Tamanho : 50mg
Telefone : +1 850 650 7790
Synonyms: PT2977, MK-6482
| Description | Belzutifan (MK-6482, PT2977) is a small-molecule inhibitor and a HIF-2α inhibitor (IC50 = 9 nM) with high selectivity, oral activity, and improved pharmacokinetic characteristics, used for the treatment of clear cell renal cell carcinoma and related VHL diseases. |
| Targets & IC50 | HIF2α:9 nM |
| In vitro | Methods: Cell proliferation assays and CRISPR functional experiments were used to detect the in vitro activity of Belzutifan. VHL-deficient clear cell renal cell carcinoma OSRC2, TUHR4TKB, and 786-O cells were selected and incubated with 2 μM drug for 16 days, with HIF2α knockout groups set as controls. Results: Belzutifan significantly inhibited cell proliferation, blocked HIF2α binding to ARNT, and downregulated CCND1 expression; sustained overexpression of Cyclin D1 in cells reversed the proliferation inhibitory effect of Belzutifan. [1] Methods: VHL-deficient clear cell renal cell carcinoma (ccRCC) cells were selected and incubated with gradient concentrations of Belzutifan to detect HIF-2α target gene expression and cell proliferation changes. Results: Belzutifan specifically blocked HIF-2α dimerization with ARNT, significantly downregulated pro-oncogenic gene expression, and effectively inhibited ccRCC cell proliferation in a dose-dependent manner, providing evidence for in vivo antitumor activity. [2] |
| In vivo | Methods: A clear cell renal cell carcinoma xenograft mouse model was used. Belzutifan was administered by oral gavage at doses set according to preclinical equivalent regimens, once daily for 21–28 consecutive days, with a vehicle of 0.5% methylcellulose, PEG400, and ethanol mixture, and a blank vehicle control group was established. Results: Belzutifan significantly inhibited tumor growth, downregulated HIF-2α target gene expression in tumor tissue, reduced VEGF and Cyclin D1 levels, showed no significant body weight loss or organ toxicity, and demonstrated definite in vivo antitumor activity with good tolerability. [3] |
| Synonyms | PT2977, MK-6482 |
| Molecular Weight | 383.34 |
| Formula | C17H12F3NO4S |
| Cas No. | 1672668-24-4 |
| Smiles | CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)[C@@H](F)[C@@H](O)c12 |
| Relative Density. | 1.56 g/cm3 (Predicted) |
| Storage | Store under nitrogen,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50.5 mg/mL (131.74 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.22 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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