SD-36,2429877-44-9

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SD-36

CAS No. : 2429877-44-9

MCE 国际站：SD-36

产品活性：SD-36 是一种有效的 STAT3 PROTAC 降解剂 (K_d=~50 nM)，与其他 STAT 成员相比具有很高的选择性。SD-36 有效降解细胞中突变的 STAT3 蛋白，并抑制 STAT3 的转录活性 (IC₅₀=10 nM)。SD-36 发挥强大的抗肿瘤活性，并在小鼠肿瘤模型中实现了完整而持久的肿瘤消退。SD-36 由 STAT3 抑制剂 SI-109、 linker 和一个用于 E3 泛素连接酶的 Cereblon 配体 Lenalidomide 类似物组成。

研究领域：PROTAC  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Apoptosis

作用靶点：PROTACs  |  STAT  |  Apoptosis

In Vitro: SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large-cell lymphoma cell lines by inducing cell-cycle arrest and/or apoptosis.
SD-36 (0.005-5 μM; 4 days) demonstrates potent activity (IC₅₀＜2 μM) in MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines.
SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells.

In Vivo: SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice.
?SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model.
?SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model.

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