3PO
作者：齐岳
发布时间：2023-09-13
17:38:33
点击数：
产品名称：3PO
产品描述：
| 产品描述 | 3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH. |
| 靶点活性 | PFKFB3:22.9 μM |
| 体外活性 | 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. Compared with the wild-type PFKFB3+/+transformed cells (IC50, 49 μM), the PFKFB3+/- fibroblasts were more sensitive to compound 3PO treatment (IC50, 26 μM). 3PO Causes G2-M phase arrest, which Is preceded by decreased Fru-2,6-BP and glucose uptake. 3PO slows growth through inhibition of PFK-2 activity, then ectopic expression of the PFKFB3 isozyme may thwart the cytostatic activity of 3PO. [1] 3PO inhibits the glycolytic regulator PFKFB3 in endothelial cells (ECs). 3PO decreases glycolysis in ECs and impairs vessel sprouting. 3PO also suppresses vascular hyperbranching induced by inhibition of Notch or VEGF receptor 1 (VEGFR1) and amplified the antiangiogenic effect of VEGF blockade[2]. |
| 体内活性 | Compared with vehicle control, compound 3PO treatment significantly reduced Fru-2,6-BP in tumor xenografts (vehicle: 13.1 ± 1.9 pmol/mg, 3PO: 8.5 ± 1.7 pmol/mg). [1] 3PO also impairs (pathological) angiogenesis. |
| 分子量 | 210.23 |
| 分子式 | C13H10N2O |
| CAS No. | 18550-98-6 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: Insoluble
DMSO: 113mg/ml（537.51mM）
Ethanol: 11 mg/mL (52.32 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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