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445835-M

Mer RTK Inhibitor, UNC569

Mer RTK Inhibitor, UNC569, 1350547-65-7 is a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM).

Synonym(s):

Mer RTK Inhibitor, UNC569, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-(( trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine

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About This Item

Empirical Formula (Hill Notation):
C22H29FN6
Molecular Weight:
396.50
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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Quality Segment

100

assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

beige

solubility

DMSO: 100 mg/mL, water: 2.5 mg/mL (with gentle warming)

storage temp.

2-8°C

General description

An orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM) with ~10-fold greater selectivity over other TAM family kinases (IC50 = 37 and 48 nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30 nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC50 of 141 nM. Exhibits desirable pharmacokinetic profile and efficacy in mice.

Physical form

Supplied as a trifluoroacetate salt.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable fo rup to 6 months at -20°C.

Other Notes

Liu, J., et al. 2012. ACS Med. Chem. Lett.3, 129.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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