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Synonyms: Werner syndrome RecQ helicase-IN-1, HRO-761


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $55 | In Stock | In Stock | |
| 5 mg | $127 | In Stock | In Stock | |
| 10 mg | $186 | In Stock | In Stock | |
| 25 mg | $312 | In Stock | In Stock | |
| 50 mg | $528 | In Stock | In Stock | |
| 100 mg | $787 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $239 | In Stock | In Stock |
| Description | HRO761 (Werner syndrome RecQ helicase-IN-1, Example 42) is a small molecule inhibitor, a potent WRN inhibitor with high efficacy, and can be used for research on cancers such as colon cancer and gastric cancer. |
| Targets & IC50 | WRN ATPase:100 nM, SW48 cells:50 nM, DLD1 WRN-KO cells:> 10 μM |
| In vitro | Methods: HRO761 was administered to SW48 (MSI) and CAL33 (MSS) cells for 4 days. Results: CellTiter-Glo assay demonstrated selective inhibition of MSI cell proliferation with a GI50 of 40 nM, while showing no activity against MSS cells. Colony formation assays (10–14 days) confirmed GI50 ranges of 50–1000 nM in MSI cells. Western blot detected activation of DNA damage markers and WRN degradation. [1] Methods: An LC-MS/MS method was established for the determination of HRO761 concentration in rat plasma and applied to pharmacokinetic studies. Results: Following oral administration of HRO761 (5, 10, 20 mg/kg), rapid absorption was observed with time to peak concentration of 1.0–4.0 h, and absolute bioavailability ranged from 79.0% to 99.1%. [2] |
| In vivo | Methods: In the SW48 cell-derived xenograft tumor model (female nude mice), HRO761 was administered orally (20, 40, 60, 120 mg/kg, once daily, dissolved in 20% hydroxypropyl-β-cyclodextrin) for 92 consecutive days of treatment. Results: The 20 mg/kg dose achieved tumor stasis, while 60-120 mg/kg doses induced 75-90% tumor regression in a dose-dependent manner. [1] |
| Synonyms | Werner syndrome RecQ helicase-IN-1, HRO-761 |
| Molecular Weight | 702.08 |
| Formula | C31H31ClF3N9O5 |
| Cas No. | 2869954-34-5 |
| Smiles | C(C(NC1=C(Cl)C=C(C(F)(F)F)C=C1)=O)N2C=3N(C(=O)C(=C2CC)N4CCN(C(=O)C=5C(O)=C(C)N=CN5)CC4)N=C(N3)C=6CCOCC6 |
| Storage | Store at low temperature,Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 99.7 mg/mL (142.01 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (4.7 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. | ||||||||||||||||||||||||||||||||||||
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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