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Navtemadlin
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Catalog No. TQ0127Cas No. 1352066-68-2
Alias CS-1300, AMG232
Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.
Navtemadlin
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Purity: 99.08%
Catalog No. TQ0127Alias CS-1300, AMG232Cas No. 1352066-68-2
Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $67 | In Stock | In Stock | |
| 2 mg | $95 | In Stock | In Stock | |
| 5 mg | $147 | In Stock | In Stock | |
| 10 mg | $228 | In Stock | In Stock | |
| 25 mg | $463 | In Stock | In Stock | |
| 50 mg | $683 | In Stock | In Stock | |
| 100 mg | $973 | In Stock | 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:99.08%
ee:100%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM. |
| Targets&IC50 | MDM2:0.045 nM (Kd), p53-MDM2:0.6 nM |
| In vitro | METHODS: Navtemadlin (0.1, 1, 10 μM) treated B16-F10 cells to determine whether reactivation of p53 by Navtemadlin would induce tumor growth arrest. RESULTS Navtemadlin induced significant p53-dependent growth arrest but minimal apoptosis in B16-F10 cells. [1] |
| In vivo | METHODS: Navtemadlin (AMG232)(20 mg/kg (ip)) was used to treat C57Bl/6 mice bearing B16-F10 melanoma tumors to observe whether it inhibited tumor growth in mice. RESULTS When Navtemadlin (AMG232) was administered daily starting from day 3, p53 tumor size was reduced by approximately 30%-50%. [1] METHODS: Navtemadlin (AMG232) (10, 25, 75 mg/kg, once daily, orally) was used to observe whether it could inhibit the growth of mouse tumor xenografts. RESULTS Navtemadlin (AMG232) activated p53 pathway activity in vivo and effectively inhibited the growth of mouse tumor xenografts. It also blocked DNA synthesis and induced apoptosis in vivo[2]. |
| Cell Research | Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347, and A427 cells. Concentration: 0-10 μM [1]. Incubation Time: 72 hours. |
| Animal Research | Animal Model: Female athymic nude mice (n=10) based cancer models. Dosage: 10, 25, 75 mg/kg. Administration: Once daily by oral gavage [1]. |
| Synonyms | CS-1300, AMG232 |
| Molecular Weight | 568.55 |
| Formula | C28H35Cl2NO5S |
| Cas No. | 1352066-68-2 |
| Smiles | CC(C)[C@@H](CS(=O)(=O)C(C)C)N1[C@@H]([C@H](C[C@](C)(CC(O)=O)C1=O)c1cccc(Cl)c1)c1ccc(Cl)cc1 |
| Relative Density. | 1.254 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 | H2O: Insoluble DMSO: 150 mg/mL (263.83 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.52 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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