Takeda-6d

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Takeda-6d

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1125632-93-0

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。

生物活性

Takeda-6D (compound 6d) is an orally active and potentBRAF/VEGFR2inhibitor, withIC₅₀values 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 ofERK1/2phosphorylation. 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].

分子量

547.99

Formula

C₂₇H₁₉ClFN₅O₃S

CAS 号

1125632-93-0

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.