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AS-99 TFA

CAS No. :

MCE 站：AS-99 TFA

产品活性：AS-99 TFA 是首创的、有效的、选择性的 ASH1L 组蛋白甲基转移酶抑制剂 (IC₅₀=?0.79??M, K_d=?0.89??M)，具有抗白血病活性。AS-99 TFA 在体内阻断细胞增殖，诱导细胞凋亡 (apoptosis) 和分化，下调 MLL 融合靶基因，减轻白血病。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Histone Methyltransferase  |  Apoptosis

In Vitro: AS-99 TFA is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50??M of AS-99 TFA on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L.
AS-99 TFA shows effect on the growth of the MLL leukemia cells (MV4;11, MOLM13, KOPN8, RS4;11) with the GI₅₀ values ranging from 1.8??M to 3.6??M.
AS-99 (1-8 ?M; 7 days) TFA also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells.
AS-99 TFA suppresses MLL fusion driven transcriptional programs.

In Vivo: AS-99 (30?mg/kg; i.p.; q.d., treated for 14 consecutive days) TFA reduces leukemia burden in mice.
AS-99 TFA is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC?=?9701?hr* ng/mL and 10,699?hr* ng/mL, respectively), suitable half-life (~5–6?h) and Cmax?>10??M.

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