Uplarafenib
Based on 1 Customer Validation
Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. Uplarafenib shows antitumor activity.
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- Purity : 99.63%
- CAS No.: 1425485-87-5
- 화학식: C22H21F3N4O4S
- 분자량:494.49
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
IC50 & Target
[1]|
BRAF-V600E < 50 nM (IC50) |
Braf 50-100 nM (IC50) |
In Vitro
Uplarafenib (Compound C09) (1 μM) shows more than 89% inhibition against BRAF and BRAF V600E[1].
Uplarafenib shows an IC50 between 50 and 100 nM against BRAF, less than 50 nM against BRAF V600E[1].
Uplarafenib (72 h) inhibits A375 and SK-MEL-28 cells growth but not CHL-1 and SK-MEL-31 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A375, SK-MEL-28, SK-MEL-31 and CHL-1
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Concentration:
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Incubation Time:72 h
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Result:Showed inhibition with IC50s less than 500 nM against A375 and SK-MEL-28 cells, and showed no inhibition against CHL-1 and SK-MEL-31.
Chemical Information
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CAS No. 1425485-87-5
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Appearance Solid
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분자량 494.49
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화학식 C22H21F3N4O4S
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Color Light yellow to yellow
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SMILES
O=C(C1=C(F)C(NS(=O)(CCC)=O)=CC(F)=C1F)C2=CC=C3N=CC(N4CCOCC4)=NC3=C2
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Synonyms
B-Raf IN 10
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (202.23 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)
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
순도&문서
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Data Sheet (270 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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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 | 2.0223 mL | 10.1114 mL | 20.2229 mL | 50.5571 mL |
| 5 mM | 0.4045 mL | 2.0223 mL | 4.0446 mL | 10.1114 mL | |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0223 mL | 5.0557 mL | |
| 15 mM | 0.1348 mL | 0.6741 mL | 1.3482 mL | 3.3705 mL | |
| 20 mM | 0.1011 mL | 0.5056 mL | 1.0111 mL | 2.5279 mL | |
| 25 mM | 0.0809 mL | 0.4045 mL | 0.8089 mL | 2.0223 mL | |
| 30 mM | 0.0674 mL | 0.3370 mL | 0.6741 mL | 1.6852 mL | |
| 40 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2639 mL | |
| 50 mM | 0.0404 mL | 0.2022 mL | 0.4045 mL | 1.0111 mL | |
| 60 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8426 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2528 mL | 0.6320 mL | |
| 100 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5056 mL |