UNC2250 |
| Catalog No.GC17793 |
UNC2250은 1.7nM의 IC50, 밀접하게 관련된 키나제 Axl/Tyro3에 비해 약 160배 및 60배 선택성을 갖는 강력하고 선택적인 Mer 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1493694-70-4
Sample solution is provided at 25 µL, 10mM.
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UNC2250 is a highly selective inhibitor of Mer receptor tyrosine kinase with IC50 value of 1.7nM [1].
UNC2250 shows a potent inhibitory activity against Mer with IC50 value of 1.7nM. The IC50 values for other TAM kinases such as Axl and Tyro3 are 270nM and 100nM, respectively. In addition, UNC2250 shows no significant inhibition of a panel of 30 other kinases. In cell-based assays, UNC2250 inhibits the phosphorylation of Mer with IC50 value of 9.8nM in B-ALL cells. It also prevents the colony formation both in BT-12 cell lines and in Colo699 NSCLC cell lines. Furthermore, UNC2250 is proved to have a moderate half-life, clearance, distribution volume and good oral bioavailability [1].
References:
[1] Zhang W, Zhang D, Stashko M A, et al. Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors. Journal of medicinal chemistry, 2013, 56(23): 9683-9692.
| Cas No. | 1493694-70-4 | SDF | |
| Chemical Name | 4-[[2-(butylamino)-5-[5-(morpholin-4-ylmethyl)pyridin-2-yl]pyrimidin-4-yl]amino]cyclohexan-1-ol | ||
| Canonical SMILES | CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C3=NC=C(C=C3)CN4CCOCC4 | ||
| Formula | C24H36N6O2 | M.Wt | 440.58 |
| Solubility | ≥ 22.05mg/mL in DMSO with gentle warming | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2697 mL | 11.3487 mL | 22.6974 mL |
| 5 mM | 0.4539 mL | 2.2697 mL | 4.5395 mL |
| 10 mM | 0.227 mL | 1.1349 mL | 2.2697 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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: >98.00%
- 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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