- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC50 = 207 nM compared to 22.9 µM for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 µM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 µM. Induces apoptosis and reduces proliferation in transformed cells (mean GI50 of ~3 µM in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PFKFB3
Reversible: yes
Target IC50: 207 nM for hrPFKFP3
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Use only fresh DMSO for reconstitution.
Other Notes
Clem, B. F., et al. 2013. Mol. Cancer Ther.12, 1461.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Level | 100 |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | light beige |
| solubility | DMSO: 10 mg/mL |
| storage temp. | 2-8°C |
| SMILES string | n1ccc(cc1)C(=O)\C=C\c2nc3c(cc2)cccc3 |
| InChI | 1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+ |
| InChI key | UJJUKZPBUMCSJZ-BQYQJAHWSA-N |
| 长度(mm) | |
| 宽度(mm) | |
| 高度(mm) | |
| 重量(kg) |
-
询价
-
¥ 4164.19
-
询价
-
询价
-
询价
-
询价
-
¥ 4968.78
-
¥ 4390.38
-
¥ 2869.87
-
¥ 3662.39
-
询价
-
¥ 51018.02
-
询价
-
询价
-
¥ 21702.96
-
询价
-
询价
-
询价
-
询价
-
询价
微信小程序
7X24小时在线咨询