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Art. -Nr.: HY-184434

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PRMT5-IN-57

PRMT5-IN-57 is an orally active andselective MTA-cooperative PRMT5 inhibitor, with an IC₅₀ of 8.39 nM against PRMT5/MTA complex. PRMT5-IN-57 exhibits potent and selective antiproliferative activity against MTAP-null cancer cells. PRMT5-IN-57 demonstrates significant in vivo antitumor efficacy in an HCT116 MTAP-/- CDX model. PRMT5-IN-57 can be used for the research of MTAP-deleted cancers.

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CAS. Nr.: 3064280-41-4
Formel: C₂₇H₂₃FN₈O
Molecular Weight:494.52

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PRMT5-IN-57 Chemical Structure

CAS. Nr.: 3064280-41-4

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PRMT5

8.39 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-HEP1	IC50	3 nM	Exhibits potent antiproliferative activity against SK-HEP-1 cells. Exhibits potent antiproliferative activity against SK-HEP-1 cells.	42305212
NCI-H1650	IC50	5 nM	Exhibits potent antiproliferative activity against NCI-H1650 cells. Exhibits potent antiproliferative activity against NCI-H1650 cells.	42305212
HCT116 MTAP-de	IC50	6.4 nM	Exhibits potent antiproliferative activity against HCT116 MTAP-del cells. Exhibits potent antiproliferative activity against HCT116 MTAP-del cells.	42305212

In Vitro

PRMT5-IN-57 (Compound 27; up to 20 μM; 10 days) exhibits potent antiproliferative activity against MTAP-null cancer cells, with IC₅₀ values of 6.4 nM (HCT116 MTAP-del), 5.0 nM (NCI-H1650), and 3.0 nM (SK-HEP-1), showing 102-, 392-, and 168-fold selectivity over their respective MTAP-WT counterparts ^[1].
PRMT5-IN-57 (10 min preincubation + 180 min reaction) shows potent PRMT5/MTA enzyme inhibition with an IC₅₀ of 8.39 nM in the MTase-Glo assay^[1].
PRMT5-IN-57 (3-6 nM; 4 days) reduces SDMA levels in MTAP-null cells (HCT116 MTAP-/-, NCI-H1650, and SK-HEP-1) while showing minimal effect on MTAP-WT cells (HCT116 WT, Calu-1, and HepG2) at the same concentrations, as determined by Western blot analysis^[1].
PRMT5-IN-57 (10 μM) shows no inhibitory effect on CYP3A4-midazolam and CYP3A4-testosterone in human liver microsomes^[1].
PRMT5-IN-57 (IC₅₀10 μM) exhibits minimal inhibition of the hERG potassium channel in the Predictor^TM hERG Fluorescence Polarization Assay^[1].
PRMT5-IN-57 demonstrates high metabolic stability in mouse, rat, and human liver microsomes, with half-lives (T_1/2) of 38.5 min, 39.1 min, and 49.6 min, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCT116 MTAP-/-, NCI-H1650, SK-HEP-1 (MTAP-null); HCT116 WT, Calu-1, HepG2 (MTAP-WT) cells
Concentration:

6 nM (HCT116 WT & MTAP-/-), 5 nM (NCI-H1650 & Calu-1), 3 nM (SK-HEP-1 & HepG2)
Incubation Time:

4 days
Result:

Reduced SDMA levels in MTAP-null cells while showing minimal effect on MTAP-WT cells.

Parmacokinetics

Species	Dose	Route	AUC_inf	C_max	MRT_0-inf	T_1/2	T_max	CL	V_d	F
Mice^[1]	10 mg/kg	p.o.	11.455 ng·h/mL	3037 ng/mL	3.32	2.52 h	0.58 h	/	/	/
Rat^[1]	1 mg/kg	i.v.	630 ng·h/mL	530 ng/mL	1.12	0.87 h	0.08 h	1587 mL/h/kg	1.99 L/kg	/
Rat^[1]	5 mg/kg	p.o.	1582 ng·h/mL	724 ng/mL	1.83	1.22 h	0.42 h	/	/	50.2 %

In Vivo

PRMT5-IN-57 (Compound 27; 50 mg/kg; p.o.; once daily; for 21 days) significantly inhibits tumor growth in the HCT116 MTAP-/- CDX model, with superior anti-tumor efficacy compared to MRTX1719 (HY-139611)^[1].

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

Animal Model:

Female BALB/c nude mice (6-8 weeks old, 17-20 g) were subcutaneously injected with 0.1 mL of a suspension containing 1 × 10⁷ HCT116 MTAP-/- cells (1 × 10⁸ cells/mL in serum-free McCoy's 5A medium) into the left axilla^[1].
Dosage:

50 mg/kg
Administration:

Oral gavage (p.o.); once daily; 21 days (starting when tumors reached a mean volume of approximately 150 mm³)
Result:

Significantly suppressed tumor growth with a tumor growth inhibition (TGI) of 74% and a mean tumor volume of 348 mm³ at the study endpoint, compared to 1362 mm³ in the vehicle group.
Reduced mean tumor weight to 0.24 g, compared to 1.04 g in the vehicle group and 0.39 g in the MRTX1719 group.
Demonstrated superior antitumor efficacy compared to the clinical benchmark MRTX1719 at the same dose, which achieved 63% TGI.
No significant body weight loss was observed.

Chemical Information

CAS. Nr. 3064280-41-4
Molecular Weight 494.52
Formel C₂₇H₂₃FN₈O
SMILES

CN1C=C(C=N1)C#CC2=CC=C(N=C2)CN(C3CC3)C(C4=C(C=C5N=C(C6=C(N(N=C6)C)C5=C4)N)F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Huang C, et al. Structure-Guided Discovery of Novel Highly Potent and Selective MTA-Cooperative PRMT5 Inhibitors. ACS Med Chem Lett. 2026 Jun 3;17(6):1275-1284. [Content Brief]

Calculators

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)}

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.

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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PRMT5-IN-57

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PRMT5-IN-57 Related Classifications

HY-184434 Related Classifications