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UNC2025 (mrx-6313)(IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $33 | In Stock | |
5 mg | $52 | In Stock | |
10 mg | $85 | In Stock | |
25 mg | $126 | In Stock | |
50 mg | $207 | In Stock | |
100 mg | $369 | In Stock | |
1 mL x 10 mM (in DMSO) | $54 | In Stock |
Description | UNC2025 (mrx-6313)(IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3. |
Targets&IC50 | Mer:0.74 nM, FLT3:0.8 nM |
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. [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 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. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2] |
Alias | UNC-2025, UNC 2025, mrx-6313 |
Molecular Weight | 476.66 |
Formula | C28H40N6O |
Cas No. | 1429881-91-3 |
Smiles | CCCCNc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccc(CN2CCN(C)CC2)cc1 |
Relative Density. | 1.24 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | H2O: Insoluble Ethanol: 8 mg/mL (15.59 mM), Heating is recommended. DMSO: 6.25 mg/mL (13.11 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO/Ethanol
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