Art. -Nr.: HY-153390

AMG-193

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC₅₀=0.107 μM), thereby protecting normal cells with wild-type MTAP.

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Reinheit: 99.71%
CAS. Nr.: 2790567-82-5
Formel: C₂₂H₁₉F₃N₄O₃
Molecular Weight:444.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AMG-193 Chemical Structure

CAS. Nr.: 2790567-82-5

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

AMG 193 (200 μM; 6 d) induces alternative splicing defects, cell cycle arrest, and DNA damage response in MTAP-deficient HCT116 cells^[2].

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

Cell Cycle Analysis^[2]

Cell Line:

MTAP-deficient HCT116 cells
Concentration:

200 µM
Incubation Time:

6 d
Result:

Reduced the S phase and increased the G2/M cell population in mtap-deficient cells.

In Vivo

AMG 193 (3-100 mg/kg; p.o.; once every 5 days for 4 doses) dose-dependently inhibits tumor growth in MTAP-deficient xenograft mice^[2].
AMG 193 (100 mg/kg; p.o.; once daily for 11 days) slightly reduces body weight in mice implanted with DLBCL (DOHH-2) tumors and causes tumor regression in 70% of mice, with preservation of normal hematopoietic cell lineages^[2].

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

Animal Model:

HCT116 MTAP-deficient mice^[2]
Dosage:

3、10、30、100 mg/kg
Administration:

p.o.; The drug was administered on day 20 after mice were implanted with DLBCL (DOHH-2) tumor cells and was administered once every 5 days for a total of 4 doses.
Result:

Inhibited SDMA signaling in mtap-deleted tumors at all doses.

Animal Model:

Mice implanted with DLBCL (DOHH-2) tumors^[2]
Dosage:

100 mg/kg
Administration:

p.o.; Once daily for 11 days
Result:

Caused a significant increase in the Sub-G1 population and induced tumor cell death.

Chemical Information

CAS. Nr. 2790567-82-5
Appearance Solid
Molecular Weight 444.41
Formel C₂₂H₁₉F₃N₄O₃
Color White to light yellow
SMILES

O=C(N1[C@@H](C2=CC=C(C=C2)C(F)(F)F)COCC1)C3=NC=C4N=C(N)C(COC5)=C5C4=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Cell Rep

LKB1 inactivation elicits an NNMT-mediated methyl sink and confers dependence on PRMT5 in lung cancer. [Abstract]

2026 Jun 2;45(6):117487. PMID: 42234565

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (225.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2502 mL

11.2509 mL

22.5017 mL

5 mM

0.4500 mL

2.2502 mL

4.5003 mL

10 mM

0.2250 mL

1.1251 mL

2.2502 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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: ≥ 5 mg/mL (11.25 mM); Clear solution

Working 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: 0.5% CMC-Na/0.5% Tween-80 in Saline water

Solubility: 2.49 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Belmontes B, et al. Abstract B177: The discovery and preclinical characterization of AMG 193, a first-in-class MTA-cooperative PRMT5 inhibitor with broad activity against MTAP-null cancers[J]. Molecular Cancer Therapeutics, 2023, 22(12_Supplement): B177-B177.

[2]. Belmontes B, et al. AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients with MTAP-Deleted Cancers[J]. Cancer Discovery, 2024: OF1-OF23. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2502 mL	11.2509 mL	22.5017 mL	56.2544 mL
	5 mM	0.4500 mL	2.2502 mL	4.5003 mL	11.2509 mL
	10 mM	0.2250 mL	1.1251 mL	2.2502 mL	5.6254 mL
	15 mM	0.1500 mL	0.7501 mL	1.5001 mL	3.7503 mL
	20 mM	0.1125 mL	0.5625 mL	1.1251 mL	2.8127 mL
	25 mM	0.0900 mL	0.4500 mL	0.9001 mL	2.2502 mL
	30 mM	0.0750 mL	0.3750 mL	0.7501 mL	1.8751 mL
	40 mM	0.0563 mL	0.2813 mL	0.5625 mL	1.4064 mL
	50 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1251 mL
	60 mM	0.0375 mL	0.1875 mL	0.3750 mL	0.9376 mL
	80 mM	0.0281 mL	0.1406 mL	0.2813 mL	0.7032 mL
	100 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL

Keywords

AMG-193

1 Cited Publications

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AMG-193

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AMG-193

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-193

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) AMG-193

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG-193 Related Classifications

HY-153390 Related Classifications