[CAS NO. 2070015-17-5] UNC2025 HCl
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PRODUCTS SPECIFICATIONS [2070015-17-5]
Catalog
SLK-S7576
Brand
Selleck
CAS
2070015-17-5
DESCRIPTION [2070015-17-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 513.12 |
| Molecular Formula | C28H41ClN6O |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9489 mL | 9.7443 mL | 19.4886 mL |
| 5 mM | 0.3898 mL | 1.9489 mL | 3.8977 mL |
| 10 mM | 0.1949 mL | 0.9744 mL | 1.9489 mL |
| 50 mM | 0.0390 mL | 0.1949 mL | 0.3898 mL |
Description
UNC2025 HCl is a potent and orally bioavailable dual inhibitor with of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
Targets
In vitro
In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation.
In vivo
In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth.
References
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