SCH772984

For research use only. Not for use in humans.

目录号:S7101

SCH772984 Chemical Structure

CAS No. 942183-80-4

SCH772984是一种新型特异性的ERK1/2抑制剂,无细胞试验中IC50分别为4 nM和1 nM, 对含有RAS或BRAF突变的癌细胞具有强大的功效。

规格 价格 库存 购买数量  
RMB 2210.07 现货
RMB 11220.78 现货
RMB 44799.48 现货
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客户使用Selleck生产的SCH772984发表文献320篇:

产品安全说明书

ERK抑制剂选择性比较

生物活性

产品描述 SCH772984是一种新型特异性的ERK1/2抑制剂,无细胞试验中IC50分别为4 nM和1 nM, 对含有RAS或BRAF突变的癌细胞具有强大的功效。
特性 SCH772984不直接抑制MEK1, MEK2, BRAF, 或 CRAF酶活性。
靶点
ERK2 [1]
(Cell-free assay)
ERK1 [1]
(Cell-free assay)
1 nM 4 nM
体外研究

SCH772984是新型,选择性,ATP竞争性的ERK1/2抑制剂。SCH772984抑制ERK底物p90核糖体S6激酶(T359/S363 磷酸化-RSK)的磷酸化,这种作用存在剂量依赖性。SCH772984也能抑制ERK自身活化环中残基的磷酸化。SCH772984分别抑制约88%和49%BRAF突变型或RAS-突变型肿瘤细胞系,EC50值<500 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
2P-ERK2 NVf4NWFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX1WVk4UUN3ME2wMlI1KG6P M2m3PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WwPVMyLz5{NUO1NFk{OTxxYU6=
WM-266-4 NGX3PIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJyIH7N MkLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
UACC-62 M1LRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP6TWM2OD1|MDDuUS=> M334TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
Colo-205 M{XPb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3oTWM2OD1|NjDuUS=> M4XIN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SK-Mel-1 NEfDd3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XQemlEPTB;M{egcm0> NFjlOWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
WiDr Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGyTWM2OD1|OTDuUS=> NXf6O5h[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
M14 NX3uNVJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjuR2xKSzVyPUS3JI5O MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HT-29 M3zDNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTFOJFJUUN3ME21NEBvVQ>? M3XhVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
8505C MoDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnGV|ZKSzVyPUWwJI5O MoLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
HT-144 Moe4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7uZ5JXUUN3ME22NEBvVQ>? NGDZRYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
SK-Mel-5 NYnpNZdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KzZWlEPTB;Nk[gcm0> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
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CAPAN-1 NXnMVG43T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVraUIZ6UUN3ME2xNFQhdk1? M170VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
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AsPc-1 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni2TWM2OD1{N{Cgcm0> M33B[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
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MB-231 M1HnbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILmfGVKSzVyPUGwNFAhdk1? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SU.86.86 NGDPTYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHuTWM2OD1zMECxJI5O MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
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A375 Mn\DSpVv[3Srb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKEWUS{KgbY4hcHWvYX6gRVM4PSClZXzsd{Bp[XKkb4LpcochSlKDRjDWOlAxTSCvdYThcpQh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1\WRiRWLLNkBt\X[nbIOsJGlEPTBiPTCwMlAxPCEQvF2u M33O[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|A3Lz5{OEO3OlMxPjxxYU6=
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A375 M2LEOmZ2dmO2aX;uJIF{e2G7 MXOyJIhzew>? MY\Jcohq[mm2aX;uJI9nKEWUS{GvNkBqdiCqdX3hckBCOzd3IHPlcIx{KGijcnLvdolv\yCELWLBSkBXPjByRTDteZRidnRiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4heGixc4Doc{1TW0tibHX2[Ywh[W[2ZYKgNkBpenNiYomgR4VtdG:vaXPzJGFzemG7U3PhcnROKF[WSTDpcYFocW6pIHHuZYx6e2m|LDDJR|UxKD1iMD6wNkDPxE1w NUiydlJiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|c6QDFpPkK1PVc4QThzPD;hQi=>
A375 MXXGeY5kfGmxbjDhd5NigQ>? NYPvcndvOiCqcoO= NX\xVnRCUW6qaXLpeIlwdiCxZjDFVmsyNzJiaX6gbJVu[W5iQUO3OUBk\WyuczDoZZJjd3KrbnegRk1TSUZiVk[wNGUhdXW2YX70JIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIDoc5NxcG9vUmPLJIxmfmWuIHHmeIVzKDJiaILzJIJ6KEOnbHzvcYlkeyCDcoLhfXNk[W6WTTDWWGkhcW2jZ3nu[{BidmGueYPpd{whUUN3MDC9JFAvODJizszNMi=> M4\jXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O|k5OTxxYU6=
A375 MX3GeY5kfGmxbjDhd5NigQ>? MnzBTY5pcWKrdHnvckBw\iCHUluyJIlvKGi3bXHuJGE{PzViY3XscJMhcGG{Yn;ybY5oKEKUQV[gWlYxOEVibYX0ZY51KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJJBpd3OyaH;yfYxifGWmIGLTT{Bt\X[nbIOsJGlEPTBiPTCwMlAzKM7:TT6= M4Ts[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|A3Lz5{OEO3OlMxPjxxYU6=
HT-29 MnTMRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MWO0JIRigXN? NVfVbGoxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bp[XKkb4LpcochSlKDRjDWOlAxTS:GIH31eIFvfCCvZXHzeZJm\CCjZoTldkA1KGSjeYOsJGlEPTBiPTCwMlA2QSEQvF2u NV25OGw2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|Q3OTVpPkOwNFM1PjF3PD;hQi=>
HT-29 M1vHNmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M2nXT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgbIFz[m:{aX7nJGJTSUZxS2LBV{BufXSjboSsJGlEPTBiPTCwMlA2QSEQvF2u MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd2OEC1NUc,Ojl5NEiwOVE9N2F-
A375 M{DvV2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MlvGO|IhcHK| NHjUdo5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgbIFz[m:{aX7nJGIuWkGIIG[2NFBGKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdG:vaXPzJGFzemG7U3PhcnROKF[WSTDpcYFocW6pIHHuZYx6e2m|LDDJR|UxKD1iMD6wO{DPxE1w MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl5N{m4NUc,OjV7N{e5PFE9N2F-
HT-29 MY\BdI9xfG:|aYOgZZN{[Xl? MWPJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiWLUK5JINmdGy|IHjhdoJwemmwZzDCVmFHN0uUQWOgcZV1[W62IHL5JINie3Cjc3WgZYN1cX[jdHnvckBie3OjeTygTWM2OCB;IECuNFk3KM7:TT6= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd2OEC1NUc,Ojl5NEiwOVE9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cyclin B1 / cyclin D1 / p21; 

PubMed: 26725216     


Cells treated as above were collected for western blot for total cyclin B1, cyclin D1 and p21, and of phosphorylated, inactivated RB (S807/811; pRB). Western blot for pERK was done to verify SCH772984 inhibition; β-actin was the loading control.

pRSK / pERK / pAKT / pMEK; 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984, then evaluated by western blot with phospho-specific antibodies for RSK (T395/S363; pRSK), MEK1/2 (S217/221; pMEK), AKT (S473; pAKT), and ERK (T202/Y204; pERK). Total RSK, ERK, AKT, MEK and β-actin were also analyzed. Data are representative of three independent experiments.

DUSP1 / DUSP4 / DUSP6; 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984 for 72 hr and evaluated by western blot for DUSP1, DUSP4, DUSP6 and β-actin.

pCRAF(S338, S289, S296, S301); 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984 for 72 hr and evaluated by western blot for pCRAF (S338), pCRAF (S289/296/301), total CRAF and β-actin.

Aurora B / ETS1 / ETS2; 

PubMed: 26725216     


Cells were treated with vehicle or SCH772984 for 7 days, then immunoblotted for Aurora B, MYC, ETS1 or ETS2, and β-actin. Data are representative of three independent experiments.

26725216
Growth inhibition assay
Cell viability; 

PubMed: 30118499     


NCI-H747, SW837, SW480, and SW620 cells were treated with the ERK inhibitor SCH772984 at indicated concentrations for 72 hours. Dimethyl sulfoxide (DMSO) (0.01%) was used as the control treatment. Each data point represents the mean of five replicates; error bars indicate one SD.

30118499
Immunofluorescence
TOMM20; 

PubMed: 30833752     


Mitochondrial morphologies of PDAC cells treated with SCH772984 (ERKi, 1 µM) for 24 h. Green, Anti-TOMM20; blue, DAPI; scale bar, 20 μm.

pERK1/2; 

PubMed: 30213106     


After treatment with 10 µM of the ERIK1/2 inhibitors, the expression of p-ERK1/2 protein in HeLa cells was detected using immunofluorescence (400×), bar = 50 μm.

30833752 30213106
体内研究 SCH772984按耐受剂量处理移植瘤模型,诱导肿瘤衰退。SCH772984作用于抗BRAF或MEK抑制剂的模型,有效抑制MAPK信号和细胞增殖。[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]

- 合并

ERK2 IMAP 酶实验:

SCH772984作用于纯化的ERK2或ERK1,按一式两份进行8点稀释曲线。酶添加到实验板中。与化合物温育,然后加入底物肽和ATP溶液中。384孔板中每孔加入14μl稀释的酶(每组反应含0.3ng活性ERK2)。实验板轻轻震荡混合试剂,然后在室温下温育45分钟。加入60μl of IMAP 结合溶液 (IMAP珠在1X结合缓冲液中按1:2200稀释)终止反应。实验板在室温下再温育0.5小时,使磷酸肽与IMAP珠完全结合。然后在 LJL分析仪上读数。
细胞实验:

[1]

- 合并
  • Cell lines: BRAF突变型或 RAS突变型肿瘤系
  • Concentrations: ~10 μM
  • Incubation Time: 5 天
  • Method:

    在96孔板中进行细胞增殖实验,细胞按每孔 4,000个的密度接种。接种24小时后,使用DMSO处理细胞,9点IC50稀释 (0.001-10 μM) ,DMSO终浓度为1%。使用ViaLight发光试剂盒5天后,测定存活力。细胞系存活力检测中,使用SCH772984处理细胞4天,然后进行CellTiterGlo发光细胞活力检测。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 裸鼠
  • Dosages: 12.5 mg/kg, 25 mg/kg, 50 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 14 mg/mL warmed (23.82 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):
5% DMSO+30% PEG 300+ddH2O
0.6mg/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 587.67
化学式

C33H33N9O2

CAS号 942183-80-4
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

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 inhibit Erk1/2 by treating the mice with the inhibitor. by what kind of administration way and at what concentration could it be done?

  • 回答:

    SCH772984 can be administrated by I.P. The dosages can be used as: 12.5 mg/kg, 25 mg/kg, 50 mg/kg. For more detail information please find the paper below: http://cancerdiscovery.aacrjournals.org/content/3/7/742.full

ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID