SCH772984

For research use only. Not for use in humans.

目录号:S7101

SCH772984 Chemical Structure

Molecular Weight(MW): 587.67

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。

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RMB 2210.07 现货
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客户使用Selleck生产的SCH772984发表文献269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 NGHsfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMkSgcm0> MVGyOVM2ODl|MR?=
WM-266-4 MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f2PWlEPTB;MkCgcm0> MYmyN|YyPDh7OB?=
UACC-62 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH6N4JKSzVyPUOwJI5O MX2yN|YyPDh7OB?=
Colo-205 M1;FSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\OW4pKSzVyPUO2JI5O M{XtUVI{PjF2OEm4
SK-Mel-1 NGPXeVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrOVIpKSzVyPUO3JI5O NEXsN28zOzZzNEi5PC=>
WiDr NVHaN5p7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzaN216UUN3ME2zPUBvVQ>? Mlf3NlM3OTR6OUi=
M14 NVP2RldoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3KyT2lEPTB;NEegcm0> NYeyTZA6OjN4MUS4PVg>
HT-29 NFrBZ3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvQSZpDUUN3ME21NEBvVQ>? NX3DfXN1OjN4MUS4PVg>
8505C NY\0NplqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\le4g1UUN3ME21NEBvVQ>? NEDKb4YzOzZzNEi5PC=>
HT-144 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojZTWM2OD14MDDuUS=> MXmyN|YyPDh7OB?=
SK-Mel-5 NE\vZ5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HJcWlEPTB;Nk[gcm0> NGj2eoUzOzZzNEi5PC=>
A375-SM MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\p[GlEPTB;N{Wgcm0> NIrPWZAzOzZzNEi5PC=>
SK-Mel-28 M1jpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TxSWlEPTB;OEWgcm0> NXXWZ5F4OjN4MUS4PVg>
LOX NX7jdJhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MluyTWM2OD1zMECgcm0> NHfHOW8zOzZzNEi5PC=>
SK-Mel-3 NVj0UYFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHaTWM2OD1zMUigcm0> M4Tkc|I{PjF2OEm4
K1 M2K4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLtTWM2OD1zM{Cgcm0> M1jETVI{PjF2OEm4
Hs-695T NYjzR4lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;ETWM2OD1zNkWgcm0> NWTyfnVwOjN4MUS4PVg>
BHT-101 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLCcoN1UUN3ME2zNFAhdk1? MlzLNlM3OTR6OUi=
RPMI-7951 NX\BcIlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\EOnhYUUN3ME2zOFQhdk1? M1HX[lI{PjF2OEm4
A2058 M3r5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe1PJlKSzVyPUO2NEBvVQ>? NEK2XmEzOzZzNEi5PC=>
SK-Hep-1 NEXLZopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF2MkKgcm0> NIjHfmUzOzZzNEi5PC=>
A673 NUPSZ2w4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnrdVIzUUN3ME2zNFAyKG6P MWOyN|YyPDh7OB?=
DBTRG-05MG M4n1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTNyMEGgcm0> MXyyN|YyPDh7OB?=
SW-626 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXNR4RKSzVyPUOzJI5O MYmyN|YyPDh7OB?=
LoVo MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR5IH7N NG\zR|EzOzZzNEi5PC=>
MiaPaCa M{nYSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\ZTWM2OD13MzDuUS=> NYjKSoNbOjN4MUS4PVg>
SW-620 NELzdFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTFyNDDuUS=> NIXRWZQzOzZzNEi5PC=>
CAPAN-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFyNDDuUS=> NVjqcGN[OjN4MUS4PVg>
SW-527 NIPKS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTETWM2OD1zMkGgcm0> NGXZWJEzOzZzNEi5PC=>
HCT-116 M1\N[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnYNFlpUUN3ME2xNlghdk1? Ml\PNlM3OTR6OUi=
SW-480 NY\pbIh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTF4NTDuUS=> MmXlNlM3OTR6OUi=
HPAC NGjj[WtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF5MDDuUS=> M4LVeFI{PjF2OEm4
OVCAR-5 MoHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfqOopKSzVyPUKwPEBvVQ>? NW\qOIpGOjN4MUS4PVg>
AsPc-1 NGTmSZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV2yVZVqUUN3ME2yO|Ahdk1? NV7kd2U2OjN4MUS4PVg>
A549 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHYVVVKSzVyPUOyOkBvVQ>? NGL6NYMzOzZzNEi5PC=>
SNU-1 NVThV3lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHtTWM2OD1|NUSgcm0> NFS0bIgzOzZzNEi5PC=>
HOP62 M1;IO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTZ5NjDuUS=> M3nSXVI{PjF2OEm4
H23 NEjKVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTFyMECgcm0> MVeyN|YyPDh7OB?=
MB-231 M3nkeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrMZWdGUUN3ME2xNFAxKG6P NFzPelEzOzZzNEi5PC=>
SU.86.86 NUTGUml1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTyZ3pnUUN3ME2xNFAyKG6P MoDaNlM3OTR6OUi=
CFPAC-1 NIjVTmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\aTWM2OD1zMECxJI5O NEjye4YzOzZzNEi5PC=>
A427 NGj1RVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3tdGZKSzVyPUG0N|Mhdk1? NVnXSFhmOjN4MUS4PVg>
MDAH-2774 NWnhUoU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P2UmlEPTB;Mk[1O{BvVQ>? MXuyN|YyPDh7OB?=
NCI-H157 M2LFXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jtc2lEPTB;M{CwNEBvVQ>? MUKyN|YyPDh7OB?=
HTB-177 M2\jT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTNyMECgcm0> NYjmbG9UOjN4MUS4PVg>
UM-UC-3 M4fPfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnnd3N2UUN3ME2zNFAyKG6P MmW4NlM3OTR6OUi=
HCT-8 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTNyMEGgcm0> MYWyN|YyPDh7OB?=
Panc-1 MljaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLpN2NQUUN3ME2zNFAyKG6P NX\DXJhMOjN4MUS4PVg>
DLD-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjhWYFoUUN3ME2zNFAyKG6P NYDuVndKOjN4MUS4PVg>
HCT-15 M1HWWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTNyMEGgcm0> M{XYRlI{PjF2OEm4
HL-60 Ml3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPQTWM2OD1|MDDuUS=> Mm\6NlM3OTR6OUi=
SK-Mel-2 MmjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPZTWM2OD1|NDDuUS=> Mn;VNlM3OTR6OUi=
RD M1fQVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DkR2lEPTB;MUKzJI5O MnHBNlM3OTR6OUi=
HT-1197 M{DR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXoTWM2OD1|MU[gcm0> NEe5d3UzOzZzNEi5PC=>
Molt-3 MnTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zmS2lEPTB;NkCwJI5O NHG2NmMzOzZzNEi5PC=>
PA-1 NX3QV3pUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TsR2lEPTB;MUCwNUBvVQ>? M33jZVI{PjF2OEm4
Molt-4 NWLXc4h[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LJSmlEPTB;M{CwNUBvVQ>? NWGyWYtzOjN4MUS4PVg>
NCI-H292 NFftO|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLJ[2Z{UUN3ME25NEBvVQ>? Mn\CNlM3OTR6OUi=
A2780 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLsTWM2OD1zNEOgcm0> M2nnfFI{PjF2OEm4
IGROV-1 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF2NjDuUS=> NF7sU|IzOzZzNEi5PC=>
SK-N-SH MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjVTWM2OD1zNUCgcm0> MkPZNlM3OTR6OUi=
N-87 Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7vNHBKSzVyPUOwO{BvVQ>? Mn\pNlM3OTR6OUi=
H322 M1nwVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTN{NTDuUS=> M4XTcFI{PjF2OEm4
H716 M1j1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTN|NDDuUS=> MVOyN|YyPDh7OB?=
TT M3fEOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHiNoFKSzVyPUSwOkBvVQ>? NFGzO4gzOzZzNEi5PC=>
Caki-1 Ml;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL5SpdRUUN3ME20OVAhdk1? NF7ZUJUzOzZzNEi5PC=>
5637 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrlN|Z3UUN3ME22NVAhdk1? Mk\HNlM3OTR6OUi=
MB-453 M3;XR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnZTWM2OD14N{Kgcm0> NYLyZVE6OjN4MUS4PVg>
RT-4 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIi1[VdKSzVyPUixNEBvVQ>? MnjVNlM3OTR6OUi=
HOP92 NYDhT3JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTh{MDDuUS=> Ml34NlM3OTR6OUi=
KG-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTlyMDDuUS=> MYiyN|YyPDh7OB?=
Hs-294T NHnoc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO4bI1KSzVyPUm0OUBvVQ>? NIG3SlgzOzZzNEi5PC=>
SF-539 NYW3V2V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv2eoVKSzVyPUGwNFAhdk1? MV:yN|YyPDh7OB?=
U-251 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfsTWM2OD1zMECwJI5O M1vwelI{PjF2OEm4
MB-468 NEKyVItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFyMECgcm0> NGXaOYszOzZzNEi5PC=>
HS746T NELwVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HUWmlEPTB;MUCwNEBvVQ>? MoXGNlM3OTR6OUi=
SCABER M3rQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33w[GlEPTB;MUCwNEBvVQ>? M4HGXFI{PjF2OEm4
MCF-7 M4\s[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i5WWlEPTB;MUCwNUBvVQ>? MlnoNlM3OTR6OUi=
CHL-1 MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLwNWhKSzVyPUG0OlAhdk1? MV:yN|YyPDh7OB?=
U87MG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7K[FRKSzVyPUKwNFAhdk1? MonxNlM3OTR6OUi=
SJCRH30 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPNTWM2OD1{MECyJI5O MnzkNlM3OTR6OUi=
ES-2 NIq5PZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn0TWM2OD1{NkW5JI5O NGDpN24zOzZzNEi5PC=>
HT-1376 M1TFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnGTXZKSzVyPUK4NFAhdk1? NWTkWVlmOjN4MUS4PVg>
A172 NWrQdGwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTNyMECgcm0> Mn7hNlM3OTR6OUi=
769P NILEN5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jzd2lEPTB;M{CwNEBvVQ>? NV\qTmcxOjN4MUS4PVg>
NCI-H520 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PySWlEPTB;M{CwNEBvVQ>? MYOyN|YyPDh7OB?=
DU145 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7qOVRKSzVyPUOwNFAhdk1? NXOwUpp{OjN4MUS4PVg>
K562 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfsR5dKSzVyPUOwNFAhdk1? NITzO5ozOzZzNEi5PC=>
U-937 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXBeXpNUUN3ME2zNFAxKG6P MXOyN|YyPDh7OB?=
A204 M4C3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;DTWM2OD1|MECxJI5O M3P6dVI{PjF2OEm4
DAOY MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\adVNKSzVyPUOwNFEhdk1? M3Xpd|I{PjF2OEm4
SF-268 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe0ZmxuUUN3ME2zNFAyKG6P NVzZcYNiOjN4MUS4PVg>
SF-295 NV;Zc2hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHTTWM2OD1|MECxJI5O NULkNXFIOjN4MUS4PVg>
SNB-19 NWnvUIJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPhRWZKSzVyPUOwNFEhdk1? NIW3d5EzOzZzNEi5PC=>
SNB-75 MnrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\1ZmlEPTB;M{CwNUBvVQ>? M3rhTlI{PjF2OEm4
U373-MG MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LSV2lEPTB;M{CwNUBvVQ>? M3TBR|I{PjF2OEm4
786-O MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPldFAyUUN3ME2zNFAyKG6P NFHjOlczOzZzNEi5PC=>
A498 MlnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfQbnlMUUN3ME2zNFAyKG6P MmjtNlM3OTR6OUi=
ACHN Ml7wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjwVFZNUUN3ME2zNFAyKG6P MlzLNlM3OTR6OUi=
EKVX NHm5RmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTNyMEGgcm0> Mn3MNlM3OTR6OUi=
H226 NEm1OlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLhTWM2OD1|MECxJI5O NWfsWllTOjN4MUS4PVg>
H522 NWDncFBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTNyMEGgcm0> MljkNlM3OTR6OUi=
HeLa M1[5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIj3XmhKSzVyPUOwNFEhdk1? NYLreYFlOjN4MUS4PVg>
SK-OV-3 NFnCTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\UTWM2OD1|MECxJI5O M{[zelI{PjF2OEm4
Ln Cap M{K4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTNyMEGgcm0> NE\CUWEzOzZzNEi5PC=>
PC3 NIjXRmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTNyMEGgcm0> NFjtTGkzOzZzNEi5PC=>
SNU-16 M4XYNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDOTWM2OD1|MECxJI5O M2rDUlI{PjF2OEm4
FTC-133 NFe0ZXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTNyMEGgcm0> M13HSlI{PjF2OEm4
Ro82-W-1 Mn3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTNyMEGgcm0> NXXPXYpROjN4MUS4PVg>
Daudi M3:0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPvRXFPUUN3ME2zNFAyKG6P NH;1XIgzOzZzNEi5PC=>
Jijoye M1[0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTs[IpMUUN3ME2zNFAyKG6P MnniNlM3OTR6OUi=
Jurkat MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TqXGlEPTB;M{CwNUBvVQ>? M1Ta[lI{PjF2OEm4
J-82 NWTk[5N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\ueVB{UUN3ME2zNFAyKG6P MYmyN|YyPDh7OB?=
TCC-SUP M1zNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4i4WWlEPTB;M{CwNUBvVQ>? MV6yN|YyPDh7OB?=
BT-474 MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmH0TWM2OD1|MECxJI5O M2HWeFI{PjF2OEm4
ZR-75-1 NF\I[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLUTWM2OD1|MECxJI5O NHjOeWozOzZzNEi5PC=>

... 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
  • Formulation: --
  • 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

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