MM-206 是一种 STAT3 活性抑制剂，有效抑制 STAT3 SH2 结构域-磷酸肽相互作用，IC50 为 1.2 μM。 MM-206 在急性髓性白血病 (AML) 细胞系中表现出剂量依赖性诱导细胞凋亡。
| Cas No. | 1809581-87-0 |
| Canonical SMILES | OC(C(C=CC=C1)=C1C(NS(C2=C(F)C(F)=C(F)C(F)=C2F)(=O)=O)=C3)=C3SC4=CC=CC=C4 |
| 分子式 | C22H12F5NO3S2 |
| 分子量 | 497.5 |
| 溶解度 | DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:8): 0.11 mg/ml,DMSO: 16 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | MM-206 is an inhibitor of STAT3 (IC50 = 1.16 µM in an SPR-based competitive assay). It inhibits STAT3 phosphorylation induced by granulocyte colony-stimulating factor (G-CSF) in HL-60, Kasumi-1, and MOLM-13 acute myeloid leukemia (AML) cells (IC50s = 0.8, 1.9, and 1.1 µM, respectively). MM-206 induces apoptosis more potently in AML cell lines and patient-derived primary AML tumor cells than in acute lymphoblastic leukemia cells, which do not have upregulated STAT3 activity. It also slows disease progression and improves survival in an AML mouse xenograft model when administered at a dose of 30 mg/kg per day. |
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