- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Inhibitors
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 1493764-08-1] UNC2881
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15798 |
| Brand: | MCE |
| CAS: | 1493764-08-1 |
Overview
| MDL | MFCD28142814 |
|---|---|
| Molecular Weight | 463.58 |
| Molecular Formula | C25H33N7O2 |
| SMILES | CCCCNC1=NC(N[C@H]2CC[C@H](O)CC2)=C(C(NCC3=CC=C(N4C=NC=C4)C=C3)=O)C=N1 |
Summary
UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC 50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC 50 s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research [1] .
IC50 & Target
IC50: 4.3 nM (Mer), 360 nM (Axl), 250 nM (Tyro) [1]
In Vitro
UNC2881 (compound 23) (0-1000 nM; 1 h) block ligand-stimulated activation of a chimeric EGFR-MerTK. UNC2881 also inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells
[1]
.
UNC2881 (3 μM; 1 h) suppresses platelet aggregation by greater than 25% in human platelet-rich plasma in response to stimulation with fibrillar type I equine collagen
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | 32D cells |
| Concentration: | 0, 10, 30, 100, 300, 1000 nM |
| Incubation Time: | 1 hour; prior to stimulation with 100 ng/mL EGF ligand for 15 min |
| Result: | Reduced the phospho-tyrosine level in a dose-dependent manner. |
In Vivo
UNC2881 (3 mg/kg; p.o.; single dose) has high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability, displays terminal half-life of 0.80 h
[1]
.
UNC2881 (3 mg/kg; i.v.; injected with VSV on days -3, -2, -1, and 0) limits Mertk signaling, and promotes the antiviral immune response, reducing the viral replication of vesicular stomatitis virus (VSV) in infected mice
[2]
.
Pharmacokinetics of UNC2881 in mice
[1]
| Route | Dose (mg/kg) | T 1/2 (h) | T max (h) | C max (ng/mL) | AUC last (ng·h/mL) | CL obs (mL/min) | V ss (L/kg) | F (%) |
| IV | 3 | 0.8 | 2609 | 527 | 94.5 | 1.65 | ||
| PO | 3 | 0.30 | 90.0 | 71.7 | 14 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6 mice (7-10 weeks old) [2] |
| Dosage: | 3 mg/kg |
| Administration: | Intravenous injection; infected with 2×10 8 PFU vesicular stomatitis virus (VSV) (i.v.) on days -3, -2, -1, and 0 |
| Result: | Reduced VSV replication in spleen, liver, kidney, lung. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 44 mg/mL ( 94.91 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1571 mL | 10.7856 mL | 21.5713 mL |
| 5 mM | 0.4314 mL | 2.1571 mL | 4.3142 mL |
| 10 mM | 0.2157 mL | 1.0786 mL | 2.1571 mL |
References
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.