SHR902275
Based on 1 Customer Validation
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAFwt, and bRAFV600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 2695506-82-0
- Formula: C26H23F3N4O4
- Molecular Weight:512.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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C-Raf 1.6 nM (IC50) |
BRafV600E 5.7 nM (IC50) |
BRAFWT 10 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | GI50 |
0.17 μM
Compound: 33; SHR902275
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Cytotoxicity against human A-375 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
Cytotoxicity against human A-375 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
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[PMID: 34906761] |
| Calu-6 | GI50 |
0.4 μM
Compound: 33; SHR902275
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Cytotoxicity against human Calu-6 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
Cytotoxicity against human Calu-6 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
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[PMID: 34906761] |
| NCI-H358 | GI50 |
1.4 μM
Compound: 33; SHR902275
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Cytotoxicity against human NCI-H358 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
Cytotoxicity against human NCI-H358 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
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[PMID: 34906761] |
| SK-MEL-2 | GI50 |
0.32 μM
Compound: 33; SHR902275
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Cytotoxicity against human SK-MEL-2 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
Cytotoxicity against human SK-MEL-2 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay
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[PMID: 34906761] |
Chemical Information
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CAS No. 2695506-82-0
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Appearance Solid
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Molecular Weight 512.48
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Formula C26H23F3N4O4
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Color White to off-white
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SMILES
O=C(C1=NN=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(C3=CC4=C(NC(CC5(CCOCC5)O4)=O)C=C3)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (195.13 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
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 (4.88 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.
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.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 1.9513 mL | 9.7565 mL | 19.5130 mL | 48.7824 mL |
| 5 mM | 0.3903 mL | 1.9513 mL | 3.9026 mL | 9.7565 mL | |
| 10 mM | 0.1951 mL | 0.9756 mL | 1.9513 mL | 4.8782 mL | |
| 15 mM | 0.1301 mL | 0.6504 mL | 1.3009 mL | 3.2522 mL | |
| 20 mM | 0.0976 mL | 0.4878 mL | 0.9756 mL | 2.4391 mL | |
| 25 mM | 0.0781 mL | 0.3903 mL | 0.7805 mL | 1.9513 mL | |
| 30 mM | 0.0650 mL | 0.3252 mL | 0.6504 mL | 1.6261 mL | |
| 40 mM | 0.0488 mL | 0.2439 mL | 0.4878 mL | 1.2196 mL | |
| 50 mM | 0.0390 mL | 0.1951 mL | 0.3903 mL | 0.9756 mL | |
| 60 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8130 mL | |
| 80 mM | 0.0244 mL | 0.1220 mL | 0.2439 mL | 0.6098 mL | |
| 100 mM | 0.0195 mL | 0.0976 mL | 0.1951 mL | 0.4878 mL |
SHR902275 Related Classifications
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