Company Name: |
DC Chemicals
|
Tel: |
021-58447131 13564518121 |
Email: |
sales@dcchemicals.com |
Products Intro: |
Product Name:UNC-2025 HCl CAS:2070015-17-5 Purity:98% HPLC Package:100mg,250mg,1g
|
Company Name: |
InvivoChem
|
Tel: |
13549236410 |
Email: |
sales@invivochem.cn |
Products Intro: |
Product Name:UNC-2025 HCl CAS:2070015-17-5 Purity:98% HPLC Package:1mg Remarks:V0586
|
|
| UNC2025 HCI Basic information |
| UNC2025 HCI Chemical Properties |
storage temp. | Store at -20°C | solubility | DMSO: 25 mg/mL (48.72 mM);Ethanol: 8 mg/mL (15.59 mM) | form | Solid | color | Light yellow to yellow | Water Solubility | Water: 100 mg/mL (194.89 mM) |
| UNC2025 HCI Usage And Synthesis |
Biological Activity | UNC2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
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. [1] 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. [2]
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. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2] | References | [1] Zhang W, et al. J Med Chem. 2014, 57(16), 7031-7041.
[2] Cummings CT, et al. Mol Cancer Ther. 2015, 14(9), 2014-2022. |
| UNC2025 HCI Preparation Products And Raw materials |
|