LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.
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产品名称 | A-raf ↓ ↑ | B-Raf ↓ ↑ | C-Raf/Raf-1 ↓ ↑ | Raf ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Encorafenib | ✔ | 99%+ | |||||||||||||||||
GDC-0879 |
++++
B-Raf, IC50: 0.13 nM |
99%+ | |||||||||||||||||
SB-590885 |
++++
B-Raf, Ki: 0.16 nM |
99%+ | |||||||||||||||||
RAF265 | 99%+ | ||||||||||||||||||
Dabrafenib |
++++
B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM |
+++
C-Raf, IC50: 6.3 nM |
98% | ||||||||||||||||
Lifirafenib |
++++
WT A-RAF, IC50: 1 nM |
++
BRAF WT, IC50: 32 nM BRAF(V600E), IC50: 23 nM |
+++
C-RAF (Y340/341D), IC50: 7 nM |
EGFR | 98% | ||||||||||||||
ZM 336372 |
+
C-Raf, IC50: 70 nM |
99%+ | |||||||||||||||||
NVP-BHG 712 |
+
C-Raf, IC50: 0.395 μM |
99%+ | |||||||||||||||||
CCT196969 |
+
BRAF, IC50: 0.1 μM |
++
CRAF, IC50: 0.01 μM |
Src | 98% | |||||||||||||||
Vemurafenib |
++
B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM |
+
C-Raf, IC50: 48 nM |
98+% | ||||||||||||||||
PLX4720 |
++
B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM |
+++
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM |
BRK | 99+% | |||||||||||||||
GW 5074 |
+++
C-Raf, IC50: 9 nM |
99%+ | |||||||||||||||||
Avutometinib |
+++
BRAF, IC50: 19 nM BRAF V600E, IC50: 8.2 nM |
+
CRAF, IC50: 56 nM |
98% | ||||||||||||||||
LY3009120 |
++++
BRAF WT, IC50: 15 nM BRAF(V600E), IC50: 5.8 nM |
++++
C-Raf, IC50: 4.3 nM |
99%+ | ||||||||||||||||
Agerafenib |
++
B-Raf, Kd: 36 nM B-Raf (V600E), Kd: 14 nM |
+
C-Raf, Kd: 39 nM |
RET | 99%+ | |||||||||||||||
TAK-632 |
+++
B-Raf, IC50: 8.3 nM |
++++
C-Raf, IC50: 1.4 nM |
99%+ | ||||||||||||||||
AZ 628 |
+
B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM |
++
C-Raf-1, IC50: 29 nM |
99% | ||||||||||||||||
PLX7904 | ✔ | 98+% | |||||||||||||||||
Sorafenib |
++
B-Raf (V599E), IC50: 38 nM B-Raf, IC50: 22 nM |
++++
Raf-1, IC50: 6 nM |
++++
Raf-1, IC50: 6 nM |
99% | |||||||||||||||
Tovorafenib | ✔ | 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。 |
描述 | LJH685 is a strong, ATP-competitive, and selective inhibitor of RSK (ribosomal S6 kinase), effectively inhibiting the biochemical activities of RSK1, RSK2, and RSK3 with IC50 values of 6, 5, and 4 nM, respectively[1]. |
体外研究 | When applied in concentrations ranging from 0.01 to 100 μM over 72 hours, LJH685 significantly curtails the proliferation of MDA-MB-231 and H358 cells within a soft agar environment, displaying EC50 values of 0.73 and 0.79 μM, correspondingly[1]. Moreover, LJH685 (0.1-10 μM; 4 hours) substantially diminishes phosphorylation of YB1 at submicromolar levels, achieving almost complete suppression at elevated concentrations[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.62mL 0.52mL 0.26mL |
13.11mL 2.62mL 1.31mL |
26.22mL 5.24mL 2.62mL |
CAS号 | 1627710-50-2 |
分子式 | C22H21F2N3O |
分子量 | 381.418 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 30 mg/mL(78.65 mM),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 |