UNC2025 |
| Catalog No.GC15556 |
UNC2025는 각각 0.74nM 및 0.8nM의 IC50 값을 갖는 강력하고 ATP 경쟁적이며 경구 활성이 높은 Mer/Flt3 억제제입니다. UNC2025는 Axl에 비해 MERTK에 대해 >45배 선택도입니다(IC50= 122 nM; Ki= 13.3 nM). UNC2025는 우수한 PK 특성을 나타내어 급성 백혈병 조사에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1429881-91-3
Sample solution is provided at 25 µL, 10mM.
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UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with the IC50 value of 0.8/0.74 nM for Mer/Flt3[1].
In vitro: In duplicate versus 305 kinases at Carna Biosciences using a microcapillary electrophoresis assay, UNC2025 inhibited Mer and Flt3 with the greatest potency. In B-ALL 697 cell lysates using the ATP ActivX probe assay, UNC2025 inhhibited the activity of Mer with an IC50 of 0.05 nM. In 697 B-ALL cells, UNC2025 potently inhibited Mer phosphorylation with an IC50 of 2.7 nM. Similarly, in Flt3-ITD positive Molm-14 acute myeloid leukemia cells, treatment with UNC2025 decreased phosphorylation of Flt3 with an IC50 of 14 nM. In soft agar cultures of the A549 NSCLC and Molm-14 AML cell lines, incubation withUNC2025 significantly inhibited colony formation, which was known to depend on Merand Flt3,respectively, for optimal expression of oncogenic phenotypes. Much higher concentrations of UNC2025 were required to effectively inhibit phosphorylation of Axl (IC50 = 122 nM) and Tyro3 (IC50 = 301 nM)[1].
In vivo: In mice with human leukemia xenografts, a single dose of UNC2025 (3 mg/kg) administered orally was sufficient to decrease Merphospho-protein levels in bone marrow leukemia cells by greater than 90% [1].
Reference:
[1]. Zhang W1,DeRyckere D,Hunter D,Liu J,Stashko MA,Minson KA, et,al. UNC2025, a potent and orally bioavailableMER/FLT3dual inhibitor.J Med Chem.2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.
| Cell experiment [1]: | |
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Cell lines |
697 B-ALL cells; Flt3-ITD positive Molm-14 acute myeloid leukemia cells; A549 NSCLC cells |
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Preparation method |
The solubility of this compound in DMSO is >23.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0-300 nM; 1 h |
|
Applications |
In 697 B-ALL cells, UNC2025 inhibited Mer phosphorylation with IC50 value of 2.7 nM. In Flt3-ITD positive Molm-14 acute myeloid leukemia cells, UNC2025 inhibited phosphorylation of Flt3 with an IC50 of 14 nM. In A549 NSCLC cells and Molm-14 AML cells, UNC2025 inhibited colony formation in Mer-dependent and Flt3-dependent way. |
| Animal experiment [1]: | |
|
Animal models |
mice with human leukemia xenografts |
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Dosage form |
3 mg/kg; orally |
|
Application |
In mice with human leukemia xenografts, UNC2025 inhibited Mer phosphor-protein levels in bone marrow leukemia cells by greater than 90%. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Zhang W1,DeRyckere D,Hunter D,Liu J,Stashko MA,Minson KA, et,al. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. J Med Chem.2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6. | |
| Cas No. | 1429881-91-3 | SDF | |
| Chemical Name | (1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol | ||
| Canonical SMILES | CN1CCN(CC2=CC=C(C3=CN([C@@H]4CC[C@@H](O)CC4)C5=NC(NCCCC)=NC=C35)C=C2)CC1 | ||
| Formula | C28H40N6O | M.Wt | 476.66 |
| Solubility | ≥ 23.85mg/mL in DMSO | Storage | Desiccate 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 | 2.0979 mL | 10.4897 mL | 20.9793 mL |
| 5 mM | 0.4196 mL | 2.0979 mL | 4.1959 mL |
| 10 mM | 0.2098 mL | 1.049 mL | 2.0979 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: >99.50%
- 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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