ABC 1183

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ABC1183 是一种有效、选择性、口服活性的 GSK3α/β 和 CDK9 抑制剂，IC50 分别为 327/657 nM 和 321 nM (CDK9/cyclin T1)。

ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modulates oncogenic signaling through changes in GSK3, GS and β-catenin phosphorylation and MCL1 expression; suppresses tumor growth and inflammation-driven gastrointestinal disease symptoms without organ or hematological toxicity in vivo.

ABC1183 (3 μM, 24 h) can block cell cycle progression and thus affect cell proliferation. Cell Cycle Analysis Cell Line:LNCaP human prostate cancer cells Concentration:3 μM Incubation Time:24 hours Result:Significantly reduced cells in the G1 and S phases and increased cells in the G2/M and sub-G1 cycle phases.

ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation through negative regulation of cell growth and pro-inflammatory signalling in male C57BL/6 mice. Animal Model:Male C57BL/6 mice with melanoma B16 Dosage:5 mg/kg Administration:Oral gavage; 5 times per week; 22 days Result:Reduced tumor size and no observed toxicity.Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression.Animal Model:Male C57BL/6 mice infected crohn’s disease Dosage:50 mg/kg Administration:Oral gavage; everyday; 3 days Result:Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%.Animal Model:Male C57BL/6 mice with ulcerative colitisDosage:50 mg/kg Administration:Oral gavage; once daily; 6 days Result:Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6.

ABC1183

PI3K/Akt/mTOR signaling

GSK-3

GSK-3

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1042735-18-1

334.397

C18H14N4OS

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (373.82 mM)

N#CC1=CC=C(C(C2=C(N)N=C(NC3=CC=C(C)C=C3)S2)=O)C=C1

4-(4-Amino-2-p-tolylamino-thiazole-5-carbonyl)-benzonitrile

(-20℃)

With Ice Pack

≥ 2 years