SHY-855
Based on 1 Customer Validation
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer.
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- Purity : 98.54%
- CAS No.: 2446485-15-8
- 화학식: C26H24ClN5O2S
- 분자량:506.02
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보관: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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All MEK Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
K-Ras WT 2.5 μM (IC50) |
KRas G12D 2.5 μM (IC50) |
KRas G12C 3 μM (IC50) |
KRas Q61H 5 μM (IC50) |
MEK |
ERK1 |
ERK2 |
Akt |
In Vitro
SHY-855 competes with GTP binding to K-Ras WT, the G12D, G12C, and Q61H mutants, as well as Rac-1, Rho-A, Rab5, and Rab35 with IC50s of 2.5, 2.5, 3, 5, 2.5, 2.5, 0.3 and 0.6 μM[1].
SHY-855 (72 h) exhibits potent antiproliferative effects in multiple tumor cell lines, including pancreatic cancer (PANC-1, MIA PaCa-2, BxPC3) and non-small cell lung cancer (NCI-H1975, A549, NCI-H1299), with IC50 values ranging from 0.75-2.9 μM[1].
SHY-855 (0.3-10 μM, 6 h) significantly inhibits the phosphorylation of key signaling molecules induced by EGF in PANC-1, MIA PaCa-2 and NCI-H1975 cells[1].
SHY-855 (1.25-10 μM, 6 h) inhibits Ras-GTP complex formation with an IC50 of 1-3 μM in PANC-1, MIA PaCa-2 and NCI-H1975 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:PANC-1, MIA PaCa-2 and NCI-H1975 cells
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Concentration:0.3, 0.6, 1.25, 2.5, 5 and 10 μM
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Incubation Time:6 h
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Result:Inhibited phosphorylation and activation of MEK, Erk1/2, and Akt in PANC-1, MIA PaCa-2, and NCIH1975 cell lines in a dose-dependent manner with similar IC50 values (about 1-3 μM).
Prevented Ras-GTP complex formation with IC50 values in the range of 1 to 3 μM.
Chemical Information
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CAS No. 2446485-15-8
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Appearance Solid
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분자량 506.02
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화학식 C26H24ClN5O2S
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Color Light yellow to light brown
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SMILES
COCCNC1=NC(C2=NC=CN2C)=NC3=C1C(C4=CC=CC=C4)=C(S3)C5=C(C(OC)=CC=C5)Cl
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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 : 33.33 mg/mL (65.87 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)
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.
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.
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.
Protocol
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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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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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
순도&문서
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Data Sheet (279 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 | 1.9762 mL | 9.8810 mL | 19.7621 mL | 49.4052 mL |
| 5 mM | 0.3952 mL | 1.9762 mL | 3.9524 mL | 9.8810 mL | |
| 10 mM | 0.1976 mL | 0.9881 mL | 1.9762 mL | 4.9405 mL | |
| 15 mM | 0.1317 mL | 0.6587 mL | 1.3175 mL | 3.2937 mL | |
| 20 mM | 0.0988 mL | 0.4941 mL | 0.9881 mL | 2.4703 mL | |
| 25 mM | 0.0790 mL | 0.3952 mL | 0.7905 mL | 1.9762 mL | |
| 30 mM | 0.0659 mL | 0.3294 mL | 0.6587 mL | 1.6468 mL | |
| 40 mM | 0.0494 mL | 0.2470 mL | 0.4941 mL | 1.2351 mL | |
| 50 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.9881 mL | |
| 60 mM | 0.0329 mL | 0.1647 mL | 0.3294 mL | 0.8234 mL |
SHY-855 Related Classifications
HY-178194 Related Classifications
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