2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. Raf VEGFR PERK
  4. Takeda-6D

Takeda-6D (compound 6d) 是一种口服有效的 BRAF/VEGFR2 抑制剂，IC50 分别为 7.0 和 2.2 nM。Takeda-6D 在 293/KDR 和 VEGF 刺激的 HUVEC 细胞中通过抑制 VEGFR2 通路表现出抗血管生成的作用。Takeda-6D 显著抑制 ERK1/2 磷酸化。Takeda-6D 具有抗肿瘤活性。

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Takeda-6D Chemical Structure

Takeda-6D Chemical Structure

CAS No. : 1125632-93-0

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规格 价格 是否有货
1 mg ￥2446
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Takeda-6D 相关抗体

Top Publications Citing Use of Products

查看 Raf 亚型特异性产品:

查看所有亚型
BRaf c-Raf Raf

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity[1].

IC50 & Target

VEGFR2

2.2 nM (IC50)

Braf

7.0 nM (IC50)

体内研究
(In Vivo)

Takeda-6D (compound 6d) (10 mg/kg, Orally, once) shows sufficient oral bioavailability (F = 70.5%) in rats[1].
Takeda-6D (0-10 mg/kg, Orally, once) significantly decreases phosphorylation levels of ERK1/24 h after oral administration in an A375 (BRAFV600E mutant) human melanoma xenograft model in rats[1].
Takeda-6D (10 mg/kg, Orally, twice daily for 2 weeks) shows tumor regression with T/Cof −7.0% without severe toxicity, and this tumor regression should include the efficacy based on the antiangiogenesis potency and BRAF inhibitory activity[1].

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

547.99

Formula

C27H19ClFN5O3S
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

Takeda-6D 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Takeda-6D1125632-93-0RafVEGFRPERKRaf kinasesVascular endothelial growth factor receptorProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseantiangiogenesisHUVEC cellsantitumorpERKRAForally activeInhibitorinhibitorinhibit

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