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HLM006474
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Catalog No. T15486Cas No. 353519-63-8
HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells).
HLM006474
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Purity: 99.20%
Catalog No. T15486Cas No. 353519-63-8
HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $38 | In Stock | In Stock | |
| 5 mg | $61 | In Stock | In Stock | |
| 10 mg | $88 | In Stock | In Stock | |
| 25 mg | $166 | In Stock | In Stock | |
| 50 mg | $296 | In Stock | In Stock | |
| 100 mg | $490 | In Stock | In Stock | |
| 500 mg | $1,090 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.20%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 μM in A375 cells). |
| Targets&IC50 | E2F4 DNA-binding:29.8 μM |
| In vitro | HLM006474 causes the viability of both SCLC and NSCLC lines (IC50 ranging from 15 to 75 μM). HLM006474 displays little activities against E2F4 DNA-binding in A375 cells at 10 and 20 μM, apparently inhibits E2F4 DNA-binding at 40 μM, and increasingly suppresses the effect at 60 and 80 μM concentrations. HLM006474 dramatically causes cyclin D3 protein expression and is a potent inducer of PARP cleavage[1]. HLM006474 (20 μM) weakly synergizes with paclitaxel, but there is antagonism between HLM006474 and cisplatin and gemcitabine in H1299 cells[2]. HLM006474 (40 μM) inhibits E2F4 activity via suppression of its DNA-binding activity and down regulation of its expression and HLM006474 (40 μM) also obviously causes apoptosis in A375 and 231 cell lines for 24 hours. HLM006474 (60 μM) enhances the expression of several known E2F-regulated genes after short treatments in H292 and H1299 cell lines. HLM006474 leads to a reduction in the mRNA levels of MAD2. HLM006474 apparently suppresses the increase of Mad2 protein and pRb-S780 signal but not the level of Skp2 protein in human lung cancer A549 cellss. |
| Molecular Weight | 399.48 |
| Formula | C25H25N3O2 |
| Cas No. | 353519-63-8 |
| Smiles | CCOc1ccc(cc1C)C(Nc1ccccn1)c1ccc2ccc(C)nc2c1O |
| Relative Density. | 1.227 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 15.625 mg/mL (39.11 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.5 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
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
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.Stock Solution Preparation:
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.
Preparation of the In Vivo Formulation:
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.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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