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ALK5-IN-34

CAS No. : 2785430-90-0

MCE 站：ALK5-IN-34

产品活性：ALK5-IN-34 是一种选择性的激活素受体样激酶 (ALK) 抑制剂，具有口服活性。ALK5-IN-34 可以抑制激活素受体样激酶的活性，IC₅₀ 值 ≤10 nM。ALK5-IN-34 还具有抑制肿瘤生长的作用，可用于癌症等增殖性疾病的研究。

研究领域：TGF-beta/Smad  |  Stem Cell/Wnt

作用靶点：TGF-β Receptor  |  TGF-beta/Smad

In Vitro: ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC₅₀ value of ≤10 nM.
ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC₅₀ value of ＜100 nM.
ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC₅₀ value of ≤100 nM.
ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent.
ALK5-IN-34 (30, 300 ａnd 3000 nM) suppresses the Treg frequency in a dose dependent manner.
ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2^CI34W-driven growth in KGN ａnd COV434 cells with IC50 values of 140 nM and10 μM, respectively.
ALK5-IN-34 (10, 100 ａnd 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line.
ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent.
ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent.

In Vivo: ALK5-IN-34 (EX-11) (oral; 10-100 mg/kg) reduces the phopho SMAD2 levels (p-SMAD2) in a dose dependent manner in A549 murine xenograft model.
ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK ａnd tumor PD (pSMAD2 levels).
ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model ａnd can delay progression.
ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) ａnd increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model ａnd in Subcutaneous Cloudman S91 melanoma model.
ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability ａnd safety margin in Tolerability Model.

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