Cat. No.: HY-148419

Ralometostat

(Synonyms: TNG908)

3 Cited Publications

Avis client

Based on 3 publication(s) in Google Scholar

TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research.

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Pureté: 99.90%
CAS No.: 2760481-53-4
Formule: C₂₁H₂₃N₅O₂S
Masse moléculaire:409.50

Stockage:

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

Ralometostat Chemical Structure

CAS No.: 2760481-53-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research^[1].

IC₅₀ & Target

PRMT5

Voir tous les produits spécifiques à Isoform Histone Methyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	0.13 μM Compound: TNG908	Cytotoxicity against MTAP-null human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by CellTiter-Glo luminescent assay Cytotoxicity against MTAP-null human HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by CellTiter-Glo luminescent assay	[PMID: 38595098]
HCT-116	GI₅₀	3.1 μM Compound: TNG908	Cytotoxicity against human wild type HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by CellTiter-Glo luminescent assay Cytotoxicity against human wild type HCT-116 cells assessed as inhibition of cell growth incubated for 7 days by CellTiter-Glo luminescent assay	[PMID: 38595098]

In Vitro

TNG908 (0-10 μM, 24 h) is 15 times more selective for MTAP^null cell lines than MTAP^WT cell lines, and the stability of human liver microsomes is C< sub>lint=14 μL/min/mg^[1].

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

Western Blot Analysis^[1]

Cell Line:

SDMA cell，HAP1 MTAP WT and MTAP-null In-Cell
Concentration:

0-10 μM
Incubation Time:

24 h
Result:

Had an IC₅₀ value of 0.009μM for PRMT5 in SDMA cells.

In Vivo

TNG908 (1-120 mg/kg twice daily for 21 days, p.o. or i.v.) A promotes tumor regression in LU99 NSCLC cell line-derived xenograft mouse model^[1].

Pharmacokinetic Analysis in SD Rats^[1]

Route	Dose (mg/kg)	clearance (mL/min/kg)	V_{ss_obs} (L/kg)	T_1/2 (h)	C_max (μg/mL)	AUC_INF (μg·h/mL)
p.o.	1	38.2	1.5	2	/	/
p.o.	3	/	/	/	0.6	2.5

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2760481-53-4
Appearance Solid
Masse moléculaire 409.50
Formule C₂₁H₂₃N₅O₂S
Color White to light yellow
SMILES

CC1=CC(NC(C(N2[C@@H](C3=CC=C(SC=N4)C4=C3)CC[C@@H](C2)C)=O)=O)=CN=C1N
Synonyms

TNG908
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (3)

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Journal Impact Factor

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
Biomed Chromatogr

A novel, sensitive, and fast ultra-high-performance liquid chromatography tandem mass spectrometry method for TNG908 determination in dog plasma and pharmacokinetic study. [Abstract]

2025 Jan;39(1):e6039. PMID: 39510096
Res Sq

2025 Jul 14.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (244.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.4420 mL

12.2100 mL

24.4200 mL

5 mM

0.4884 mL

2.4420 mL

4.8840 mL

10 mM

0.2442 mL

1.2210 mL

2.4420 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (6.11 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.11 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.11 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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[1]. K. Briggs, et al. TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted cancer.MOLECULAR TARGETED AGENTS 2| VOLUME 174, SUPPLEMENT 1, S84, OCTOBER 2022.

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	2.4420 mL	12.2100 mL	24.4200 mL	61.0501 mL
	5 mM	0.4884 mL	2.4420 mL	4.8840 mL	12.2100 mL
	10 mM	0.2442 mL	1.2210 mL	2.4420 mL	6.1050 mL
	15 mM	0.1628 mL	0.8140 mL	1.6280 mL	4.0700 mL
	20 mM	0.1221 mL	0.6105 mL	1.2210 mL	3.0525 mL
	25 mM	0.0977 mL	0.4884 mL	0.9768 mL	2.4420 mL
	30 mM	0.0814 mL	0.4070 mL	0.8140 mL	2.0350 mL
	40 mM	0.0611 mL	0.3053 mL	0.6105 mL	1.5263 mL
	50 mM	0.0488 mL	0.2442 mL	0.4884 mL	1.2210 mL
	60 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0175 mL
	80 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7631 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6105 mL

Keywords

Ralometostat

3 Cited Publications

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Ralometostat

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

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Anti-Blood Cancer Compound Library

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Drug Repurposing Compound Library Plus

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Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ralometostat

Voir tous les produits spécifiques à Isoform Histone Methyltransferase

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ralometostat

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ralometostat

Voir tous les produits spécifiques à Isoform Histone Methyltransferase

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ralometostat Related Classifications

HY-148419 Related Classifications