| Identification | Back Directory | [Name]
UNC2881 | [CAS]
1493764-08-1 | [Synonyms]
110849
CS-1177
UNC2881
UNC2881 USP/EP/BP
UNC 2881; UNC-2881
N-(4-(1H-Imidazol-1-yl)benzyl)-2-(butylamino)-4-(((1r,4r)-4-hydroxycyclohexyl)amino)pyrimidine
N-(4-(1H-Imidazol-1-yl)benzyl)-2-(butylamino)-4-((trans-4-hydroxycyclohexyl)amino)pyrimidine-5-carboxamide
N-(4-(1H-iMidazol-1-yl)benzyl)-2-(butylaMino)-4-(((1r,4r)-4-hydroxycyclohexyl)aMino)pyriMidine-5-carboxaMide
2-(Butylamino)-4-[(trans-4-hydroxycyclohexyl)amino]-N-[[4-(1H-imidazol-1-yl)phenyl]methyl]-5-pyrimidinecarboxamide
5-Pyrimidinecarboxamide, 2-(butylamino)-4-[(trans-4-hydroxycyclohexyl)amino]-N-[[4-(1H-imidazol-1-yl)phenyl]methyl]-
N-(4-(1H-imidazol-1-yl)benzyl)-2-(butylamino)-4-((1r,4r)-4-hydroxycyclohexylamino)pyrimidine-5-carboxamide UNC2881 | [Molecular Formula]
C25H33N7O2 | [MDL Number]
MFCD28142814 | [MOL File]
1493764-08-1.mol | [Molecular Weight]
463.575 |
| Chemical Properties | Back Directory | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥13.55 mg/mL in DMSO | [form ]
solid | [pka]
12.70±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
UNC2881 is an inhibitor of Mer (IC50 = 4.3 nM), a member of the TAM family of receptor tyrosine kinases. It is selective for Mer over the remaining TAM family members Axl and TYRO3 (IC50s = 360 and 250 nM, respectively). UNC2881 inhibits phosphorylation of Mer in 697 B-ALL acute lymphoblastic leukemia cells (IC50 = 21.9 nM). It inhibits platelet aggregation and ATP release induced by type I equine fibrillar collagen in isolated human platelet-rich plasma when used at a concentration of 3 μM. | [Uses]
UNC2881 is a specific Mer tyrosine kinase inhibitor. It inhibits collagen-stimulated platelet aggregation. | [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) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUClast (ng·h/mL) | CLobs (mL/min) | Vss (L/kg) | F (%) | | IV | 3 | 0.8 | | 2609 | 527 | 94.5 | 1.65 | | | PO | 3 | | 0.30 | 90.0 | 71.7 | | | 14 |
| Animal Model: | C57BL/6 mice (7-10 weeks old)[2] | | Dosage: | 3 mg/kg | | Administration: | Intravenous injection; infected with 2×108 PFU vesicular stomatitis virus (VSV) (i.v.) on days -3, -2, -1, and 0 | | Result: | Reduced VSV replication in spleen, liver, kidney, lung. |
| [target]
Mer tyrosine kinase | [IC 50]
Axl; Mer | [storage]
Store at +4°C | [References]
[1]. zhang w, mciver al, stashko ma, et al. discovery of mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. j med chem, 2013, 56(23): 9693-9700. |
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| Company Name: |
ChemShuttle, Inc.
|
| Tel: |
0510-83588313-811 18800520310 |
| Website: |
www.jiehuapharma.com/ |
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