|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C28H41ClN6O |
|||
| Molecular Weight | 513.12 | CAS No. | 2070015-17-5 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (194.88 mM) | |
| Ethanol | 60 mg/mL (116.93 mM) | |||
| Water | Insoluble | |||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | 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. | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 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. [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] |
Protocol (from reference)
| Animal Study:[1] |
|
|---|
References
|
Selleck's UNC2025 HCl has been cited by 9 publications
| Lymph node medulla regulates the spatiotemporal unfolding of resident dendritic cell networks [ Immunity, 2023, 56(8):1778-1793.e10] | PubMed: 37463581 |
| Early stress-induced impaired microglial pruning of excitatory synapses on immature CRH-expressing neurons provokes aberrant adult stress responses [ Cell Rep, 2022, 38(13):110600] | PubMed: 35354026 |
| EWSR1-WT1 Target Genes and Therapeutic Options Identified in a Novel DSRCT In Vitro Model [ Cancers (Basel), 2021, 13(23)6072] | PubMed: 34885181 |
| In vivo microscopy reveals macrophage polarization locally promotes coherent microtubule dynamics in migrating cancer cells [ Nat Commun, 2020, 11(1):3521] | PubMed: 32665556 |
| Expression of TAM-R in Human Immune Cells and Unique Regulatory Function of MerTK in IL-10 Production by Tolerogenic DC [ Front Immunol, 2020, 11:564133] | PubMed: 33101282 |
| TLR7/8-agonist-loaded Nanoparticles Promote the Polarization of Tumour-Associated Macrophages to Enhance Cancer Immunotherapy [ Nat Biomed Eng, 2018, 2(8):578-588] | PubMed: 31015631 |
| Changes in cell morphology guide identification of tubulin as the off-target for protein kinase inhibitors [Hoque M, et al. Pharmacol Res, 2018, 134:166-178] | PubMed: 29944980 |
| MERTK Mediates Intrinsic and Adaptive Resistance to AXL-targeting Agents. [ Mol Cancer Ther, 2018, 17(11):2297-2308] | PubMed: 30093568 |
| New insights into Notch1 regulation of the PI3K-AKT-mTOR1 signaling axis: targeted therapy of γ-secretase inhibitor resistant T-cell acute lymphoblastic leukemia [ Cell Signal, 2014, 26(1):149-61] | PubMed: 24140475 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.