Bcr-Abl


The Philadelphia chromosome or Philadelphia translocation is a specific genetic abnormality in chromosome 22 of leukemia cancer cells (particularly chronic myelogenous leukemia (CML) cells). This chromosome is defective and unusually short because of reciprocal translocation of genetic material between chromosome 9 and chromosome 22, and contains a fusion gene called BCR-ABL1.
  • Dasatinib Monohydrate EY0800

    Dasatinib是一种Src/Abl抑制剂,IC50分别为0.6 nM和0.8 nM。

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  • Bosutinib EY1727

    Bosutinib (SKI-606)是一种新型的Sarcoma/Abelson (Src/Abl)酪氨酸激酶双重抑制剂,其IC50分别为1.2 nM和1 nM。

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  • Degrasyn EY1506

    Degrasyn (WP1130)是一种选择性的去泛素化酶(DUB: USP5, UCH-L1, USP9x, USP14, UCH37)抑制剂,也抑制Bcr/Abl,也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。

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  • Nilotinib EY1239

    Nilotinib (尼洛替尼; AMN-107) 是Bcr-Abl抑制剂,IC50小于30 nM。

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  • Saracatinib EY1111

    Saracatinib (AZD0530)是一种有效的Src抑制剂,IC50为2.7 nM,对c-Yes, Fyn, Lyn, Blk, Fgr和Lck等也有活性;但对Abl和EGFR (L858R和L861Q)活性较低。

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