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CAS No.: 942183-80-4

SCH772984 Catalog No. CSN13643

Synonyms: SCH772984

SCH772984 is a specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ERK1

IC50:4nM ERK2

IC50:1nM
描述ERK1/2 (extracellular-signal-regulated kinases) is only known substrates of the MEK1/2 as well as the essential node in RAS/RAF/MEK/ERK signaling cascade, which can be activated by catalyzing the phosphorylation on T202/Y204 through MEK1/2. SCH772984 is a specific and potent ERK1/2 inhibitor with IC50 value of 4 and 1 nM (measured by in vitro kinase activity). Exposure to SCH772984 at concentration ranging in 30-300nM dose-dependently inhibited the phosphorylation of ERK substrate, p90 ribosomal S6 kinase (RSK), on T359/S363 site, as well as caused the inhibition of phosphorylation of residues in the activation loop of ERK itself at the higher dose (>100 nM). This was further confirmed by comparison with the ATP-competitive ERK inhibitor, VTX-11e. Though both of this two inhibitor inhibited p-RSK at concentration ranging in 0.1-2 μM in BRAF^V600E-mutant A375 melanoma cell line, only SCH772984 showed suppression on p-ERK. The cell growth assay studies showed that SCH772984 was efficacious on growth inhibition of RAS- or BRAF- mutant cancer cells, as well as in cells resistant to single-agent BRAF or MEK inhibitor tested. Consistent with this cellular results, intraperitoneal injection with SCH772984 at dose of 12.5, 25 and 50 mg/kg, twice daily for 14 days, efficiently suppressed tumor growth, with obvious p-ERK inhibition, in human LOX BRAF-mutant melanoma xenograft model, while suppression of MiaPaCa KRAS-mutant pancreatic tumor growth can be observed at dose of both 25 and 50 mg/kg in nude mice^[1].
作用机制SCH772984 may inhibit ERK1/2 both through ATP-competition and inducing or stabilizing a conformational state in ERK that prevents activation by MEK.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
2P-ERK2	-	Growth Inhibition Assay	-	IC50=0.24 nM	25350931
5637	-	Growth Inhibition Assay	-	IC50=610 nM	23614898
769P	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898

更多
动物研究
剂量
Mice: 12.5 mg/kg - 25 mg/kg^[1] (i.p., twice daily)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 12.5 mg/kg - 25 mg/kg^[1] (i.p., twice daily)
给药途径	i.p.

[1] Morris EJ, Jha S, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7016 mL
- 8.5082 mL
- 17.0164 mL
- 5 mM
- 0.3403 mL
- 1.7016 mL
- 3.4033 mL
- 10 mM
- 0.1702 mL
- 0.8508 mL
- 1.7016 mL

技术信息

CAS号

942183-80-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H33N9O2

运输

蓝冰

分子量

587.67

别名

SCH772984

溶解度

DMSO	7.0 mg/mL (11.9 mM) warming
Water	insoluble

动物实验配方

IP	5% DMSO+water	0.4 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

2P-ERK2	-	Growth Inhibition Assay	-	IC50=0.24 nM	25350931
5637	-	Growth Inhibition Assay	-	IC50=610 nM	23614898
769P	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
786-O	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
8505C	-	Growth Inhibition Assay	-	IC50=50 nM	23614898
A172	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
A204	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
A2058	-	Growth Inhibition Assay	-	IC50=360 nM	23614898
A2780	-	Growth Inhibition Assay	-	IC50=143 nM	23614898
A375-SM	-	Growth Inhibition Assay	-	IC50=75 nM	23614898
A427	-	Growth Inhibition Assay	-	IC50=1433 nM	23614898
A498	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
A549	-	Growth Inhibition Assay	-	IC50=326 nM	23614898
A673	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
ACHN	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
AsPc-1	-	Growth Inhibition Assay	-	IC50=270 nM	23614898
BHT-101	-	Growth Inhibition Assay	-	IC50=300 nM	23614898
BT-474	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
Caki-1	-	Growth Inhibition Assay	-	IC50=450 nM	23614898
CAPAN-1	-	Growth Inhibition Assay	-	IC50=104 nM	23614898
CFPAC-1	-	Growth Inhibition Assay	-	IC50=1001 nM	23614898
CHL-1	-	Growth Inhibition Assay	-	IC50=1460 nM	23614898
Colo-205	-	Growth Inhibition Assay	-	IC50=36 nM	23614898
DAOY	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
Daudi	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
DBTRG-05MG	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
DLD-1	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
DU145	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
EKVX	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
ES-2	-	Growth Inhibition Assay	-	IC50=2659 nM	23614898
FTC-133	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
H226	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
H23	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
H322	-	Growth Inhibition Assay	-	IC50=325 nM	23614898
H522	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
H716	-	Growth Inhibition Assay	-	IC50=334 nM	23614898
HCT-116	-	Growth Inhibition Assay	-	IC50=128 nM	23614898
HCT-15	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
HCT-8	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
HeLa	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
HL-60	-	Growth Inhibition Assay	-	IC50=30 nM	23614898
HOP62	-	Growth Inhibition Assay	-	IC50=676 nM	23614898
HOP92	-	Growth Inhibition Assay	-	IC50=820 nM	23614898
HPAC	-	Growth Inhibition Assay	-	IC50=170 nM	23614898
Hs-294T	-	Growth Inhibition Assay	-	IC50=945 nM	23614898
Hs-695T	-	Growth Inhibition Assay	-	IC50=165 nM	23614898
HS746T	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
HT-1197	-	Growth Inhibition Assay	-	IC50=316 nM	23614898
HT-1376	-	Growth Inhibition Assay	-	IC50=2800 nM	23614898
HT-144	-	Growth Inhibition Assay	-	IC50=60 nM	23614898
HT-29	-	Growth Inhibition Assay	-	IC50=50 nM	23614898
HTB-177	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
IGROV-1	-	Growth Inhibition Assay	-	IC50=146 nM	23614898
J-82	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
Jijoye	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
Jurkat	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
K1	-	Growth Inhibition Assay	-	IC50=130 nM	23614898
K562	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
KG-1	-	Growth Inhibition Assay	-	IC50=900 nM	23614898
Ln Cap	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
LoVo	-	Growth Inhibition Assay	-	IC50=47 nM	23614898
LOX	-	Growth Inhibition Assay	-	IC50=100 nM	23614898
M14	-	Growth Inhibition Assay	-	IC50=47 nM	23614898
MB-231	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
MB-453	-	Growth Inhibition Assay	-	IC50=672 nM	23614898
MB-468	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
MCF-7	-	Growth Inhibition Assay	-	IC50=1001 nM	23614898
MDAH-2774	-	Growth Inhibition Assay	-	IC50=2657 nM	23614898
MiaPaCa	-	Growth Inhibition Assay	-	IC50=53 nM	23614898
Molt-3	-	Growth Inhibition Assay	-	IC50=600 nM	23614898
Molt-4	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
N-87	-	Growth Inhibition Assay	-	IC50=307 nM	23614898
NCI-H157	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
NCI-H292	-	Growth Inhibition Assay	-	IC50=90 nM	23614898
NCI-H520	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
OVCAR-5	-	Growth Inhibition Assay	-	IC50=208 nM	23614898
PA-1	-	Growth Inhibition Assay	-	IC50=1001 nM	23614898
Panc-1	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
PC3	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
RD	-	Growth Inhibition Assay	-	IC50=123 nM	23614898
Ro82-W-1	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
RPMI-7951	-	Growth Inhibition Assay	-	IC50=344 nM	23614898
RT-4	-	Growth Inhibition Assay	-	IC50=810 nM	23614898
SCABER	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
SF-268	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
SF-295	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
SF-539	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
SJCRH30	-	Growth Inhibition Assay	-	IC50=2002 nM	23614898
SK-Hep-1	-	Growth Inhibition Assay	-	IC50=1422 nM	23614898
SK-Mel-1	-	Growth Inhibition Assay	-	IC50=37 nM	23614898
SK-Mel-2	-	Growth Inhibition Assay	-	IC50=34 nM	23614898
SK-Mel-28	-	Growth Inhibition Assay	-	IC50=85 nM	23614898
SK-Mel-3	-	Growth Inhibition Assay	-	IC50=118 nM	23614898
SK-Mel-5	-	Growth Inhibition Assay	-	IC50=66 nM	23614898
SK-N-SH	-	Growth Inhibition Assay	-	IC50=150 nM	23614898
SK-OV-3	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
SNB-19	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
SNB-75	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
SNU-1	-	Growth Inhibition Assay	-	IC50=354 nM	23614898
SNU-16	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
SU.86.86	-	Growth Inhibition Assay	-	IC50=1001 nM	23614898
SW-480	-	Growth Inhibition Assay	-	IC50=165 nM	23614898
SW-527	-	Growth Inhibition Assay	-	IC50=121 nM	23614898
SW-620	-	Growth Inhibition Assay	-	IC50=104 nM	23614898
SW-626	-	Growth Inhibition Assay	-	IC50=33 nM	23614898
TCC-SUP	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
TT	-	Growth Inhibition Assay	-	IC50=406 nM	23614898
U-251	-	Growth Inhibition Assay	-	IC50=1000 nM	23614898
U373-MG	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
U87MG	-	Growth Inhibition Assay	-	IC50=2000 nM	23614898
U-937	-	Growth Inhibition Assay	-	IC50=3000 nM	23614898
UACC-62	-	Growth Inhibition Assay	-	IC50=30 nM	23614898
UM-UC-3	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898
WiDr	-	Growth Inhibition Assay	-	IC50=39 nM	23614898
WM-266-4	-	Growth Inhibition Assay	-	IC50=20 nM	23614898
ZR-75-1	-	Growth Inhibition Assay	-	IC50=3001 nM	23614898

靶点	Description	IC50
ERK1		IC50:4nM
ERK2		IC50:1nM

SCH772984 Catalog No. CSN13643

靶点选择性

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