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Navtemadlin
🥰Excellent
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
🥰Excellent
Purity: 98.86%
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $67 | In Stock | |
| 2 mg | $95 | In Stock | |
| 5 mg | $147 | In Stock | |
| 10 mg | $228 | In Stock | |
| 25 mg | $463 | In Stock | |
| 50 mg | $683 | In Stock | |
| 100 mg | $973 | In Stock |
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Purity:98.86%
ee:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | H2O: Insoluble DMSO: 50 mg/mL (87.94 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Sci Citations
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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