AZD3470
Based on 1 Customer Validation
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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- Pureza : 99.74%
- No. CAS: 2918814-97-6
- Fòrmula: C23H19F2N5O2
- Peso molecular:435.43
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Almacenamiento:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PRMT5 |
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.
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Cell Line:NCI-H838 CAAP1 KO/WT isogenic NSCLC cell lines, HCC15 CAAP1 KO/WT isogenic NSCLC cell lines
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Concentration:1 µM
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Incubation Time:96 h
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Result:Showed a higher percentage of cells in the G2/M phase compared to respective CAAP1 WT cells.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice (female) were established by subcutaneous (SC) injection of 5×106 NCI-H838 cells[2]
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Dosage:1 mg/kg; 10 mg/kg; 100 mg/kg
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Administration:p.o.; BID; 21 days
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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
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No. CAS 2918814-97-6
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Appearance Solid
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Peso molecular 435.43
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Fòrmula C23H19F2N5O2
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Color White to off-white
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SMILES
FC1=CC(NC(CN2[C@]3(C4=C(C2=O)C=C(F)C=C4)CCN(CC#CC)C3=O)=C5)=C5N=C1N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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 (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.
| 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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