2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation
  3. Ras ERK Cyclophilin
  4. RM-046

RM-046 是一种口服有效、选择性的 KRASQ61H (活化态) 三元复合物抑制剂。RM-046 可与 cyclophilin A 形成三元复合物，以非共价方式结合活化态 KRASQ61H，通过空间位阻阻断效应因子结合并抑制下游信号传导。RM-046 可抑制 ERK 磷酸化及癌细胞增殖，并在临床前异种移植模型中诱导持久的 RAS 通路信号抑制、抗肿瘤活性及肿瘤消退。RM-046 可用于 KRASQ61H 突变型癌症的研究。

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RM-046

RM-046 Chemical Structure

CAS No. : 3058972-05-4

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RM-046 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

查看所有亚型
K-Ras H-Ras N-Ras Ras

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

查看 Cyclophilin 亚型特异性产品:

查看所有亚型
Cyclophilin A Cyclophilin B Cyclophilin C Cyclophilin D Cyclophilin G Cyclophilin E

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RM-046 is an orally active, selective ternary complex inhibitor of KRASQ61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRASQ61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRASQ61H mutant cancers[1].

IC50 & Target

KRas Q61H

 

分子量

1137.33

Formula

C62H79F3N8O9
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

RM-046 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Help & FAQs
  • 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:

RM-0463058972-05-4RM046RM 046RasERKCyclophilinExtracellular signal regulated kinasesKRAS Q61Hcancer cell proliferationKRAS Q61H mutant cancerswildtype KRAS cancer cellsGTPasecyclophilin Akinomepreclinical xenograft modelsERK phosphorylationRAS pathway signalingInhibitorinhibitorinhibit

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HY-186087
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