Art. -Nr.: HY-158143

AZD3470

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AZD3470 is an orally active MTA-cooperative PRMT5 inhibitor, selective for MTAP-deficient tumors. AZD3470 induces cell cycle G₂/M phase alterations, DNA damage, apoptosis, and symmetric dimethylarginine reduction. AZD3470 alters alternative splicing, increases skipped exon events in DNA repair and cell cycle pathways, and inhibits cancer cell proliferation and tumor growth. AZD3470 can be used for the research of non-small cell lung cancer and MTAP-deleted solid tumors.

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Reinheit: 99.74%
CAS. Nr.: 2918814-97-6
Formel: C₂₃H₁₉F₂N₅O₂
Molecular Weight:435.43

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

AZD3470 Chemical Structure

CAS. Nr.: 2918814-97-6

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PRMT5

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

AZD3470 (1 µM; 96 h) treatment of NCI-H838 and HCC15 CAAP1 null NSCLC cells results in a higher proportion of cells in the G2/M phase compared to CAAP1 wild-type NCI-H838 and HCC15 NSCLC cells^[1].
AZD3470 (dose-dependent) HCC15 CAAP1 null NSCLC cells show dose-dependent increases in alternative splicing events (enriched in DNA repair and cell cycle pathways) following AZD3470 treatment compared to CAAP1 wild-type HCC15 NSCLC cells^[1].
AZD3470 (dose-response range; 48 h) exhibits 37-fold MTA-cooperative PRMT5 inhibition, potently reducing SDMA levels in HCT116 MTAP KO cells with an IC₅₀ of 5.4 nM, while being far less potent (IC₅₀ 198 nM) in HCT116 MTAP WT cells^[2].
AZD3470 (5 days) inhibits proliferation of HCT116 MTAP KO cells with an IC₅₀ of 170 nM, demonstrating 50-fold selectivity over HCT116 MTAP WT cells (IC₅₀ 8.53 μM) after 5 days of treatment^[2].
AZD3470 (7 days) inhibits proliferation of MTAP-null NCI-H838 cells with an IC₅₀ of 284 nM after 7 days of treatment^[2].

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

Cell Cycle Analysis^[1]

Cell Line:

NCI-H838 CAAP1 KO/WT isogenic NSCLC cell lines, HCC15 CAAP1 KO/WT isogenic NSCLC cell lines
Concentration:

1 µM
Incubation Time:

96 h
Result:

Showed a higher percentage of cells in the G2/M phase compared to respective CAAP1 WT cells.

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	Bioavailability
Rat^[2]	0.5 mg/kg	i.v.	28 mL/min/kg	1.8 L/kg	2.9 h	/
Rat^[2]	1.0 mg/kg	p.o.	/	/	2.9 h	79 %

In Vivo

AZD3470 (compound 14) (1-100 mg/kg; p.o.; BID; 21 days) induces dose-dependent tumor SDMA depletion in MTAP-null NCI-H838 xenografts, with the 100 mg/kg BID dose delivering 94% tumor growth inhibition and 98.7% SDMA reduction while maintaining tolerability^[2].

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

Animal Model:

Nude mice (female) were established by subcutaneous (SC) injection of 5×10⁶ NCI-H838 cells^[2]
Dosage:

1 mg/kg; 10 mg/kg; 100 mg/kg
Administration:

p.o.; BID; 21 days
Result:

Reduced relative tumor SDMA levels by 83.1% compared to vehicle; achieved 17% tumor growth inhibition (TGI).
Reduced relative tumor SDMA levels by 98.2% compared to vehicle; achieved 17% TGI.
Reduced relative tumor SDMA levels by 98.7% compared to vehicle; achieved 94% TGI.
Maintained mouse body weight and showed no clinical signs detected during treatment.

Chemical Information

CAS. Nr. 2918814-97-6
Appearance Solid
Molecular Weight 435.43
Formel C₂₃H₁₉F₂N₅O₂
Color White to off-white
SMILES

FC1=CC(NC(CN2[C@]3(C4=C(C2=O)C=C(F)C=C4)CCN(CC#CC)C3=O)=C5)=C5N=C1N
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (229.66 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

2.2966 mL

11.4829 mL

22.9658 mL

5 mM

0.4593 mL

2.2966 mL

4.5932 mL

10 mM

0.2297 mL

1.1483 mL

2.2966 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 (protect from light, stored under nitrogen). 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: ≥ 2.5 mg/mL (5.74 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.74 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)
Handling Instructions (2659 KB)

Verweise

[1].
Jelena Urosevic, et al. Abstract 4489: CAAP1 loss uncovers vulnerability of MTAP-
deficient NSCLC to PRMT5 inhibition with AZD3470. Cancer Res (2026) 86 (7_Supplement): 4489.

[2]. Smith JM, et al. Use of Human Dose Prediction Metrics to Enable Discovery of AZD3470, an MTA-Cooperative PRMT5 Inhibitor in Clinical Evaluation. J Med Chem. Published online May 22, 2026. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2966 mL	11.4829 mL	22.9658 mL	57.4145 mL
	5 mM	0.4593 mL	2.2966 mL	4.5932 mL	11.4829 mL
	10 mM	0.2297 mL	1.1483 mL	2.2966 mL	5.7415 mL
	15 mM	0.1531 mL	0.7655 mL	1.5311 mL	3.8276 mL
	20 mM	0.1148 mL	0.5741 mL	1.1483 mL	2.8707 mL
	25 mM	0.0919 mL	0.4593 mL	0.9186 mL	2.2966 mL
	30 mM	0.0766 mL	0.3828 mL	0.7655 mL	1.9138 mL
	40 mM	0.0574 mL	0.2871 mL	0.5741 mL	1.4354 mL
	50 mM	0.0459 mL	0.2297 mL	0.4593 mL	1.1483 mL
	60 mM	0.0383 mL	0.1914 mL	0.3828 mL	0.9569 mL
	80 mM	0.0287 mL	0.1435 mL	0.2871 mL	0.7177 mL
	100 mM	0.0230 mL	0.1148 mL	0.2297 mL	0.5741 mL

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AZD3470

MCE Bioactive Compound Library

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZD3470 Related Classifications

HY-158143 Related Classifications