UNC2025 (hydrochloride) [2070015-17-5]
Katalog-Nummer HY-12344A-5mg
Size : 5mg
Marke : MedChemExpress
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.
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UNC2025 hydrochloride Chemische Struktur
CAS. Nr. : 2070015-17-5
This product is a controlled substance and not for sale in your territory.
Based on 4 publication(s) in Google Scholar
Other Forms of UNC2025 hydrochloride:
- UNC2025 In-stock
Beschreibung |
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia[1]. |
IC50 & Target |
IC50: 0.74 nM (Mer); 0.8 nM (Flt3)[1] |
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In Vitro |
UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively[1]. UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50 of 2.7 nM in 697 B-ALL cells[1]. UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50 of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells[1].UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells[1]. UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells[2].UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis[1]
Cell Proliferation Assay[1]
Western Blot Analysis[2]
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In Vivo |
UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively[2]. UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Molekulargewicht |
513.12 |
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Formel |
C28H41ClN6O |
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CAS. Nr. |
2070015-17-5 |
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Appearance |
Solid |
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Color |
Light yellow to yellow |
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SMILES |
CN1CCN(CC2=CC=C(C3=CN([C@@H]4CC[C@@H](O)CC4)C5=NC(NCCCC)=NC=C53)C=C2)CC1.06Cl |
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Versand | Room temperature in continental US; may vary elsewhere. |
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Speicherung |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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Lösungsmittel & Löslichkeit |
In Vitro:
H2O : 55 mg/mL (107.19 mM; Need ultrasonic) DMSO : 10 mg/mL (19.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
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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. * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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Reinheit & Dokumentation |
Purity: 99.87% |
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Verweise |
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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 (sealed storage, away from moisture). 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 |
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DMSO / H2O | 1 mM | 1.9489 mL | 9.7443 mL | 19.4886 mL | 48.7215 mL |
5 mM | 0.3898 mL | 1.9489 mL | 3.8977 mL | 9.7443 mL | |
10 mM | 0.1949 mL | 0.9744 mL | 1.9489 mL | 4.8722 mL | |
15 mM | 0.1299 mL | 0.6496 mL | 1.2992 mL | 3.2481 mL | |
H2O | 20 mM | 0.0974 mL | 0.4872 mL | 0.9744 mL | 2.4361 mL |
25 mM | 0.0780 mL | 0.3898 mL | 0.7795 mL | 1.9489 mL | |
30 mM | 0.0650 mL | 0.3248 mL | 0.6496 mL | 1.6241 mL | |
40 mM | 0.0487 mL | 0.2436 mL | 0.4872 mL | 1.2180 mL | |
50 mM | 0.0390 mL | 0.1949 mL | 0.3898 mL | 0.9744 mL | |
60 mM | 0.0325 mL | 0.1624 mL | 0.3248 mL | 0.8120 mL | |
80 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6090 mL | |
100 mM | 0.0195 mL | 0.0974 mL | 0.1949 mL | 0.4872 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.