| CAS NO: | 2070015-17-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 513.12 |
|---|---|
| Formula | C28H41ClN6O |
| CAS No. | 2070015-17-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 25 mg/mL (48.7 mM) |
| Water: 100 mg/mL (194.9 mM) | |
| Ethanol: 8 mg/mL (15.6 mM) | |
| SMILES | CN1CCN(CC2=CC=C(C3=CN([C@@H]4CC[C@@H](O)CC4)C5=NC(NCCCC)=NC=C53)C=C2)CC1.[H]Cl |
| Synonyms | UNC-2025 HCl; UNC-2025 hydrochloride; UNC2025 hydrochloride; UNC 2025 HCl; UNC2025 HCl; UNC 2025 hydrochloride; UNC-2025, UNC2025, UNC 2025 |
| In Vitro | In vitro activity: 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. Kinase Assay: UNC2025 hydrochloride is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3. Cell Assay: 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 |
| Animal model | NOD/SCID/gamma mice bearing 697 acute leukemia tumor |
| Formulation & Dosage | Formulated in 0.5% (w/v) NaCMC with 0.1% (v/v) Tween-80 in water; 3 mg/kg; Oral gavage |
| References | J Med Chem. 2014 Aug 28;57(16):7031-41; Mol Cancer Ther. 2015 Sep;14(9):2014-22. |
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