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Navtemadlin (Synonyms: CS-1300, AMG232)

Name: Navtemadlin
Brand: TargetMol
SKU: TQ0127
Price: 67 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. TQ0127 Copy Product Info

Purity: 99.08%

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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

Copy Product Info

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Catalog No. TQ0127

Synonyms 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.

Cas No. 1352066-68-2

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Pack Size	Price	USA Stock	Global Stock
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

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.08%

ee:100%

Appearance:Solid

Color:White

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COA CSFC LCMS HNMR

Product Introduction

Bioactivity

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

Chemical Properties

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 | 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

	1mg	5mg	10mg	50mg
1 mM	1.7589 mL	8.7943 mL	17.5886 mL	87.9430 mL
5 mM	0.3518 mL	1.7589 mL	3.5177 mL	17.5886 mL
10 mM	0.1759 mL	0.8794 mL	1.7589 mL	8.7943 mL
20 mM	0.0879 mL	0.4397 mL	0.8794 mL	4.3972 mL
50 mM	0.0352 mL	0.1759 mL	0.3518 mL	1.7589 mL
100 mM	0.0176 mL	0.0879 mL	0.1759 mL	0.8794 mL

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.

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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 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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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