SML3620
UNC2250
≥98% (HPLC)
Sinónimos:
UNC 2250, UNC-2250, trans-4-((2-(Butylamino)-5-(5-(morpholinomethyl)pyridin-2-yl)pyrimidin-4-yl)amino)cyclohexanol
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About This Item
Fórmula empírica (notación de Hill):
C24H36N6O2
Número de CAS:
Peso molecular:
440.58
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.25
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Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Biochem/physiol Actions
UNC2250 is a potent and highly selective Mer receptor tyrosine kinase inhibitor (MerTK IC50 = 1.7 nM; Tyro3/Axl IC50 = 100/270 nM) that reduces endogenous Mer phosphorylation level (697 B-ALL IC50 = 9.8 nM post 1h treatment) and blocks ligand-stimulated activation of a chimeric EGFR-Mer in cells. UNC2250 inhibits colony-forming potential in rhabdoid (by 36% at 100 nM; BT-12 cells) and NSCLC tumor cells (Colo699 IC50 = 100 nM) with good pharmacokinetic properties. UNC2250 is reported to reduce mortality in a murine LPS-induced acute lung injury (ALI) model (2 mg/kg i.v. )
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificados de análisis (COA)
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Yuanfeng Du et al.
Brain research, 1766, 147525-147525 (2021-05-20)
The NLR family pyrin domain-containing 3 (NLRP3) multiprotein complex is associated with neuroinflammation and poor prognosis after subarachnoid hemorrhage (SAH). Accumulating evidence shows that Mer tyrosine kinase (MerTK) alleviates inflammatory responses via a negative feedback mechanism. However, the contribution and
The suppressive effects of Mer inhibition on inflammatory responses in the pathogenesis of LPS-induced ALI/ARDS
Science Signaling, 15(724) (2022)
Weihe Zhang et al.
Journal of medicinal chemistry, 56(23), 9683-9692 (2013-11-08)
Abnormal activation or overexpression of Mer receptor tyrosine kinase has been implicated in survival signaling and chemoresistance in many human cancers. Consequently, Mer is a promising novel cancer therapeutic target. A structure-based drug design approach using a pseudo-ring replacement strategy
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