Tuspetinib,2294874-49-8

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Tuspetinib

CAS No. : 2294874-49-8

MCE 国际站：Tuspetinib

产品活性：Tuspetinib (HM43239) 是具有口服活性的选择性 FLT3 抑制剂，IC₅₀ 值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。Tuspetinib 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性，并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。Tuspetinib 抑制白血病细胞的增殖，诱导细胞凋亡 (apoptosis)。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：FLT3  |  Apoptosis

In Vitro: Tuspetinib potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation, such as MV4-11 (IC₅₀: 1.3 nM), MOLM-13 (IC₅₀: 5.1 nM), and MOLM-14 (IC₅₀: 2.9 nM). Tuspetinib also inhibits KG1a cells (CD34+/CD38- cells) proliferation.
Tuspetinib induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells).
Tuspetinib potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells.

In Vivo: Tuspetinib shows the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity.
Tuspetinib prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models.

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