2. Epigenetics
  3. Histone Methyltransferase
  4. AMG-193

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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AMG-193

AMG-193 Chemische Struktur

CAS. Nr. : 2790567-82-5

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Other Forms of AMG-193:

AMG-193 Related Antibodies

Top Publications Citing Use of Products

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Beschreibung

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[1][2].

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.

AMG-193 Related Antibodies

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.
Molekulargewicht

444.41

Formel

C22H19F3N4O3
CAS. Nr.
Appearance

Solid

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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2502 mL 11.2509 mL 22.5017 mL
5 mM 0.4500 mL 2.2502 mL 4.5003 mL
View the Complete Stock Solution Preparation Table

* 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

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 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.

    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: ≥ 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.

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

mg/kg

Animal weight
(per animal)

g

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 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.
Reinheit & Dokumentation

Purity: 99.71% ee.: 100%

SDS (251 KB)

COA (254 KB) HNMR (452 KB) RP-HPLC (258 KB) NP-HPLC (163 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
Verweise

Complete Stock Solution Preparation Table

* 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.

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
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AMG-193 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.

Keywords:

AMG-1932790567-82-5AMG193AMG 193Histone MethyltransferasePRMT5 InhibitorHCT116Inhibitorinhibitorinhibit

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