DCLK1-IN-1,2222635-15-4

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DCLK1-IN-1

CAS No. : 2222635-15-4

MCE 国际站：DCLK1-IN-1

产品活性：DCLK1-IN-1 是一种选择性的、体内相容的双皮质素样激酶1 DCLK1 激酶结构域化学探针。DCLK1-IN-1抑制 DCLK1 和 DCLK2 激酶 (结合和激酶测定 IC₅₀ 分别为: DCLK1=9.5/57.2 nM 和 DCLK2=31/103 nM)。DCLK1-IN-1 具有低毒性，可以研究 DCLK1 的生物学特性，确定其在肿瘤中的作用，如 DCLK1⁺ 胰腺导管腺癌 (PDAC)。

研究领域：Others

作用靶点：Others

In Vitro: DCLK1-IN-1 shows no significant activity against ERK5, ACK, and LRRK2. DCLK1-IN-1 potently binds DCLK1 in HCT116 cells (IC₅₀?=?279?nM). DCLK1-IN-1 significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lysates and live cells.

In Vivo: DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09?hours, an area under the curve of 5506?h/ng?mL and 81% oral bioavailability.

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