Takeda-6D,1125632-93-0

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Takeda-6D

CAS No. : 1125632-93-0

MCE 国际站：Takeda-6D

产品活性：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。

研究领域：MAPK/ERK Pathway  |  Protein Tyrosine Kinase/RTK  |  Cell Cycle/DNA Damage

作用靶点：Raf  |  VEGFR  |  PERK

In Vivo: Takeda-6D (compound 6d) (10 mg/kg, Orally, once) shows sufficient oral bioavailability (F = 70.5%) in rats.
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.
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.

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