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Merck
CN

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).

别名:

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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关于此项目

经验公式（希尔记法）:
C22H29FN6
分子量:
396.50
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze
protect from light

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产品名称

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).

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

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

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.

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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