MK-8776 (SCH 900776)

For research use only. Not for use in humans.

目录号:S2735

MK-8776 (SCH 900776) Chemical Structure

CAS No. 891494-63-6

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂,无细胞试验中IC50为3 nM,比作用于Chk2选择性高500倍。Phase 2。

规格 价格 库存 购买数量  
RMB 1733.35 现货
RMB 3015.42 现货
RMB 7966.05 现货
RMB 20229.3 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的MK-8776 (SCH 900776)发表文献32篇:

产品安全说明书

Chk抑制剂选择性比较

生物活性

产品描述 MK-8776 (SCH 900776)是一种选择性Chk1抑制剂,无细胞试验中IC50为3 nM,比作用于Chk2选择性高500倍。Phase 2。
靶点
Chk1 [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
3 nM 0.16 μM
体外研究

SCH 900776是Chk2和CDK2的低效抑制剂,IC50分别为1.5 μM 和 0.16 μM。SCH 900776对细胞色素P450人肝微粒体亚型1A2,2C9,2C19,2D6,和3A4没有显著的抑制作用。羟基脲下暴露24小时后,SCH 900776诱导DNA复制能力剂量依赖性损失。SCH 900776增强γ-H2AX对羟基脲,5-氟尿嘧啶,和阿糖孢苷的响应。与抗代谢物结合,SCH 900776在2小时内诱导γ-H2AX的累积,表明复制叉瓦解,并且双链DNA断裂。此外,SCH 900776以剂量依赖的方式抑制Chk1 pS296自磷酸化的积累。增殖的WS1细胞暴露于SCH 900776,与Chk1 pS345快速的,剂量依赖性聚集相关,表明正常细胞的循环群诱导Chk1 pS345在暴露于SCH 900776后,是一部分无效循环,这也许通过AT-家族激酶和DNA-PK驱动。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U251 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3ZNlAxNzJyMECgcm0> NGHkUmwzPCCq NYfBPHIx\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NFuzbYczPDN3OUWyOi=>
HCT115 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKyNFAwOjByMDDuUS=> MlvaNlQhcA>? NXLaU5pV\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l M1;kUFI1OzV7NUK2
SW620 NELVUVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUeyNFAwOjByMDDuUS=> M2TXPFI1KGh? NGLwbWVl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NVy1UpRMOjR|NUm1NlY>
IGROV-1 M4HySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\3U|IxOC9{MECwJI5O NV;oVGtZOjRiaB?= NUjLUYlJ\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l MVKyOFM2QTV{Nh?=
HCT116 NFjkN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jxRlIxOC9{MECwJI5O Ml;FNlQhcA>? M4\KdYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NHO2XIYzPDN3OUWyOi=>
MCF10A NH3lTZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7nNlAxNzJyMECgcm0> Mkm0NlQhcA>? NYrUb5pq\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l M3TBS|I1OzV7NUK2
MiaPaCa-2 NIfZOllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e1S|IxOC9{MECwJI5O MVeyOEBp Mn\5[IVkemWjc3XzJJRp\SCLQ{WwJI9nKEenbXPpeIFjcW6n MYeyOFM2QTV{Nh?=
MDA-MB-231 NUfxXHk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETqOpozODBxMkCwNEBvVQ>? NFXOV|kzPCCq NEC5PGdl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NYLCXlNtOjR|NUm1NlY>
HCC2998 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PwdlIxOC9{MECwJI5O MV:yOEBp NUixWoZm\GWlcnXhd4V{KHSqZTDJR|UxKG:oIFflcYNqfGGkaX7l NVHNTZg5OjR|NUm1NlY>
U87 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzhXZozODBxMkCwNEBvVQ>? NFTpW2wzPCCq M3;CRoRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NFvwWmszPDN3OUWyOi=>
MDA-MB-435 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLmb|QzOjByL{KwNFAhdk1? NVfBNo5[OjRiaB?= NI\Gfoxl\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= MWiyOFM2QTV{Nh?=
SNB19 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTNVYkzODBxMkCwNEBvVQ>? MljDNlQhcA>? MUDk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M4rNVFI1OzV7NUK2
U20S MoDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[yNFAwOjByMDDuUS=> M4PWWlI1KGh? MYnk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? M2T0T|I1OzV7NUK2
A498 MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\GT|IxOC9{MECwJI5O M2PBZlI1KGh? M3LQRYRm[3KnYYPld{B1cGViSVO1NEBw\iCJZX3jbZRi[mmwZR?= NF;2VXMzPDN3OUWyOi=>
TK10 NEfjXXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKyNFAwOjByMDDuUS=> NGHnXWIzPCCq NELhRYll\WO{ZXHz[ZMhfGinIFnDOVAhd2ZiR3XtZ4l1[WKrbnW= NUPXbpd2OjR|NUm1NlY>
AsPC-1 M3rGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnwSo1nOjByL{KwNFAhdk1? MYGyOEBp MVvk[YNz\WG|ZYOgeIhmKEmFNUCgc4YhT2WvY3n0ZYJqdmV? NWjoenpLOjR|NUm1NlY>
H23 MkDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXnN4Q2PTByIH7N NHLEeGQzPCCq M4jhW2ROW09? MXflcohidmOnczD0bIUh[2inbX;z[Y5{cXSrenH0bY9vKHSxIGDNXC=> MVOyOFEyOzV2OR?=
H1437 NYXXbW9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7tfpRYPTByIH7N MUiyOEBp MnHpSG1UVw>? NYXmOWZQ\W6qYX7j[ZMhfGinIHPo[Y1we2Wwc3n0bZpifGmxbjD0c{BRVVh? MXeyOFEyOzV2OR?=
H1993 NFPEVopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXEOVAxKG6P NHznXGIzPCCq NFT3fW5FVVOR M3juXoVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:gVG1Z NWfN[2ZZOjRzMUO1OFk>
H1299 NYPubZF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPHOVAxKG6P NWDYbVNROjRiaB?= M3G1VmROW09? M1HYcYVvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:gVG1Z MV:yOFEyOzV2OR?=
AsPC-1 NHn2b5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nPUFExNTFyMECgcm0> MVSyOE01QGh? M4TkV4VvcGGwY3XzJJRp\SClaHXtc5NmdnOrdHn6ZZRqd25idH:g[4Vu[2m2YXLpcoU> M{fmS|I{QDB2NEKy
MiaPaCa-2 M2XHSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;RZnIxOTBvMUCwNEBvVQ>? MU[yOE01QGh? MmnZ[Y5p[W6lZYOgeIhmKGOqZX3vd4Vve2m2aYrheIlwdiC2bzDn[Y1kcXSjYnnu[S=> MknVNlM5ODR2MkK=
BxPC-3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW4NVAuOTByMDDuUS=> M4\SeFI1NTR6aB?= NF20OmJmdmijbnPld{B1cGViY3jlcY9{\W6|aYTpfoF1cW:wIITvJIdmdWOrdHHibY5m M2Xp[VI{QDB2NEKy
SKOV3 NU[0To4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV23[2k4OC5|INM1US=> NFPWOpY5KGR? M{\oe5NmdnOrdHn6[ZMhfGinIHPlcIwhdGmwZYOgeI8h\2WvY3n0ZYJqdmYEoB?= Mn25NlM2PDh{Nkm=
OVCAR-8 NEPGfG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljnNE4{KML3TR?= NELwZmQ5KGR? Mnfzd4Vve2m2aYrld{B1cGViY3XscEBtcW6nczD0c{Bo\W2laYThZolv\cLi NIXk[pgzOzV2OEK2PS=>
MV-4-11 MVvBdI9xfG:|aYOgRZN{[Xl? MWOxNFAuPzByIH7N MoPuOFghcA>? MX\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MUiyN|U{Pjd{MR?=
U937 M2riOWFxd3C2b4Ppd{BCe3OjeR?= M2\6flExOC15MECgcm0> M4rKU|Q5KGh? NXe4cmtFcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M1;yfVI{PTN4N{Kx
MOLM-13  NIDlPVRCeG:ydH;zbZMhSXO|YYm= MoKxNVAxNTdyMDDuUS=> M4TQO|Q5KGh? NVH3WZNkcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NHH2cmszOzV|NkeyNS=>
A2058  MlnBR4VtdCCYaXHibYxqfHliQYPzZZk> NVPUfXRQOzdwNT2zNFAhdk1? MXe3NkBp MmPtSG1UVw>? M3vM[5Jm\HWlZYOgeIhmKE2NLUG3O|UhTUN3MNMgZpkhPS2ob3zkJJRwKGGwIHH2[ZJi\2Vib3[gOFUhdk1? NGf4cnIzOzF2OE[4OC=>
H2009 M3nrVmNmdGxiVnnhZoltcXS7IFHzd4F6 NYG3SJB{PTByIH7N NEOzZpo4OiCq MnPSSG1UVw>? NXX5fnRoemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? M2\XO|I{OTR6Nki0
Su.86.86 NHz5VY5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYDQcW1RPTByIH7N NXW4XZZ1PzJiaB?= NWDaT3d6TE2VTx?= MXny[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> NXfkUGQ{OjNzNEi2PFQ>
HRE MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{nVflUxOCCwTR?= NUHwWWprPzJiaB?= MlThSG1UVw>? MYny[ZN2dHS|IHnuJGcyN1NvcHjhd4Uh[WOldX31cIF1cW:wIHPvcYJqdmWmIIfpeIghVUtvMUe3OS=> NHnh[YgzOzF2OE[4OC=>
HMEC NGDk[2hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHHFfIE2ODBibl2= M4GxRVczKGh? NFXrNG1FVVOR NVLaNJpqemW|dXz0d{BqdiCJMT;TMZBp[XOnIHHjZ5VufWyjdHnvckBkd22kaX7l[EB4cXSqIF3LMVE4PzV? M1;PNlI{OTR6Nki0
U2OS  MUHGeY5kfGmxbjDBd5NigQ>? M2jQUVIhyrWP M1jOeFAuOjRiaB?= MUfpcoR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIsyKGG2IIPldolv\SB|NEWgZZQh[m:2aDDjc45k\W62cnH0bY9veyCjczDlZZJtgSCjczCyJIgh[W[2ZYKgZYRucW6rc4TyZZRqd25? M3rwRlIzQTN5MUS3
U2OS  NV;hcHplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMVExKML3TR?= MnvqNlQwPDhiaB?= MWjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MYOyNlk{PzF2Nx?=
U937 NHLNOVdHfW6ldHnvckBCe3OjeR?= Mo[xNVAxNTVyMDDuUS=> NXqzXIs2PCCqwrC= Mojj[IVkemWjc3XzJJRp\SCleYThdoFjcW6nLXnu[JVk\WRiQ3jrNUBifXSxcHjvd5Bpd3K7bHH0bY9vKGG2IGPldlI6PsLiYX7kJJBz\X[nboTzJGNl[zJ3QTDkc5dvemWpdXzheIlwdg>? M2fuNFIzQDZ7OE[5
U937 M1e0TGZ2dmO2aX;uJGF{e2G7 M3zWR|ExOCCwTR?= NX;hbGZFPCCqwrC= NF7k[Hlz\X[ncoPld{B1cGViY4n0ZZJi[mmwZT3pcoR2[2WmIHnubIljcXSrb36gc4bDqDOKLYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGmwdH:gSG5C M2e1UFIzQDZ7OE[5
U937 MUHGeY5kfGmxbjDBd5NigQ>? NGPXTnYyODBvNUCwJI5O M2fzTlQhcMLi NFvjNJBqdmS3Y3XzJIlv[3KnYYPl[EBxcG:|cHjvdplt[XSrb36gc4YhUDKDWB?= NULSTWJkOjJ6Nkm4Olk>
HL-60 MkW0RZBweHSxc3nzJGF{e2G7 NFTO[Ww{OC9zMECvN|AxKG6P MVeyOEBp NIPiOplFVVOR M4LLfIVvcGGwY3XzJIN6fGG{YXLpcoUucW6mdXPl[EBieG:ydH;zbZM> NFrUSG4zOjh4OUi2PS=>
ML-1 MV\BdI9xfG:|aYOgRZN{[Xl? NUDqOXJrOjVxNUCvNVAxKG6P MlLUNlQhcA>? Mn[1SG1UVw>? MYflcohidmOnczDjfZRiemGkaX7lMYlv\HWlZXSgZZBweHSxc3nz MmPCNlI5Pjl6Nkm=
HCT116 MnrxSpVv[3Srb36gRZN{[Xl? NEjyRoIyKML3TR?= MViyOEBp Mlj2ZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB? NXPRfWFrOjJ3MUC1OlA>
U2OS M2W3NWZ2dmO2aX;uJGF{e2G7 NXTnR3ZIOSEEtV2= NEPOTlAzPCCq MlLYZYJzd2ejdHXzJI9nKGOnbHygZ5lkdGViYYLy[ZN1yqB? Mni0NlI2OTB3NkC=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-chk1(ser345) / CDC25A ; 

PubMed: 27690219     


Western blots for H1299 and A549 cells treated with MK-8776 for various times and assessed for expression of p-chk1 (ser345) and CDC25A.

Cyclin E / pY15-CDK / γH2AX ; 

PubMed: 26595527     


The indicated cell lines were incubated with 2 μM of each drug for 6 h, then lysed and analyzed by western blotting. The top row reflects cells sensitive to MK-8776. The second row reflects cells that are also sensitive to MK-8776, but which fail to degrade cyclin E. The third row reflects MK-8776-resistant cell lines.

27690219 26595527
体内研究 相对于gemcitabine或SCH 900776单独给药,Gemcitabine给药30分钟后,4 mg/kg SCH 900776足以诱导γ-H2AX生物标志物,而8 mg/kg增强肿瘤药效动力学和退化响应。递增剂量的SCH 900776 (16 mg/kg和32 mg/kg)诱导肿瘤响应持续改进。重要的是,在BALB/c 小鼠体内,SCH 900776的剂量与强的生物标志物活化相关,而提高的肿瘤响应与gemcitabine对血液学指标增强的毒性无关。[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)

动物实验:[1]
- 合并
  • Animal Models: 皮下注射A2780 或 MiaPaCa2细胞的额雌性裸鼠
  • Dosages: ~50 mg/kg
  • Administration: 腹腔内注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 3 mg/mL (7.97 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% propylene glycol
5 mg/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 376.25
化学式

C15H18BrN7

CAS号 891494-63-6
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00779584 Completed Drug: MK-8776|Drug: Gemcitabine Hodgkin Disease|Lymphoma Non-Hodgkin|Neoplasms Merck Sharp & Dohme Corp. October 17 2008 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

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:

    I would like to know whether your product S2735 is the optically pure R enantiomer or whether it is a racemic mix.

  • 回答:

    Our S2735 MK-8776 (SCH 900776) is R enantiomer.

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

相关Chk产品

Tags: 购买MK-8776 (SCH 900776) | MK-8776 (SCH 900776)供应商 | 采购MK-8776 (SCH 900776) | MK-8776 (SCH 900776)价格 | MK-8776 (SCH 900776)生产 | 订购MK-8776 (SCH 900776) | MK-8776 (SCH 900776)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID