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Safety Information

SML3620

Sigma-Aldrich

UNC2250

≥98% (HPLC)

Synonym(s):

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

Empirical Formula (Hill Notation):
C24H36N6O2
CAS Number:
1493694-70-4
Molecular Weight:
440.58
MDL number:
MFCD27992060
UNSPSC Code:
12352200
NACRES:
NA.25

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

SMILES string

N4(CCOCC4)Cc1cnc(cc1)c2c(nc(nc2)NCCCC)N[C@@H]3CC[C@H](CC3)O

InChI key

HSYSSKFCQHXOBP-MXVIHJGJSA-N

Biochem/physiol Actions

Potent and highly selective Mer receptor tyrosine kinase (MerTK) inhibitor in vitro and in vivo.
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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000234328
0000234329
0000228815
0000228815
0000234329

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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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