RAF709
Based on 7 publication(s) in Google Scholar
RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.92%
- CAS. Nr.: 1628838-42-5
- Formel: C28H29F3N4O4
- Molecular Weight:542.55
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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HY-L009
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Publications Citing Use of MedChemExpress (MCE) RAF709
More- Cancer Lett. 2023 Feb 28:555:216029. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Mar 5;116(10):4508-4517. [Abstract]
- Endocrinology. 2023 Mar 13;164(5):bqad042. [Abstract]
- In Vitro Cell Dev Biol Anim. 2021 Sep;57(8):817-824. [Abstract]
- Research Square Print. December 21st, 2022.
- Ann Transl Med. 2022 Mar;10(6):314. [Abstract]
- Research Square Preprint. 2020 Sep.
Biologische Aktivität
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CRAF 0.5 nM (IC50) |
Braf 0.4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Calu-6 | EC50 |
0.95 μM
Compound: 14; RAF709
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Antiproliferative activity against human Calu6 cells harboring KRAS Q61K mutant assessed as reduction cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human Calu6 cells harboring KRAS Q61K mutant assessed as reduction cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 28557458] |
RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 μM. In cellular assays, the dose-response of pMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 μM with minimal paradoxical activation and inhibition of proliferation with EC50=0.95 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1628838-42-5
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Appearance Solid
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Molecular Weight 542.55
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Formel C28H29F3N4O4
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Color White to off-white
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SMILES
O=C(NC1=CN=C(C)C(C2=CC(N3CCOCC3)=C(OC4CCOCC4)N=C2)=C1)C5=CC=CC(C(F)(F)F)=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Lett
SHP2 inhibition mitigates adaptive resistance to MEK inhibitors in KRAS-mutant gastric cancer through the suppression of KSR1 activity. [Abstract]2023 Feb 28:555:216029. PMID: 36493900 -
Proc Natl Acad Sci U S A
2019 Mar 5;116(10):4508-4517. PMID: 30709910 -
Endocrinology
2023 Mar 13;164(5):bqad042. PMID: 36929849 -
In Vitro Cell Dev Biol Anim
MicroRNA-7a inhibits Isl1 expression to regulate insulin secretion by targeting Raf1 and Mapkap1 in NIT-1 cells. [Abstract]2021 Sep;57(8):817-824. PMID: 34713362 -
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Ann Transl Med
RAF1 mediates the FSH signaling pathway as a downstream molecule to stimulate estradiol synthesis and secretion in mouse ovarian granulosa cells. [Abstract]2022 Mar;10(6):314. PMID: 35433952 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (184.31 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (4.61 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.61 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Nishiguchi GA, et al. Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers. J Med Chem. 2017 Jun 22;60(12):4869-4881. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8431 mL | 9.2157 mL | 18.4315 mL | 46.0787 mL |
| 5 mM | 0.3686 mL | 1.8431 mL | 3.6863 mL | 9.2157 mL | |
| 10 mM | 0.1843 mL | 0.9216 mL | 1.8431 mL | 4.6079 mL | |
| 15 mM | 0.1229 mL | 0.6144 mL | 1.2288 mL | 3.0719 mL | |
| 20 mM | 0.0922 mL | 0.4608 mL | 0.9216 mL | 2.3039 mL | |
| 25 mM | 0.0737 mL | 0.3686 mL | 0.7373 mL | 1.8431 mL | |
| 30 mM | 0.0614 mL | 0.3072 mL | 0.6144 mL | 1.5360 mL | |
| 40 mM | 0.0461 mL | 0.2304 mL | 0.4608 mL | 1.1520 mL | |
| 50 mM | 0.0369 mL | 0.1843 mL | 0.3686 mL | 0.9216 mL | |
| 60 mM | 0.0307 mL | 0.1536 mL | 0.3072 mL | 0.7680 mL | |
| 80 mM | 0.0230 mL | 0.1152 mL | 0.2304 mL | 0.5760 mL | |
| 100 mM | 0.0184 mL | 0.0922 mL | 0.1843 mL | 0.4608 mL |
RAF709 Related Classifications
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