2. MAPK/ERK Pathway Stem Cell/Wnt
  3. MEK ERK
  4. IK-595

IK-595 是一种高亲和力（7.39 nM）的 MEK1/MEK2 抑制剂。IK-595 能阻断 EGF 诱导的 AsPC-1 细胞中 ERK1/2 的磷酸化 IC50 值为 0.1 nM。IK-595 具有口服活性，并能穿透血脑屏障。IK-595 可用于 Ras/MAPK 通路异常癌症的研究。

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IK-595

IK-595 Chemical Structure

CAS No. : 3018909-73-1

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IK-595 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers[1].

体外研究
(In Vitro)

IK-595（3 nM；4 h）可增强 HCT-116 细胞中 MEK 与 CRAF 的相互作用并促进 HT-29、NCI-H1755 和 NCI-H1666 细胞中 MEK 与 BRAFV600E、II 类和 III 类突变体的相互作用[1]。
IK-595 (25 nM；长期监测) 联合 sotorasib (62.5 nM) 可在 NCI-H358 细胞中维持对细胞活力的抑制作用超过 30 天 [1]。
IK-595 (3 nM；120 h) 联合 sotorasib (1000 nM) 在 NCI-H358 细胞中诱导的细胞凋亡水平高于其他 MEK 抑制剂组合 。IK-595 (10 nM；120 h) 联合 RMC-7977 (1 nM) 可增强 NCI-H358 细胞的凋亡[1]。
IK-595 (3 nM；长期监测) 联合 sotorasib (250 nM) 可阻断索托拉西布耐药型 NCI-H358-R 细胞的生长。IK-595 可抑制索托拉西布耐药型 NCI-H358-R 细胞中的 ERK1/2 的磷酸化 [1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IK-595 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI-H2122, AsPC-1, 5637
Concentration: 10 nM
Incubation Time: up to 96 h
Result: Inhibited ERK1/2 phosphorylation for as long as 96 h in NCI-H2122 and AsPC-1 cells; recovery occurred after 48 h in 5637 cells, delayed relative to reference compounds.
体内研究
(In Vivo)

IK-595 (6 mg/kg；灌胃；隔日一次) 在异种移植小鼠模型中表现出抗肿瘤活性 [1]。
IK-595 (6 mg/kg；灌胃；单剂量) 在颅内和皮下接种 A549 肿瘤的小鼠中表现出更优异的脑部药效学活性 [1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (female)[1]
Dosage: 6 mg/kg
Administration: p.o.; single dose
Result: Significantly reduced DUSP6 mRNA expression in intracranial tumors compared to trametinib, avutometinib, and selumetinib; Reduced DUSP6 mRNA expression in subcutaneous tumors compared to avutometinib and selumetinib.
Animal Model: Rag2/Il2rg-knockout (female) [1]
Dosage: 0.3 mg/kg
Administration: p.o.; QOD
Result: Demonstrated superior antitumor activity (TGI = 89.27%) compared to trametinib; Maintained more substantial inhibition of tumor ERK1/2 phosphorylation at 4 and 24 hours post-treatment and stronger inhibition of tumor DUSP6 mRNA expression compared to trametinib.
分子量

675.90

Formula

C24H24ClFIN5O5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

IK-595 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IK-5953018909-73-1IK595IK 595MEKERKMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesCRAFERK1/2MEK1pancreatic ductal adenocarcinomaARAFKRAS-G12CMEK2non-small cell lung cancerMAPK pathwayBRAFInhibitorinhibitorinhibit

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HY-181067
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