ML 281 |
| カタログ番号GC11380 |
ML 281 は、IC50 が 14 nM の強力で選択的な STK33 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1404437-62-2
Sample solution is provided at 25 µL, 10mM.
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ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM. ML281 showed a 550-fold selectivity over AurB and greater than 700-fold selectivity over PKA.target: STK33IC50: 14 nM [1]ML281 showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors. Even at the highest concentration tested (10 μM), ML281 had no effect on the viability of KRAS-dependent cancer cells. [2]
ML281 (10 μM; 72 hours) suppresses cell viability of NCI-H446 cells[3].
References:
[1]. We wer M et al. A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett, 2012 Dec 13, 3(12):1034-1038.
[2]. Sun EL, et al. Knockdown of human serine/threonine kinase 33 suppresses human small cell lung carcinoma by blocking RPS6/BAD signaling transduction. Neoplasma. 2017;64(6):869-879.
[3]. Spoonamore J et al. Screen for Inhibitors of STK33 Kinase Activity. National Center for Biotechnology Information (US); 2010-2011 Dec 16.
| Cas No. | 1404437-62-2 | SDF | |
| Chemical Name | N-(4-isopropyl-2-(3-oxo-3,4-dihydroquinoxalin-2-yl)phenyl)thiophene-2-carboxamide | ||
| Canonical SMILES | CC(C1=CC(C2=NC3=CC=CC=C3NC2=O)=C(NC(C4=CC=CS4)=O)C=C1)C | ||
| Formula | C22H19N3O2S | M.Wt | 389.47 |
| 溶解度 | DMF: 33 mg/ml,DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml,DMSO: 20 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5676 mL | 12.838 mL | 25.6759 mL |
| 5 mM | 513.5 μL | 2.5676 mL | 5.1352 mL |
| 10 mM | 256.8 μL | 1.2838 mL | 2.5676 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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