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KW-2449

CAS No. : 1000669⁻⁷2-6

MCE 国际站：KW-2449

产品活性：KW-2449是多靶点激酶抑制剂，对FLT3，ABL，ABL^T315I和 Aurora kinase 的 IC₅₀ 值分别为6.6，14，4 和 48 nM。

研究领域：Protein Tyrosine Kinase/RTK | Epigenetics | Cell Cycle/DNA Damage | Apoptosis

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

In Vitro: KW-2449 shows growth inhibitory activities against FLT3/ITD-, FLT3/D835Y-, and wt-FLT3/FL-expressing 32D cells, MOLM-13 and MV4;11 with GI₅₀ values of 0.024, 0.046, 0.014, 0.024, and 0.011 µM, respectively. KW-2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent manner. KW-2449 increases the percentage of cells in the G1 phase of the cell cycle and reciprocally reduced the percentage of cells in the S phase, resulting in the increase of apoptotic cell population.

In Vivo: Oral administration of KW-2449 shows dose-dependent and significant tumor growth inhibition in FLT3-mutated xenograft model with minimum bone marrow suppression. In FLT3 wild-type human leukemia, it induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis. In imatinib-resistant leukemia, KW-2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases. Furthermore, the antiproliferative activity of KW-2449 is confirmed in primary samples from AML and imatinib-resistant patients. The inhibitory activity of KW-2449 is not affected by the presence of human plasma protein, such as α1-acid glycoprotein.

相关产品：Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Cytoskeleton Compound Library | Anti-Lung Cancer Compound Library | Anti-Blood Cancer Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11⁻⁷082 | Etoposide | Mitomycin C | CCCP | DAPT | Rotenone | Etomoxir | Stattic | Docetaxel | Fulvestrant

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