Navtemadlin (Synonyms: AMG 232; KRT-232)

Name: Navtemadlin
Brand: MedChemExpress
SKU: HY-12296
Rating: 5.0 (18 reviews)

Cat. No.: HY-12296 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM.

For research use only. We do not sell to patients.

Navtemadlin Chemical Structure

CAS No. : 1352066-68-2

Size	Price	Stock	Quantity
1 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1520	In-stock	Estimated Time of Arrival: December 31
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Based on 18 publication(s) in Google Scholar

Other Forms of Navtemadlin:

(3S,5S,6R)-Navtemadlin Get quote
Navtemadlin-d₇ Get quote

17 Publications Citing Use of MCE Navtemadlin

: Navtemadlin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2020 Jul 6;6:57. [Abstract]; The effect of AMG-232 on the p53 signaling pathway, and the expression of IL-6 and PD-L1 at different drug doses is assessed by immunoblotting. AMG-232 treatment leads to activation of the p53 signaling pathway in the cancer cells in a dose-dependent manner. The effect of significant reduction in IL-6 expression is observed with AMG-232 in a dose-dependent manner.

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Description

Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM^[1]^[2].

IC₅₀ & Target

IC50: 0.6 nM (p53-MDM2 interaction)^[1]
Kd: 0.045 nM (MDM2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	> 25 μM Compound: 2, AMG 232	Antiproliferative activity against p53 -deficient human HCT116 cells after 16 hrs by BrdU proliferation assay Antiproliferative activity against p53 -deficient human HCT116 cells after 16 hrs by BrdU proliferation assay	[PMID: 24456472]
HCT-116	IC₅₀	10 nM Compound: 2, AMG 232	Antiproliferative activity against human HCT116 cells expressing p53 wild type after 16 hrs by BrdU proliferation assay Antiproliferative activity against human HCT116 cells expressing p53 wild type after 16 hrs by BrdU proliferation assay	[PMID: 24456472]
HCT-116	GI₅₀	33 μM Compound: AMG 232	Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	[PMID: 29691156]
HCT-116	GI₅₀	7 μM Compound: AMG 232	Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	[PMID: 29691156]
SJSA-1	ED₅₀	2.8 nM Compound: 2, AMG 232	Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as unbound concentration causing inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treat Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as unbound concentration causing inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treat	[PMID: 24456472]
SJSA-1	IC₅₀	47 nM Compound: 1, AMG 232	Binding affinity to MDM2 in human SJSA1 cells assessed as induction of p21 gene level after 7 hrs by qRT-PCR assay in presence of 10% human serum Binding affinity to MDM2 in human SJSA1 cells assessed as induction of p21 gene level after 7 hrs by qRT-PCR assay in presence of 10% human serum	[PMID: 25384157]
SJSA-1	ED₅₀	9.1 mg/kg Compound: 2, AMG 232	Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treated control Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treated control	[PMID: 24456472]
SJSA-1	IC₅₀	9.1 nM Compound: 2, AMG 232	Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum	[PMID: 24456472]
SJSA-1	IC₅₀	9.2 nM Compound: 1, AMG 232	Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 16 hrs by Click-iT EdU HCS assay in presence of 10% human serum Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 16 hrs by Click-iT EdU HCS assay in presence of 10% human serum	[PMID: 25384157]

In Vitro

Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines^[1].
Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC₅₀=10 nM)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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.
Incubation Time:	72 hours.
Result:	Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN). Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.

In Vivo

Navtemadlin (AMG 232) (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo^[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice^[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo^[1].
Navtemadlin causes a dose-dependent tumor growth inhibition with an ED₅₀ of 16 mg/kg^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice (n=10/group) based cancer models^[1].
Dosage:	10, 25, 75 mg/kg.
Administration:	Once daily by oral gavage.
Result:	Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED₅₀ of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.

Clinical Trial

Molecular Weight

568.55

Formula

C₂₈H₃₅Cl₂NO₅S

CAS No.

1352066-68-2

Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)C[C@]1(C)C(N([C@H](CS(=O)(C(C)C)=O)C(C)C)[C@H](C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC(Cl)=C3)C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (87.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7589 mL	8.7943 mL	17.5886 mL
5 mM	0.3518 mL	1.7589 mL	3.5177 mL
10 mM	0.1759 mL	0.8794 mL	1.7589 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 1.5 mg/mL (2.64 mM); Clear solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.59 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (258 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Canon J, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58. [Content Brief]

[2]. Rew Y, et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41. [Content Brief]

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7589 mL	8.7943 mL	17.5886 mL	43.9715 mL
	5 mM	0.3518 mL	1.7589 mL	3.5177 mL	8.7943 mL
	10 mM	0.1759 mL	0.8794 mL	1.7589 mL	4.3972 mL
	15 mM	0.1173 mL	0.5863 mL	1.1726 mL	2.9314 mL
	20 mM	0.0879 mL	0.4397 mL	0.8794 mL	2.1986 mL
	25 mM	0.0704 mL	0.3518 mL	0.7035 mL	1.7589 mL
	30 mM	0.0586 mL	0.2931 mL	0.5863 mL	1.4657 mL
	40 mM	0.0440 mL	0.2199 mL	0.4397 mL	1.0993 mL
	50 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8794 mL
	60 mM	0.0293 mL	0.1466 mL	0.2931 mL	0.7329 mL
	80 mM	0.0220 mL	0.1099 mL	0.2199 mL	0.5496 mL

Navtemadlin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Navtemadlin (Synonyms: AMG 232; KRT-232)

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17 Publications Citing Use of MCE Navtemadlin

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