SCH772984 是一种高度选择性和 ATP 竞争性的 ERK 抑制剂,对 ERK1 和 ERK2 的 IC50 值分别为 4 nM 和 1 nM。它在含有 BRAF 或 RAS 突变的 MAPK 抑制剂天真和 MAPK 抑制剂耐药细胞中具有抗肿瘤活性。
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | ERK ↓ ↑ | ERK1 ↓ ↑ | ERK2 ↓ ↑ | ERK5 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
DEL-22379 |
+
ERK, IC50: 0.5 μM |
+
ERK, IC50: 0.5 μM |
98% | ||||||||||||||||
Pluripotin |
++
ERK1, Kd: 98 nM |
RasGAP | 99%+ | ||||||||||||||||
FR 180204 |
+
ERK1, Ki: 0.31 μM |
++
ERK2, Ki: 0.14 μM |
99%+ | ||||||||||||||||
Ravoxertinib |
+++
ERK1, IC50: 1.1 nM |
++++
ERK2, IC50: 0.3 nM |
99%+ | ||||||||||||||||
SCH772984 |
+++
ERK1, IC50: 4 nM |
++++
ERK2, IC50: 1 nM |
99%+ | ||||||||||||||||
Temuterkib |
+++
ERK1, IC50: 5 nM |
+++
ERK2, IC50: 5 nM |
99%+ | ||||||||||||||||
VX-11e |
+++
ERK2, Ki: <2 nM |
99%+ | |||||||||||||||||
Ulixertinib |
++++
ERK2, IC50: <0.3 nM |
99%+ | |||||||||||||||||
XMD17-109 |
++
ERK5, IC50: 162 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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 BRAFV600E-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] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
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 | ||
Dose | Mice: 12.5 mg/kg - 25 mg/kg[1] (i.p., twice daily) |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.70mL 0.34mL 0.17mL |
8.51mL 1.70mL 0.85mL |
17.02mL 3.40mL 1.70mL |
CAS号 | 942183-80-4 |
分子式 | C33H33N9O2 |
分子量 | 587.674 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(85.08 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 5% DMSO+water 0.4 mg/mL clear PO 0.5% CMC-Na 60 mg/mL suspension |