AMG-47A |
| Catalog No.GC17669 |
destabilizer of the KRAS oncoprotein
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 882663-88-9
Sample solution is provided at 25 µL, 10mM.
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AMG-47A is a destabilizer of the KRAS oncoprotein.
Ras is a small GTPase that involves in numerous cellular signaling pathways governing growth, survival, and motility. In humans, there are three Ras genes: KRAS, HRAS, and NRAS. Oncogenic
mutations in all three Ras family members have been identified in human cancers. In particular, KRAS is one of the most frequently mutated oncogenes across cancer types.[1]
In the HeLa EGFP-KRASG12V cells, 48-hour treatment of AMG-47a has a 30–40% decrease in EGFP signal, treating cells for 3 and 5 days shows the similar results. AMG-47a selectively affects EGFP-KRASG12V protein levels. AMG-47a also has a mild effect on EGFP-KRASG12V protein levels after three days. The loss of EGFP-KRASG12V signal plateaus at 50% for AMG-47a. [1]
References:
1. Carver J, Dexheimer TS, Hsu D et al. A high-throughput assay for small molecule destabilizers of the KRASoncoprotein. PLoS One. 2014 Aug 5;9(8):e103836
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| Cas No. | 882663-88-9 | SDF | |
| Chemical Name | (Z)-4-methyl-3-((E)-2-((2-morpholinoethyl)imino)-2,3-dihydroquinazolin-6-yl)-N-(3-(trifluoromethyl)phenyl)benzimidic acid | ||
| Canonical SMILES | CC1=C(C(C=CC2=N/3)=CC2=CNC3=N/CCN4CCOCC4)C=C(/C(O)=N/C5=CC=CC(C(F)(F)F)=C5)C=C1 | ||
| Formula | C29H28F3N5O2 | M.Wt | 535.56 |
| Solubility | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8672 mL | 9.336 mL | 18.672 mL |
| 5 mM | 0.3734 mL | 1.8672 mL | 3.7344 mL |
| 10 mM | 0.1867 mL | 0.9336 mL | 1.8672 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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