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    Association details:
    Biomarker:SRSF2 P95H
    Cancer:Acute Myelogenous Leukemia
    Drug:E7107 (SF3B1 inhibitor)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: D – Preclinical
    New
    Source:
    ASH 2021
    Title:

    CTX-712, a Novel Clk Inhibitor Targeting Myeloid Neoplasms with SRSF2 Mutation

    Published date:
    11/04/2021
    Excerpt:
    To further investigate the effect of CTX-712 on tumor growth in vivo, we established 13 MDS/AML-derived xenografts (PDXs), which were treated with varying doses of CTX-712. Among the 13 PDX models, SRSF2 mutation was found in 2 cases, which had the SRSF2 P95H or P95L mutation...Overall, 10 out of 13 PDX AML/MDS models, including 2 SRSF2-mutated models, showed anti-tumor effect of CTX-712.
    DOI:
    10.1182/blood-2019-131559
    Evidence Level:
    Sensitive: D – Preclinical
    Source:
    Nat Med
    Title:

    Modulation of splicing catalysis for therapeutic targeting of leukemias with spliceosomal mutations

    Excerpt:
    Ten days of intravenous administration of E7107 at 4mg/kg/day resulted in decreased disease burden as assessed by peripheral blood leukocyte count and GFP percentage (Fig. 2f), histological analyses (Supplementary Fig. 3h) and survival benefit in Srsf2P95H/+ mice (p=0.001),...
    DOI:
    https://dx.doi.org/10.1038%2Fnm.4097