzNh?=
SK-N-DZ M2rWdmFxd3C2b4Ppd{BCe3OjeR?= NFTDZXM2ODBibl2= NEDFe4g1QCCq NXq1dXI{cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NXPwRm94OjV|MEi5NVY>
THP-1 M1W4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PBUVEzPS9{NUCvOVAxKG6P MofUOFghcA>? M2C2VYlv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M4rwUlI2ODh2NkG0
MV4-11 Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV73cHhMOTJ3L{K1NE82ODBibl2= MljiOFghcA>? MWjpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NH62V2gzPTB6NE[xOC=>
U937 NYryVYU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jtXFEzPS9{NUCvOVAxKG6P MXm0PEBp M{fWfYlv[3KnYYPld{Bk\WyuIHTlZZRpKGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MkXZNlUxQDR4MUS=
HL-60 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xNlUwOjVyL{WwNEBvVQ>? M2XvWlQ5KGh? NYnudWw2cW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MUOyOVA5PDZzNB?=
OCI-AML3 NH75RldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\HXVEzPS9{NUCvOVAxKG6P NIOzNIk1QCCq NVjQem51cW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? Mlu4NlUxQDR4MUS=
MOLM-13 NFex[m5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLzNVI2NzJ3MD:1NFAhdk1? MWW0PEBp Mon4bY5kemWjc3XzJINmdGxiZHXheIghcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> M3TiclI2ODh2NkG0
CMK NYOybIh1S2WubDDWbYFjcWyrdImgRZN{[Xl? MV6xNE0yODByMDDuUS=> NGjvVnc4OiCq MXzy[YR2[2W|IHPlcIwhfmmjbHnibZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MkPJNlQ6PjJ|M{G=
CMY NHPhc5BE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUKxNE0yODByMDDuUS=> NWPYWI9ZPzJiaB?= MUfy[YR2[2W|IHPlcIwhfmmjbHnibZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M3;OeFI1QTZ{M{Ox
Dayo MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj1bIlKSzVyPUG1NEBvVQ>? NUHGcFd1OjR4NkG5NVA>
UW228 NFLZRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\kOWlEPTB;MkOyJI5O MVeyOFY3OTlzMB?=
IST-MES1 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGfmXFYyPTBxMkWwJI5O NHixWWU4OiCq NF3UV|BmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MlHKNlQ{PjV5OEK=
IST-MES2 NH;odFVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGLrNmYyPTBxMkWwJI5O NXLXfmljPzJiaB?= NFfmbGVmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NW\4eWJoOjR|NkW3PFI>
REN M4rkWGNmdGxiVnnhZoltcXS7IFHzd4F6 MUixOVAwOjVyIH7N MXq3NkBp Mn;Y[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MnKwNlQ{PjV5OEK=
NCI-H2452 M1zPOWNmdGxiVnnhZoltcXS7IFHzd4F6 Mnq5NVUxNzJ3MDDuUS=> NIfneJQ4OiCq NV\WNVhN\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NW\VWXBQOjR|NkW3PFI>
MSTO-211H NHnGNXZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1izZVE2OC9{NUCgcm0> NID1RoQ4OiCq NYq0cVV7\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MWOyOFM3PTd6Mh?=
NCI-H2052 M{fsT2NmdGxiVnnhZoltcXS7IFHzd4F6 MVGxOVAwOjVyIH7N NF3VfmE4OiCq M4\4b4VvcGGwY3XzJJRp\SClaYPwcIF1cW5iY4n0c5RwgGmlIHXm[oVkfCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MnTzNlQ{PjV5OEK=
WEE1 NXi5PGF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPrSZBKSzVyPUWuNkBvVQ>? NHqzO4ozOzZ7OU[1OS=>
CDC2 NVjhW|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\JXFZEUUN3MP-8olExODBibl2= MV[yN|Y6QTZ3NR?=
CDK7 NFm5N4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4O0NGlEPTExvK6xNFAxKG6P NXrIRVRROjN4OUm2OVU>
MYT1 NXz6OFRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLCTWM2OD13M{Cgcm0> M1u3VlI{Pjl7NkW1
T98G  MWrBdI9xfG:|aYOgRZN{[Xl? NF3EfVUyODBxMkWwJI5O MUS2JIg> NYDDWpo2\W6qYX7j[ZMhemGmaXH0bY9vNWmwZIXj[YQh[2WubDDrbYxtcW6p M1XZdFIyQTl{N{mz
A549 MXjBdI9xfG:|aYOgRZN{[Xl? M1m4PFIxOCCwTR?= M{P6OVEhcA>? M4fCdJJi\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXy MmW2NlE4QTlyM{O=
H460 NGPiVoZCeG:ydH;zbZMhSXO|YYm= M4DPOlIxOCCwTR?= MoXKNUBp MnH1doFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= NGjsUHczOTd7OUCzNy=>
H1299 MkHHRZBweHSxc3nzJGF{e2G7 MkK4NlAxKG6P NIrSOJAyKGh? MnfpdoFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= M1W0OFIyPzl7MEOz
Calu-6  M3LROWFxd3C2b4Ppd{BCe3OjeR?= M1nQ[VIxOCCwTR?= NV7XSIQ6OSCq M{jYTZJi\Gmxc3Xud4l1cXqnczDOV2NNSyClZXzsd{BqdiCjIIC1N{1l\XCnbnTlcpQhdWGwbnXy MUKyNVc6QTB|Mx?=
WiDr M1zvV2tqdmG|ZTDBd5NigXN? M17PbFExNTFyMECwJI5O MkOzPEBp NXvCfnhQcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEOGQ{KgZZQhXHm{MUWge4l1cCCjbjDFR|UxyqC4YXz1[UBw\iB6NTDucY9tN0xicILleJJm[XSnZDD3bZRpKGenbXPpeIFjcW6n MnjBNVk5QDd3NEW=

... 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 <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

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
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.

  • * Indicates a Required Field

Wee1 Signaling Pathway Map

Related Wee1 Products

Tags: buy MK-1775 | MK-1775 supplier | purchase MK-1775 | MK-1775 cost | MK-1775 manufacturer | order MK-1775 | MK-1775 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID