Adavosertib (MK-1775)

目录号:S1525

Adavosertib (MK-1775) Chemical Structure

Molecular Weight(MW): 500.6

MK-1775是一种有效的,高选择性Wee1抑制剂,无细胞试验中IC50为5.2 nM;阻碍G2期DNA损伤检验点。Phase 2。

规格 价格 库存 购买数量  
RMB 1960.96 现货
RMB 1376.38 现货
RMB 2226.67 现货
RMB 3835.28 现货
RMB 6297.29 现货
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客户使用该产品的6个实验数据:

  • 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.

产品安全说明书

Wee1抑制剂选择性比较

生物活性

产品描述 MK-1775是一种有效的,高选择性Wee1抑制剂,无细胞试验中IC50为5.2 nM;阻碍G2期DNA损伤检验点。Phase 2。
特性 首个报道的 Wee1抑制剂。
靶点
Wee1 [1]
(Cell-free assay)
5.2 nM
体外研究

MK-1775以ATP竞争的方式抑制Wee1激酶。与作用于Wee1相比,MK-1775对Yes的效能低2-到3-倍,IC50为14 nM,对7种其他激酶的效能低10倍,1 μM浓度下抑制率>80%,比对人Myt 1选择性高100倍以上,并抑制周期蛋白依赖性激酶1 (CDC2) 在可选择位点(Thr14) 的磷酸化作用。通过阻断负荷突变型p53的WiDr细胞中Wee1活性,废止DNA损伤检控点,MK-1775治疗抑制Tyr15 (CDC2Y15)位点的CDC2基础磷酸化作用,EC50为49 nM,并剂量依赖性抑制gemcitabine-,carboplatin- 或cisplatin-诱导的CDC2磷酸化和细胞周期阻滞,EC50分别为82 nM和81 nM,180 nM 和163 nM,以及159 nM 和 160 nM。30-100 nM 的MK-1775单独治疗在WiDr 和 H1299细胞中没有显著的抗增殖作用,而300 nM的MK-1775足以抑制>80%的Wee1,表现出温和但显著的抗增殖作用,在WiDr和H1299细胞中抑制率分别为34.1%和28.4%。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ASPC-1 M13aWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPJTWM2OD1zMz6yJOKyKDFwMTFOwG0> MXeyOVQ2QDl3NB?=
BxPC-3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\POWZKSzVyPUCuPEDDuSByLkCzJO69VQ>? NUPOZXFZOjV2NUi5OVQ>
CFPAC-1 NF7MdVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjwVmVKSzVyPUOuN{DDuSByLkKg{txO NXPV[nM3OjV2NUi5OVQ>
HPAC M4jrbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnztTWM2OD1yLkWgxtEhOC5yMTFOwG0> Mor4NlU1PTh7NUS=
MIAPaCa-2 Mlr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwNTFCtUAxNjB3IN88US=> NIS4cZYzPTR3OEm1OC=>
PANC-1 NXi1flJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TOeWlEPTB;MUCuOkDDuSBzLkGg{txO NVG0eYJlOjV2NUi5OVQ>
SK-N-BE (2) NGLrcpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPQbIhMUUN3ME2yMlTjiIoEsfMAjVAvOyEQvF2= M1r3dlI2OzB6OUG2
SK-N-BE (2), PAN→MK NVjB[lA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDwWJhuUUN3ME2yOk436oDLwsJihKk6NjZizszN M{jCPFI2OzB6OUG2
SK-N-BE (2), MK→PAN M4Hafmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorTTWM2OD1{LkVihKnDueLCiUCuN{DPxE1? NVLJbI9oOjV|MEi5NVY>
SK-N-AS NEPzVoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjjTWM2OD1yLkWw5qCKyrIkgJmwMlAzKM7:TR?= MX6yOVMxQDlzNh?=
SK-N-DZ NXzjNFV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[xcY9PUUN3ME2wMlM36oDLwsJihKkxNjBzIN88US=> NVfJWY1IOjV|MEi5NVY>
SK-N-AS MXvBdI9xfG:|aYOgRZN{[Xl? M33tOFUxOCCwTR?= M3PtZlQ5KGh? MkTNbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NF\iVWkzPTNyOEmxOi=>
SK-N-DZ M3yzbmFxd3C2b4Ppd{BCe3OjeR?= MnfmOVAxKG6P NV\mWHkyPDhiaB?= MWHpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MkjpNlU{ODh7MU[=
THP-1 M1zWO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxNlUwOjVyL{WwNEBvVQ>? M1rDSVQ5KGh? NGLlNo9qdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MWKyOVA5PDZzNB?=
MV4-11 NHXtTJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqxNlUwOjVyL{WwNEBvVQ>? NGPDc3M1QCCq NHnT[GpqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NEK5UYszPTB6NE[xOC=>
U937 NHS2e2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LQWFEzPS9{NUCvOVAxKG6P M{fXUFQ5KGh? NF:wNFZqdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MVuyOVA5PDZzNB?=
HL-60 MnrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInlZXgyOjVxMkWwM|UxOCCwTR?= M2nNbFQ5KGh? NV7a[GsxcW6lcnXhd4V{KGOnbHyg[IVifGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NXLZO|E6OjVyOES2NVQ>
OCI-AML3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmO0NVI2NzJ3MD:1NFAhdk1? MXe0PEBp NIrZO21qdmO{ZXHz[ZMh[2WubDDk[YF1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NXTNbllqOjVyOES2NVQ>
MOLM-13 NF3XU|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\ZNVI2NzJ3MD:1NFAhdk1? M1zWTVQ5KGh? MWnpcoNz\WG|ZYOgZ4VtdCCmZXH0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MkTyNlUxQDR4MUS=
CMK MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2SzeVExNTFyMECwJI5O MWe3NkBp NX3rTYhZemWmdXPld{Bk\WyuII\pZYxq[mm2eTDpckBiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JI1idm6nch?= MmD4NlQ6PjJ|M{G=
CMY MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoP0NVAuOTByMECgcm0> NEG4SFU4OiCq MVLy[YR2[2W|IHPlcIwhfmmjbHnibZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz Mmq2NlQ6PjJ|M{G=
Dayo MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTF3MDDuUS=> NXrJTng6OjR4NkG5NVA>
UW228 NGLyTm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37PNGlEPTB;MkOyJI5O MYiyOFY3OTlzMB?=
IST-MES1 Mkf4R4VtdCCYaXHibYxqfHliQYPzZZk> MU[xOVAwOjVyIH7N MmnNO|IhcA>? MlfK[Y5p[W6lZYOgeIhmKGOrc4DsZZRqdiCleYTveI95cWNiZX\m[YN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MojtNlQ{PjV5OEK=
IST-MES2 M2\VWGNmdGxiVnnhZoltcXS7IFHzd4F6 NI\Yfo4yPTBxMkWwJI5O NGTBV4M4OiCq NIriR3lmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NG\xO5YzPDN4NUe4Ni=>
REN NVP2OZhVS2WubDDWbYFjcWyrdImgRZN{[Xl? MknENVUxNzJ3MDDuUS=> MV23NkBp NWH1[Glr\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ MlzrNlQ{PjV5OEK=
NCI-H2452 MkD4R4VtdCCYaXHibYxqfHliQYPzZZk> MXyxOVAwOjVyIH7N NUfQR|ZtPzJiaB?= MUnlcohidmOnczD0bIUh[2m|cHzheIlvKGO7dH;0c5hq[yCnZn\lZ5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NV3nTWdoOjR|NkW3PFI>
MSTO-211H MX7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYH2dldzOTVyL{K1NEBvVQ>? NEf5d2U4OiCq NX;ZZWZU\W6qYX7j[ZMhfGinIHPpd5Bt[XSrbjDjfZRwfG:6aXOg[YZn\WO2IHnuJIEh[2:wY3XueJJifGmxbj3k[ZBmdmSnboSgcYFvdmW{ NE\IcIUzPDN4NUe4Ni=>
NCI-H2052 MkLER4VtdCCYaXHibYxqfHliQYPzZZk> MVWxOVAwOjVyIH7N MUW3NkBp NH;pTlZmdmijbnPld{B1cGViY3nzdIxifGmwIHP5eI91d3irYzDl[oZm[3RiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MV6yOFM3PTd6Mh?=
WEE1 MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq0TWM2OD13LkKgcm0> MWiyN|Y6QTZ3NR?=
CDC2 M2Hz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf5b2NHUUN3MP-8olExODBibl2= MnG0NlM3QTl4NUW=
CDK7 NXvyWFc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHW3TW5KSzVy78{eNVAxOCCwTR?= NV70Z|ZYOjN4OUm2OVU>
MYT1 NF\INoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvaTWM2OD13M{Cgcm0> M2rxc|I{Pjl7NkW1
T98G  M4iw[WFxd3C2b4Ppd{BCe3OjeR?= MoTCNVAxNzJ3MDDuUS=> NF3HPGs3KGh? MkP4[Y5p[W6lZYOgdoFlcWG2aX;uMYlv\HWlZXSgZ4VtdCCtaXzsbY5o NHf3RnUzOTl7Mke5Ny=>
A549 MVvBdI9xfG:|aYOgRZN{[Xl? NUTtZXpzOjByIH7N NGThTFcyKGh? NXXYNJZkemGmaX;z[Y5{cXSrenXzJG5US0yFIHPlcIx{KGmwIHGgdFU{NWSncHXu[IVvfCCvYX7u[ZI> NF;qZmozOTd7OUCzNy=>
H460 NVjIe4ROSXCxcITvd4l{KEG|c3H5 Mn7wNlAxKG6P NFLtUVAyKGh? MV7yZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= NEfOPIIzOTd7OUCzNy=>
H1299 NEjvdYtCeG:ydH;zbZMhSXO|YYm= M3\CS|IxOCCwTR?= NHrITJIyKGh? MYHyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= M{nyNFIyPzl7MEOz
Calu-6  NIHYeHRCeG:ydH;zbZMhSXO|YYm= NHXySlIzODBibl2= NXvFc3ZyOSCq MUDyZYRqd3OnboPpeIl7\XNiTmPDUGMh[2WubIOgbY4h[SCyNUOt[IVx\W6mZX70JI1idm6nch?= M1Pu[lIyPzl7MEOz
WiDr NHK5eW1McW6jc3WgRZN{[Xm| NVjZV2FbOTBvMUCwNFAhdk1? NVPhRplKQCCq NIrqenNqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhS0SFMjDheEBVgXJzNTD3bZRpKGGwIFXDOVDDqH[jbIXlJI9nKDh3IH7tc4wwVCCycnX0doVifGWmIIfpeIgh\2WvY3n0ZYJqdmV? NFu2PI4yQTh6N{W0OS=>

... Click to View More Cell Line Experimental Data

体内研究 MK-1775(~20 mg/kg)单独治疗对WiDr异种移植物表现出最小的抗肿瘤作用,在大鼠体内第3天时T/C为69%。在裸鼠HeLa-luc和TOV21G-shp53异种移植模型中,MK-1775单独的抗肿瘤效能是温和的。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

+ 展开

体外激酶试验:

使用重组人Wee1。激酶反应使用10 μM ATP,1.0 μCi of [γ-33P]ATP,和2.5 μg poly(Lys, Tyr)作为底物,在逐渐增加浓度的MK-1775存在下,在30°C环境中进行30分钟。整合到底物的放射性被捕获到MultiScreen-PH平板,在液体闪烁计数器上计数。
细胞实验:

[1]

+ 展开
  • Cell lines: WiDr,NCI-H1299,TOV21G,和 HeLa细胞
  • Concentrations: 在DMSO中溶解,终浓度为~10 μM
  • Incubation Time: 24小时
  • Method: 细胞在gemcitabine存在或不存在下处理24小时,然后用MK-1775再处理24小时。细胞活性使用SpectraMax通过WST-8试剂盒测定。细胞内caspase-3/7活性使用Caspase-3/7 Glo试剂盒测定。
    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: 负荷WiDr,HeLa-luc,或TOV21G-shp53肿瘤的免疫缺陷裸鼠(F344/NJcl-rnu)
  • Formulation: 在0.5%甲基纤维素溶液载体中制备
  • Dosages: ~20 mg/kg/day
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 80 mg/mL (159.8 mM)
Ethanol 10 mg/mL (19.97 mM)
Water 0.0001 mg/mL (0.0 mM)
体内 从左到右依次将纯溶剂加入产品,现配现用:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 500.6
化学式

C27H32N8O2

CAS号 955365-80-7
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

相关Wee1产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID