2. MAPK/ERK Pathway
  3. Raf
  4. Everafenib

Everafenib 是一种有效且具有血脑屏障透过性的 BRAF 抑制剂，也抑制 MAPK 通路。Everafenib 对一系列 V600EBRAF 黑色素瘤细胞系具有抑制活性，IC50 范围为 2-10 nM，优于 Dabrafenib (HY-14660) 和 Vemurafenib (HY-12057)。Everafenib 能有效提高颅内转移性黑色素瘤小鼠模型的存活天数。

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Everafenib Chemical Structure

Everafenib Chemical Structure

CAS No. : 2923700-82-5

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Everafenib 相关抗体

Top Publications Citing Use of Products

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BRaf c-Raf Raf

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma[1].

IC50 & Target

BRAF, MAPK[1]
体外研究
(In Vitro)

Everafenib (1-10 μM; 1 or 24 h) inhibits MAPK signaling in A375 cells[1].

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

Everafenib 相关抗体:

Western Blot Analysis[1]

Cell Line: A375 (V600EBRAF)
Concentration: 0.01, 0.1, 1 and 10 μM
Incubation Time: 1 or 24 h
Result: Inhibited phospho-ERK1/2 in a dose-dependent manner, also inhibited phospho-MEK1/2.
体内研究
(In Vivo)

Everafenib (50 mg/kg; IP; once daily, for 5 days) increases median survival of melanoma mice from 39 to 50.5 days[1].

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

Animal Model: Female athymic nude mice (intracranially injected with 5×104 A375 melanoma cells)[1]
Dosage: 50 mg/kg
Administration: IP; once daily, for 5 days
Result: Increased median survival from 39 to 50.5 days, and outperformed Dabrafenib (HY-14660).
分子量

484.01

Formula

C20H23ClFN5O2S2
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

Everafenib 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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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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:

Everafenib2923700-82-5RafRaf kinasesmetastatic melanomaBBBCNSV600E BRAFintracranialMAPK pathwayInhibitorinhibitorinhibit

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