MK-1775

製品コードS1525

MK-1775化学構造

分子量(MW):500.6

MK-1775は一種の有効で、選択性的なWee1阻害剤で、無細胞試験でIC50値が5.2nMですが、G2期DNA損傷チェックポイント(checkpoint)を防げます。臨床2期。

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カスタマーフィードバック(5)

  • 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.

製品安全説明書

Wee1阻害剤の選択性比較

生物活性

製品説明 MK-1775は一種の有効で、選択性的なWee1阻害剤で、無細胞試験でIC50値が5.2nMですが、G2期DNA損傷チェックポイント(checkpoint)を防げます。臨床2期。
特性 The first reported Wee1 inhibitor.
ターゲット
Wee1 [1]
(Cell-free assay)
5.2 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ASPC-1 NEDLXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LzWmlEPTB;MUOuNkDDuSBzLkGg{txO MUCyOVQ2QDl3NB?=
BxPC-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDFTWM2OD1yLkigxtEhOC5yMzFOwG0> M2DqS|I2PDV6OUW0
CFPAC-1 NGjxSYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\pOWlEPTB;Mz6zJOKyKDBwMjFOwG0> NWXBZYNsOjV2NUi5OVQ>
HPAC MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\RWHBKSzVyPUCuOUDDuSByLkCxJO69VQ>? NVfWcG5nOjV2NUi5OVQ>
MIAPaCa-2 MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fYc2lEPTB;MD61JOKyKDBwMEWg{txO M1KxRVI2PDV6OUW0
PANC-1 NH3qeFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTFyLk[gxtEhOS5zIN88US=> MUGyOVQ2QDl3NB?=
SK-N-BE (2) NWDxW3U1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPRfmFKSzVyPUKuOQKBkcLz4pEJNE4{KM7:TR?= MmHaNlU{ODh7MU[=
SK-N-BE (2), PAN→MK NISy[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHIVFlKSzVyPUK2MlbjiIoEsfMAjVkvPiEQvF2= NGTNeI8zPTNyOEmxOi=>
SK-N-BE (2), MK→PAN M3OxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnWxTWM2OD1{LkVihKnDueLCiUCuN{DPxE1? MkDCNlU{ODh7MU[=
SK-N-AS NUiwN|RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DqSmlEPTB;MD61NQKBkcLz4pEJNE4xOiEQvF2= MX2yOVMxQDlzNh?=
SK-N-DZ MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzSZo1KSzVyPUCuN|bjiIoEsfMAjVAvODFizszN M{TORlI2OzB6OUG2
SK-N-AS NVvzfJp[SXCxcITvd4l{KEG|c3H5 NGn2R2M2ODBibl2= MWi0PEBp NYDFT5JTcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NHTBWm0zPTNyOEmxOi=>
SK-N-DZ NUHUeHd5SXCxcITvd4l{KEG|c3H5 MnvvOVAxKG6P M371SVQ5KGh? MVfpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NEnQN48zPTNyOEmxOi=>
THP-1 NULyWlFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXexNlUwOjVyL{WwNEBvVQ>? NEHweFY1QCCq MYTpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NECyflgzPTB6NE[xOC=>
MV4-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon3NVI2NzJ3MD:1NFAhdk1? M4j0TlQ5KGh? NUL5RmROcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? M2fUd|I2ODh2NkG0
U937 NFjmdVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3W5NVEzPS9{NUCvOVAxKG6P M3jCZVQ5KGh? NITqRm5qdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? Mn\DNlUxQDR4MUS=
HL-60 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXMSJQyOjVxMkWwM|UxOCCwTR?= MUi0PEBp MWrpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> M3v0ZVI2ODh2NkG0
OCI-AML3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH5NVI2NzJ3MD:1NFAhdk1? NGnIZo01QCCq NIrLeo5qdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NYfiV|RoOjVyOES2NVQ>
MOLM-13 NInxfGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzsR3JPOTJ3L{K1NE82ODBibl2= NVfvNJJHPDhiaB?= NV;YVodmcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NX\nc2p[OjVyOES2NVQ>
CMK M1PqV2NmdGxiVnnhZoltcXS7IFHzd4F6 M{fuPFExNTFyMECwJI5O NV\4V4FbPzJiaB?= MWjy[YR2[2W|IHPlcIwhfmmjbHnibZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M2DXUFI1QTZ{M{Ox
CMY MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M37uN|ExNTFyMECwJI5O NXzsU|I5PzJiaB?= NFnEWYVz\WS3Y3XzJINmdGxidnnhcIljcXS7IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ M1rsTVI1QTZ{M{Ox
Dayo M3TDRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXK[XJ5UUN3ME2xOVAhdk1? NWLT[VhHOjR4NkG5NVA>
UW228 M36w[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTJ|MjDuUS=> NHfJRoIzPDZ4MUmxNC=>
IST-MES1 NFPEWHBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHPMRW8yPTBxMkWwJI5O MXS3NkBp MXHlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MWGyOFM3PTd6Mh?=
IST-MES2 NHuwc|FE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXuxOVAwOjVyIH7N NVzycpk3PzJiaB?= NEixSVFmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MYGyOFM3PTd6Mh?=
REN NX[wXXM6S2WubDDWbYFjcWyrdImgRZN{[Xl? M4XqOFE2OC9{NUCgcm0> MU[3NkBp MWTlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NHXNemEzPDN4NUe4Ni=>
NCI-H2452 MkiyR4VtdCCYaXHibYxqfHliQYPzZZk> MnHyNVUxNzJ3MDDuUS=> NX;S[5Y5PzJiaB?= NXzhWGpz\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ M3q3elI1OzZ3N{iy
MSTO-211H NF3ISpJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV7tWXdTOTVyL{K1NEBvVQ>? NYf4XZVpPzJiaB?= NW\LSG06\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MUGyOFM3PTd6Mh?=
NCI-H2052 MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVvsUmRlOTVyL{K1NEBvVQ>? NIL6UW44OiCq MXjlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NXrNc2gzOjR|NkW3PFI>
WEE1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTVwMjDuUS=> MoTuNlM3QTl4NUW=
CDC2 Mmj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|Ux97zgMUCwNEBvVQ>? NGPlTIUzOzZ7OU[1OS=>
CDK7 M4PJOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|Ux97zgMUCwNEBvVQ>? MY[yN|Y6QTZ3NR?=
MYT1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjlTWM2OD13M{Cgcm0> MortNlM3QTl4NUW=
T98G  NWrTT|N2SXCxcITvd4l{KEG|c3H5 M3HhUlExOC9{NUCgcm0> M3i1SFYhcA>? MXTlcohidmOnczDyZYRq[XSrb36tbY5lfWOnZDDj[YxtKGurbHzpcoc> MVyyNVk6Ojd7Mx?=
A549 M1fqb2Fxd3C2b4Ppd{BCe3OjeR?= MUSyNFAhdk1? MYexJIg> MkT3doFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= M{LyRVIyPzl7MEOz
H460 MlzrRZBweHSxc3nzJGF{e2G7 MU[yNFAhdk1? NFLieYEyKGh? NEDVW2dz[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=> NVjLd3o{OjF5OUmwN|M>
H1299 MUfBdI9xfG:|aYOgRZN{[Xl? MnX0NlAxKG6P MXOxJIg> NHzkV4Jz[WSrb4PlcpNqfGm8ZYOgUnNEVENiY3XscJMhcW5iYTDwOVMu\GWyZX7k[Y51KG2jbn7ldi=> MXOyNVc6QTB|Mx?=
Calu-6  MonFRZBweHSxc3nzJGF{e2G7 NGXtbGQzODBibl2= NIPmXY0yKGh? MmnldoFlcW:|ZX7zbZRqgmW|IF7TR2xEKGOnbHzzJIlvKGFicEWzMYRmeGWwZHXueEBu[W6wZYK= NIPDSZAzOTd7OUCzNy=>
WiDr MVrLbY5ie2ViQYPzZZl{ NGPjSYYyOC1zMECwNEBvVQ>? MmfGPEBp NF7l[41qdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhS0SFMjDheEBVgXJzNTD3bZRpKGGwIFXDOVDDqH[jbIXlJI9nKDh3IH7tc4wwVCCycnX0doVifGWmIIfpeIgh\2WvY3n0ZYJqdmV? NYjzPXZIOTl6OEe1OFU>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[1]

+ 展開
  • 細胞株: WiDr, NCI-H1299, TOV21G, and HeLa
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 24 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Immunodeficient nude rats (F344/NJcl-rnu) bearing WiDr, HeLa-luc, or TOV21G-shp53 tumors
  • 製剤: Prepared in a vehicle of 0.5% methylcellulose solution
  • 投薬量: ~20 mg/kg/day
  • 投与方法: Orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 80 mg/mL (159.8 mM)
Ethanol slightly soluble or insoluble
Water 0.0001 mg/mL (0.0 mM)
体内 順序で溶剤を入れること:
2% DMSO+30% PEG 300+5% Tween+ddH2O
5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 500.6
化学式

C27H32N8O2

CAS No. 955365-80-7
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

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

  • 回答:

    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信号経路図

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID