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Chemical Structure| 1493694-70-4 Chemical Structure| 1493694-70-4

Structure of UNC2250
CAS No.: 1493694-70-4

Chemical Structure| 1493694-70-4

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CAS No.: 1493694-70-4

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UNC2250 is an inhibitor of Mer with IC50 of 1.7 nM.

4.5 *For Research Use Only !

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Product Details of UNC2250

CAS No. :1493694-70-4
Formula : C24H36N6O2
M.W : 440.58
SMILES Code : O[C@H]1CC[C@H](NC2=NC(NCCCC)=NC=C2C3=NC=C(CN4CCOCC4)C=C3)CC1
MDL No. :MFCD27992060
InChI Key :HSYSSKFCQHXOBP-UHFFFAOYSA-N
Pubchem ID :73211763

Safety of UNC2250

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of UNC2250

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
697 B-ALL cells 9.8 nM (IC50) 1 hour Inhibition of Mer tyrosine kinase activation PMC3980660
JVM-2 cells 4 μM 24 hours Inhibited invasive abilities of JVM-2 cells PMC5859520
Mino cells 2 or 4 μM 24 hours Inhibited invasive abilities of Mino cells PMC5859520
Z-138 cells 2 or 4 μM 24 hours Inhibited invasive abilities of Z-138 cells PMC5859520
Raw264.7 macrophages 5 μM 24 hours Reduced FDT phagocytosis and enhanced STING pathway activation PMC11120279
BT-12 rhabdoid tumor cells 10 nM to 3 μM 3 weeks Inhibition of colony formation PMC3980660
Z-138 cells 1, 2, 3, 4, 5 μM 1 hour Inhibited phosphorylation of MerTK and downstream signaling pathways AKT and p38 PMC5859520
BMDMs (bone marrow-derived macrophages) 5 μM 24 hours Inhibited MerTK-mediated efferocytosis and promoted M1-like polarization PMC11120279
Human umbilical vein endothelial cells (HUVEC) 5 μM 24 hours UNC2250 significantly suppressed the upregulation of ICAM-1 and VCAM-1 induced by Gas6 or GVHD sera. PMC6650735
Human platelets 5 μM 4 hours UNC2250 decreased the mRNA expression of Gas6 but did not affect the mRNA expression of Mer. PMC6650735
Vascular smooth muscle cells (VSMCs) 1 μM 48 hours UNC2250 significantly inhibited csEV-induced proliferation and migration of VSMCs PMC10104856

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice MC38 colon cancer peritoneal metastasis model Intraperitoneal injection 25 mg/kg Administered on Days 3, 7, and 11, sacrificed on Day 22 Combination with FDT vaccine significantly inhibited tumor growth and promoted M1-like macrophage polarization PMC11120279
NOD/SCID mice Z-138 cell-derived xenograft model Oral gavage 25, 50, 75 mg/kg Once daily for 10 days Evaluated the anti-tumor effects of UNC2250 in Z-138 cell-derived xenograft model PMC5859520
Mice Hematopoietic stem cell transplantation model Intravenous 3 mg/kg Single dose, observed until day 21 UNC2250 markedly attenuated the histopathological characteristics of GVHD and TA-TMA, including hepatocellular necrosis, fibrosis, and thrombus formation. PMC6650735

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.13mL

22.70mL

4.54mL

2.27mL

References

 

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