AT9283,896466-04-9

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AT9283

CAS No. : 896466-04-9

MCE 国际站：AT9283

产品活性：AT9283 是一种多靶点激酶抑制剂，有效抑制 Aurora A/B，JAK2/3，Abl (T315I)，和 Flt3 (IC₅₀ 值范围为 1-30 nM)。AT9283 抑制多种实体瘤在体内外的生长和存活。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Cell Cycle/DNA Damage  |  Apoptosis  |  Autophagy

作用靶点：JAK  |  Aurora Kinase  |  Bcr-Abl  |  FLT3  |  Apoptosis  |  Autophagy

In Vitro: AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC₅₀ of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation.
AT9283 induces apoptosis in a dose and time dependent manner and inhibits cell proliferation with an IC₅₀ < 1 μM in B-NHL cell lines.
AT9283 inhibits growth, induces dose dependent cytotoxicity, and inhibits STAT3 signaling pathway in MM cell lines. T9283 inhibits phospho Histone H3 and phospho Aurora A at Thr 288. AT9283 increases G2/M phase and induces apoptosis of MM cells in a time-dependent manner.

In Vivo: In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors (2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice.
AT9283 (15 mg/kg) and docetaxel (10 mg/kg) alone has modest anti-tumor activity. T9283 at 20 mg/kg and AT9283 (15 or 20 mg/kg) plus docetaxel (10 mg/kg) demonstrate a statistically significant tumor growth inhibition and enhance survival inmouse xenograft model of mantle cell lymphoma.
AT9283 (45 mg/kg, i.p.) inhibits tumor growth in mice. Two cycles of AT9283 45 mg/kg 14 hours after drug administration confirm decreased expression of phospho-Histone H3 and Aurora B in treated animals.

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